Synopsis of pharmaceutical chemistry. Pharmaceutical chemistry - Glushchenko N.N. Professional activity of graduates

Year of issue: 2004

Genre: Pharmacology

Format: DjVu

Quality: Scanned pages

Description: The volume of the material presented in the textbook "Pharmaceutical Chemistry" significantly exceeds the content curriculum for pharmaceutical schools. The authors deliberately went for such an extension, taking into account the examples of some foreign and domestic textbooks, where the subject is presented with the involvement of information about the latest scientific achievements. This allows the teacher to independently select the material recommended by the program in accordance with the established traditions of the educational institution. Pay attention to high level preparation of some students, a broader presentation of the subject will help them in studying some sections.
A feature of the presentation of the material is the use of data from the Russian Encyclopedia of Medicines (2003), the US Pharmacopoeia (USP-24), the European Pharmacopoeia (EP-2002), the British Pharmacopoeia (BF-2001), scientific publications of recent years and current scientific periodicals on the chemistry of drugs (LS). The use of foreign pharmacopoeias in the preparation of the textbook is quite justified, since the domestic Pharmacopoeia has not been republished in full since 1968, and the receipt of temporary pharmacopoeial articles educational institutions associated with tangible financial costs. In addition, in Russia, as is known, work is underway to introduce GP (Good Practice - Good Practice) methods into pharmacy at all stages of the drug's "life". Good Pharmaceutical Practice has crossed the borders of the US and Europe. Therefore, the future domestic Pharmacopoeia will certainly absorb a lot of positive things that have been achieved and used in countries that are members of the European Pharmacopoeia (EP) community as members and observers.
It is quite possible that the integration of countries at all levels will facilitate the task of Russia joining the European Pharmacopoeia, as 27 states have already done. Such unity, coordination (harmonization) of the pharmacopoeia of different countries is not accidental: the medicine that we sell or purchase has ceased to belong to one country. Substances, excipients, reagents, packaging, quality control methods for all components, analysis equipment are the fruit of the work of specialists from different countries. Ultimately, drugs may end up on the market of a completely different state. Unfortunately, at present, the requirements applied in different countries for assessing the safety and efficacy of drugs are different. That is why the issue of harmonizing the Pharmacopoeia of various states, both producing drugs and using them on their territory, is so important.
Approaches unconventional for pharmaceutical chemistry have been used to characterize the biological activity of drugs in biological media. Thus, the authors applied the methods of "pH-diagrams" and "pH-potential" diagrams for acid-base and redox processes involving drugs. When describing the features of synthesis, analysis, storage conditions, therapeutic activity, fundamental laws were used, in particular, the law of mass action for equilibrium and the law of mass action for speed.
For the first time in the educational literature for assessing the pyrogenicity of injectable dosage forms, the LAL test is described, which is included in the latest pharmacopoeial editions and meets the requirements of GMP (Good Manufacturing Practice - Good Manufacturing Practice).
Unfortunately, some issues important for pharmaceutical chemistry were left out of the exposition, which is explained by the limitations of the volume of the publication.
The textbook "Pharmaceutical Chemistry" was written by a team of authors representing three interrelated areas - biology, chemistry, and pharmacy.
Glushchenko Natalia Nikolaevna - Doctor of Biological Sciences, Head. Laboratory of Problems of the Impact of Heavy Metals on Biosystems of the Institute of Energy Problems chemical physics RAN.
Pleteneva Tatyana Vadimovna - professor, doctor chemical sciences, Head of the Department of Pharmaceutical and Toxicological Chemistry, Faculty of Medicine, Peoples' Friendship University of Russia.
Popkov Vladimir Andreevich - Professor, Doctor of Pharmaceutical Sciences, Doctor of Pedagogical Sciences, Academician of the Academy of Education, Head of the Department of General Chemistry of the Moscow medical academy them. THEM. Sechenov.
The authors will be grateful for critical comments and suggestions for improving the content of the textbook.

The textbook "Pharmaceutical Chemistry" is intended for students of secondary medical schools and colleges studying in the specialty 0405 "Pharmacy". Separate sections of the textbook can be used by university students and students of advanced training faculties.

"Pharmaceutical Chemistry"

INTRODUCTION TO DRUG CHEMISTRY
Pharmaceutical Chemistry Content

1. Relationship of pharmaceutical chemistry with other sciences
2. Basic terms and concepts used in pharmaceutical chemistry
3. Classification of medicines

Obtaining and researching medicines. Basic provisions and documents regulating pharmaceutical analysis

1. Sources of obtaining medicines
2. The main directions of search and creation of medicinal substances
3. Criteria for the quality of medicines
4. Standardization of medicines. Control and Permit System for Quality Assurance of Medicinal Products
5. Methods of drug analysis
6. General information about methods and tests of drugs for toxicity, sterility and microbiological purity
7. Determination of bioequivalence and bioavailability of drugs by kinetic methods
8. Shelf life and stabilization of medicines
9. Intra-pharmacy drug control

CHEMISTRY OF DRUGS OF INORGANIC NATURE
Medicines s-elements

1. General characteristics of the group
2. Magnesium Drug Chemistry
3. Chemistry of Calcium Drugs
4. Chemistry of barium drugs

Medicines of p-elements

1. Medicines of p-elements of group VII
2. Medicines of p-elements of group VI
3. Medicines of group V
4. Medicines of p-elements of group IV
5. Medicines p-elements III groups

Medicines of d- and f-elements

1. Drugs of d-elements of group I
2. Drugs of d-elements of group II
3. Drugs of d-elements of group VIII
4. f-element drugs

Radiopharmaceuticals
Homeopathic medicines
CHEMISTRY OF DRUGS OF ORGANIC NATURE
Medicinal products of organic nature and features of their analysis

1. Classification
2. Analysis

Acyclic drugs

1. Alcohols
2. Aldehydes
3. Carbohydrates
4. Ethers
5. carboxylic acids. Aminocarboxylic acids and their derivatives

Carbocyclic drugs

1. Aromatic amino alcohols
2. Phenols, quinones and their derivatives
3. Aromatic acids, hydroxy acids and their derivatives
4. Aromatic amino acids
5. Aromatic acetamine derivatives

Heterocyclic drugs

1. Furan derivatives
2. Pyrazole derivatives
3. Imidazole derivatives
4. Pyridine derivatives
5. Pyrimidine derivatives
6. Tropane derivatives
7. Quinoline derivatives
8. Isoquinoline derivatives
9. Purine derivatives
10. Isoalloxazine derivatives

Antibiotics

1. Antibiotics with an azetidine core (p-lactamides)
2. Tetracycline antibiotics
3. Antibiotics - aminoglycosides
4. Aromatic antibiotics - derivatives of nitrophenylalkylamines (chloramphenicol group)
5. Antibiotics macrolides and azalides

Bibliography

. activity, physical and chem. Saint-va, as well as methods of qualities, and quantities, analysis. Main problems of pharmaceutical chemistry: obtaining biologically active in-in and their research; identification of patterns between the structure and biol. chemical activity. conn.; improving the quality assessment of lek. Wed-in to ensure their max, therapeutic. efficiency and safety; research and development of methods for the analysis of lek. in-in in biol. objects for toxicology. and eco-go-pharmaceutical. monitoring.

F pharmaceutical chemistry is closely related to special. disciplines, such as technology lek. forms, pharmacognosy (studies lek. raw materials grows, and animal origin), organization and economics of pharmacy, and is included in the complex of disciplines that form the basic pharmaceutical. education.

The use of chem. B-B as a lek. Wed-in was already carried out in ancient and medieval medicine (Hippocrates, Galen, Avicenna). The emergence of pharmaceutical chemistry is usually associated with the name of Paracelsus (he contributed to the introduction of chemical preparations into medicine) and subsequent discoveries of the therapeutic effect of MH. chem. conn. and elements (K. Scheele, L. Vauquelin, B. Courtois), as well as with the works of M. V. Lomonosov and his school on methods for obtaining and methods for studying the quality of lek. Wed-in. The formation of pharmaceutical chemistry as a science is attributed to the 2nd floor. 19th century The milestone periods in the development of pharmaceutical chemistry include the 90s. 19th century (obtaining aspirin, phenacetin, barbiturates), 1935-37 (use of sulfonamides), 1940-42 (discovery of penicillin), 1950 (psychotropic drugs of the pheno-thiazine group), 1955-60 (semi-synthetic penicillins and later cephalosporins), 1958 (b-blockers) and the 80s. (antibacterial drugs of the fluoroquinolone group).

Prerequisites for the search for lek. Wed-va usually serve as data on biol. activity in-va, the similarity of its structure with biogenic physiologically active substances (for example, decomp. metabolites, hormones). Sometimes lek. Wed-va can be obtained by modifying biogenic Comm. (e.g. animal steroid hormones) or due to research into, alien to the human body (eg, derivatives of phenothiazine and benzodiazepine).

Synthetic in-va receive by org. synthesis or apply methods of microbiological synthesis using the achievements of genetic engineering.

Methods for studying the content of lek are important in pharmaceutical chemistry. in-va in the preparation, its purity, and other factors underlying the quality indicators. Analysis of lek. Wed, or pharmaceutical. analysis, aims to identify and quantify DOS. ingredient(s) in a drug. Pharmaceutical pharmacological analysis. drug action (appointment, dosage, route of administration) provides for the determination of impurities, auxiliary. and accompanying in-in in lek. forms. Lek. Wed-va assess comprehensively, for all indicators. Therefore, the expression "pharmacopoeial quality" means the suitability of the drug for use in medicine.

Compliance lek. cf-in the required quality level is set using standard methods analysis, usually specified in the pharmacopoeia. For identification of lek. in-in along with group chem. p-tions use NMR and IR spectroscopy. For the analysis of multicomponent lek. formsusually thin layer chromatography is used. Purity tests are designed to confirm the absence (within the method used) of individual impurities, and in some cases to assess their content. For this purpose, chromatography is used. methods, often combined with optical ones.

Pharmacokinetic. characteristics of lek. avg (the effect of the drug and its distribution in the body over time) are extremely important and mandatory information that ensures the rational and effective use of drugs, allow you to expand knowledge regarding

- this is a science based on the general laws of chemical sciences, studying issues related to medicinal substances: their composition and structure, production and chemical nature, the influence of individual structural features of their molecules on the nature of the action on the body, chemical and physical properties medicinal substances, as well as methods for controlling their quality, storing medicines.

Translation into English - " pharmaceutical chemistry«.

Pharmaceutical chemistry plays a leading role along with related pharmaceutical sciences (, toxicological chemistry,). For a more thorough study of the topic, carefully read the above articles!

What is Pharmaceutical Chemistry (Pharmchemistry)?

On the other hand, it can be said that it is a specialized science based on the knowledge of related chemical (organic, inorganic, analytical, physical and colloidal chemistry), as well as biomedical (, biological chemistry, physiology) disciplines.

Knowledge of biological disciplines reveals the understanding of complex physiological processes occurring in the body, based on chemical and physical reactions, which makes it possible to more rationally use medicinal substances, observe their action in the body and, on the basis of this, change the structure of the molecules of the created medicinal substances in the right direction in order to obtain the desired pharmacological effect.

Of great importance in pharmaceutical chemistry are methods for studying the content of medicinal substances in the preparation, their purity and other factors underlying the quality indicators. Drug analysis (pharmaceutical analysis) aims to identify and quantify the main components in a drug.

Pharmaceutical analysis, depending on the pharmacological action of the drug (appointment, dosage, route of administration), involves the determination of impurities, concomitants and excipients in dosage forms.

It is important that medicines are evaluated in a comprehensive manner for all indicators. Therefore, based on the results of the pharmacological analysis of drugs, a conclusion is issued on the possibility of using them in medical practice.

The study of the structure of a drug molecule, in addition, the development of methods for synthesis and analysis is impossible without knowledge of organic and analytical chemistry. The pharmacokinetic characteristics of drugs represent extremely important and mandatory information that ensures the rational and effective use of drugs, and allows expanding knowledge regarding the specificity of their action.

Compatibility of medicinal substances in the prescription, expiration dates, manufacturing methods, storage and dispensing conditions of drugs connects pharmaceutical chemistry with drug technology, economics and organization of pharmacy. But only a competent specialist with knowledge of pharmaceutical chemistry (pharmacist-analyst) solves these issues.

Modern pharmaceutical chemistry (pharma chemistry).

On the present stage pharmaceutical chemistry is closely related to both physics and mathematics, when these sciences are used to conduct physicochemical methods of drug analysis and calculations in pharmaceutical analysis, therefore, in conjunction with many sciences, it is of great importance both in pharmacy and in medicine in general.

Thanks to the achievements of modern pharmaceutical chemistry, medicines have been created that provide our healthcare with effective and safe methods of treating many diseases. However, along with this, there are areas in medicine where there is still a lot of work to be done to create new highly effective drugs, these are: oncological, cardiovascular and viral diseases.

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Pharmaceutical chemistry and pharmaceutical analysis

Introduction

1. Characteristics of pharmaceutical chemistry as a science

1.1 Subject and tasks of pharmaceutical chemistry

1.2 Relationship of pharmaceutical chemistry with other sciences

1.3 Pharmaceutical chemistry objects

1.4 Contemporary Issues pharmaceutical chemistry

2. History of development of pharmaceutical chemistry

2.1 The main stages in the development of pharmacy

2.2 Development of pharmaceutical chemistry in Russia

2 .3 Development of pharmaceutical chemistry in the USSR

3. Pharmaceutical analysis

3.1 Basic principles of pharmaceutical and pharmacopoeial analysis

3.2 Pharmaceutical Analysis Criteria

3.3 Mistakes during Pharmaceutical Analysis

3.4 General principles for testing the authenticity of medicinal substances

3.5 Sources and causes of poor quality of medicinal substances

3.6 General requirements for purity testing

3.7 Methods for studying the quality of medicines

3.8 Validation of methods of analysis

findings

List of used literature

Introduction

Among the tasks of pharmaceutical chemistry - such as the modeling of new drugs, drugs and their synthesis, the study of pharmacokinetics, etc., the analysis of the quality of drugs occupies a special place. The State Pharmacopoeia is a collection of mandatory national standards and regulations that normalize the quality of drugs.

Pharmacopoeial analysis of medicines includes quality assessment for a variety of indicators. In particular, the authenticity of the medicinal product is established, its purity is analyzed, and a quantitative determination is carried out. Initially, only chemical methods were used for such analysis; authenticity tests, impurity reactions and titration in quantitation.

Over time, not only the level of technical development of the pharmaceutical industry has increased, but also the requirements for the quality of medicines have changed. AT last years there has been a trend towards a transition to the expanded use of physical and physico-chemical methods of analysis. In particular, spectral methods are widely used - infrared and ultraviolet spectrophotometry, spectroscopy nuclear magnetic resonance and others. The methods of chromatography (high-performance liquid, gas-liquid, thin-layer), electrophoresis, etc. are actively used.

The study of all these methods and their improvement is one of the most important tasks of pharmaceutical chemistry today.

1. Characteristics of pharmaceutical chemistry as a science

1.1 Subject and tasks of pharmaceutical chemistry

Pharmaceutical chemistry is a science that, based on the general laws of chemical sciences, explores the methods of obtaining, structure, physical and chemical properties of medicinal substances, the relationship between their chemical structure and effect on the body, quality control methods and changes that occur during storage.

The main methods for the study of medicinal substances in pharmaceutical chemistry are analysis and synthesis - dialectically closely related processes that complement each other. Analysis and synthesis are powerful means of understanding the essence of phenomena occurring in nature.

The tasks facing pharmaceutical chemistry are solved using classical physical, chemical and physicochemical methods, which are used both for the synthesis and for the analysis of medicinal substances.

To learn pharmaceutical chemistry, the future pharmacist must have deep knowledge in the field of general theoretical chemical and biomedical disciplines, physics, and mathematics. Strong knowledge in the field of philosophy is also necessary, because pharmaceutical chemistry, like other chemical sciences, deals with the study of the chemical form of the motion of matter.

1.2 Relationship of pharmaceutical chemistry with other sciences

Pharmaceutical chemistry is an important branch of chemical science and is closely related to its individual disciplines (Fig. 1). Using the achievements of basic chemical disciplines, pharmaceutical chemistry solves the problem of targeted search for new drugs.

For example, modern computer methods make it possible to predict the pharmacological action (therapeutic effect) of a drug. A separate direction has been formed in chemistry associated with the search for one-to-one correspondences between the structure of a chemical compound, its properties and activity (QSAR-, or KKSA-method - quantitative structure-activity correlation).

The relationship "structure - property" can be detected, for example, by comparing the values topological index(indicator reflecting the structure of the medicinal substance) and therapeutic index (the ratio of the lethal vine to the effective dose LD50/ED50).

Pharmaceutical chemistry is also related to other, non-chemical disciplines (Fig. 2).

So, knowledge of mathematics allows, in particular, to apply the metrological assessment of the results of the analysis of drugs, computer science provides timely receipt of information about drugs, physics - the use of fundamental laws of nature and the use of modern equipment in analysis and research.

There is an obvious relationship between pharmaceutical chemistry and special disciplines. The development of pharmacognosy is impossible without the isolation and analysis of biologically active substances of plant origin. Pharmaceutical analysis accompanies individual stages of technological processes for obtaining drugs. Pharmacoeconomics and pharmacy management come into contact with pharmaceutical chemistry when organizing a system for standardization and quality control of medicines. Determination of the content of drugs and their metabolites in biological media in equilibrium (pharmacodynamics and toxicodynamics) and in time (pharmacokinetics and toxicokinetics) demonstrates the possibilities of using pharmaceutical chemistry to solve problems of pharmacology and toxicological chemistry.

A number of disciplines of biomedical profile (biology and microbiology, physiology and pathophysiology) represent the theoretical basis for the study of pharmaceutical chemistry.

A close relationship with all of these disciplines provides a solution to modern problems of pharmaceutical chemistry.

Ultimately, these problems come down to the creation of new, more effective and safe drugs and the development of methods for pharmaceutical analysis.

1.3 Pharmaceutical chemistry facilities

The objects of pharmaceutical chemistry are extremely diverse in terms of chemical structure, pharmacological action, mass, number of components in mixtures, the presence of impurities and related substances. These objects include:

Medicinal substances (LM) -- (substances) are individual substances of plant, animal, microbial or synthetic origin that have pharmacological activity. Substances are intended for obtaining medicines.

Medicines (PM) -- inorganic or organic compounds, possessing pharmacological activity, obtained by synthesis, from plant materials, minerals, blood, blood plasma, organs, tissues of a human or animal, as well as using biological technologies. Drugs also include biologically active substances (BAS) of synthetic, plant or animal origin, intended for the production or manufacture of medicines. Dosage form (DF) -- attached to the drug or MPC convenient for use in the state in which the desired therapeutic effect is achieved.

Medicinal preparations (MP) - dosed drugs in a specific LF, ready for use.

All of these drugs, drugs, drugs and drugs can be both domestic and foreign production, approved for use in Russian Federation. The given terms and their abbreviations are official. They are included in the OSTs and are intended for use in pharmaceutical practice.

The objects of pharmaceutical chemistry also include starting products used to obtain drugs, intermediate and by-products of synthesis, residual solvents, excipients and other substances. In addition to patented drugs, the objects of pharmaceutical analysis are generics (generic drugs). For the developed original drug, the pharmaceutical manufacturing company receives a patent, which confirms that it is the property of the company for a certain period (usually 20 years). The patent provides the exclusive right to implement it without competition from other manufacturers. After the expiration of the patent, the free production and sale of this drug is allowed to all other companies. It becomes a generic drug, or generic, but must be absolutely identical to the original. The difference is only in the difference in the name given by the manufacturer. A comparative evaluation of a generic and original drug is carried out according to pharmaceutical equivalence (equal content of the active ingredient), bioequivalence (equal concentrations of accumulation when taken in the blood and tissues), therapeutic equivalence (same efficacy and safety when administered under equal conditions and doses). The advantages of generics are a significant reduction in costs compared to the creation of the original drug. However, their quality is assessed in the same way as the corresponding original drugs.

The objects of pharmaceutical chemistry are also various finished medicinal products (FPP) of the factory and dosage forms of pharmaceutical production (DF), medicinal plant raw materials (MP). These include tablets, granules, capsules, powders, suppositories, tinctures, extracts, aerosols, ointments, patches, eye drops, various injectable dosage forms, ophthalmic medicinal films (OMFs). The content of these and other terms and concepts is given in the terminological dictionary of this textbook.

Homeopathic medicines are single- or multi-component medicinal products containing, as a rule, microdoses of active compounds produced according to a special technology and intended for oral, injection or topical use in the form of various dosage forms.

An essential feature of the homeopathic method of treatment is the use of small and ultra-low doses of drugs, prepared by stepwise serial dilution. This determines the specific features of the technology and quality control of homeopathic medicines.

The range of homeopathic drugs consists of two categories: monocomponent and complex. For the first time, homeopathic drugs were included in the State Register in 1996 (in the amount of 1192 monopreparations). Subsequently, this nomenclature expanded and now includes, in addition to 1192 monopreparations, 185 domestic and 261 foreign homeopathic drugs. Among them are 154 substances-tinctures of matrix, as well as various dosage forms: granules, sublingual tablets, suppositories, ointments, creams, gels, drops, injection solutions, lozenges for resorption, oral solutions, patches.

Such a large range of homeopathic dosage forms requires high quality requirements. Therefore, their registration is carried out in strict accordance with the requirements of the licensing system, as well as for allopathic drugs with subsequent registration with the Ministry of Health. This provides a reliable guarantee of the effectiveness and safety of homeopathic drugs.

Biologically active additives (BAA) to food (nutraceuticals and parapharmaceuticals) are concentrates of natural or identical biologically active substances intended for direct intake or introduction into the composition food products to enrich the human diet. BAA is obtained from vegetable, animal or mineral raw materials, as well as by chemical and biotechnological methods. Dietary supplements include bacterial and enzyme preparations that regulate the microflora of the gastrointestinal tract. Dietary supplements are produced at food, pharmaceutical and biotechnological enterprises in the form of extracts, tinctures, balms, powders, dry and liquid concentrates, syrups, tablets, capsules and other forms. Pharmacies and diet food stores sell dietary supplements. They should not contain strong, narcotic and poisonous substances, as well as VP, not used in medicine and not used in nutrition. Expert assessment and hygienic certification of dietary supplements is carried out in strict accordance with the regulation approved by Order No. 117 of April 15, 1997 “On the procedure for examination and hygienic certification of biologically active food supplements”.

For the first time dietary supplements appeared in medical practice in the United States in the 60s. 20th century Initially, they were complexes consisting of vitamins and minerals. Then they began to include various components of plant and animal origin, extracts and powders, incl. exotic natural products.

When compiling dietary supplements, the chemical composition and dosages of components, especially metal salts, are not always taken into account. Many of them can cause complications. Their effectiveness and safety are not always studied in sufficient volume. Therefore, in some cases, dietary supplements can do harm instead of good, because. their interaction with each other, dosages, side effects, and sometimes even narcotic effect. In the United States from 1993 to 1998, 2621 reports of adverse reactions to dietary supplements were registered, incl. 101 fatalities. Therefore, the WHO decided to tighten control over dietary supplements and impose requirements on their effectiveness and safety similar to the criteria for the quality of medicines.

1.4 Modern problems of pharmaceutical chemistry

The main problems of pharmaceutical chemistry are:

* creation and research of new medicines;

* development of methods for pharmaceutical and biopharmaceutical analysis.

Creation and research of new drugs. Despite the huge arsenal of available drugs, the problem of finding new highly effective drugs remains relevant.

The role of drugs is constantly growing in modern medicine. This is due to a number of reasons, the main ones being:

ѕ a number of serious diseases are not yet cured by drugs;

* long-term use of a number of drugs forms tolerant pathologies, to combat which new drugs with a different mechanism of action are needed;

* the processes of evolution of microorganisms lead to the emergence of new diseases, the treatment of which requires effective drugs;

* some of the drugs used cause side effects, and therefore it is necessary to create safer drugs.

The creation of each new original drug is the result of the development of fundamental knowledge and achievements of medical, biological, chemical and other sciences, intensive experimental research, and the investment of large material costs. The successes of modern pharmacotherapy were the result of deep theoretical studies of the primary mechanisms of homeostasis, the molecular basis of pathological processes, the discovery and study of physiologically active compounds (hormones, mediators, prostaglandins, etc.). Achievements in the study of the primary mechanisms of infectious processes and the biochemistry of microorganisms contributed to the development of new chemotherapeutic agents. The creation of new drugs turned out to be possible on the basis of achievements in the field of organic and pharmaceutical chemistry, the use of a complex of physicochemical methods, and technological, biotechnological, biopharmaceutical and other studies of synthetic and natural compounds.

The future of pharmaceutical chemistry is connected with the demands of medicine and further progress in research in all these areas. This will create the prerequisites for opening up new areas of pharmacotherapy, obtaining more physiological, harmless drugs both with the help of chemical or microbiological synthesis, and by isolating biologically active substances from plant or animal raw materials. Priority developments are in the field of obtaining insulin, growth hormones, drugs for the treatment of AIDS, alcoholism, and the production of monoclonal bodies. Active research is being carried out in the field of creating other cardiovascular, anti-inflammatory, diuretic, neuroleptic, anti-allergic drugs, immunomodulators, as well as semi-synthetic antibiotics, cephalosporins and hybrid antibiotics. The most promising is the creation of drugs based on the study of natural peptides, polymers, polysaccharides, hormones, enzymes and other biologically active substances. The identification of new pharmacophores and targeted synthesis of generations of drugs based on previously unexplored aromatic and heterocyclic compounds related to the biological systems of the body are extremely important.

The production of new synthetic drugs is practically limitless, since the number of synthesized compounds increases with their molecular weight. For example, the number of even the simplest compounds of carbon with hydrogen with a relative molecular weight 412 exceeds 4 billion substances.

In recent years, the approach to the process of creating and researching synthetic drugs has changed. From a purely empirical "trial and error" method, researchers are increasingly moving to the use of mathematical methods for planning and processing the results of experiments, the use of modern physical and chemical methods. This approach opens up wide opportunities for predicting the likely types of biological activity of synthesized substances, reducing the time for creating new drugs. In the future, the creation and accumulation of data banks for computers, as well as the use of computers to establish the relationship between chemical structure and pharmacological action of synthesized substances. Ultimately, these works should lead to the creation of a general theory of the directed design of effective drugs related to the systems of the human body.

The creation of new drugs of plant and animal origin consists of such main factors as the search for new species of higher plants, the study of organs and tissues of animals or other organisms, the establishment of the biological activity of the substances contained in them. chemical substances.

Of no small importance are also the study of new sources of obtaining drugs, the widespread use for their production of waste from chemical, food, woodworking and other industries. This direction is directly related to the economics of the chemical and pharmaceutical industry and will help reduce the cost of drugs. Especially promising is the use of modern methods of biotechnology and genetic engineering for the creation of drugs, which are increasingly being used in the chemical and pharmaceutical industry.

Thus, the modern nomenclature of drugs in various pharmacotherapeutic groups requires further expansion. Created new drugs are promising only if they surpass existing ones in terms of their effectiveness and safety, and meet world requirements in terms of quality. In solving this problem, an important role belongs to specialists in the field of pharmaceutical chemistry, which reflects the social and medical significance of this science. The most widely involving chemists, biotechnologists, pharmacologists and clinicians, comprehensive research in the field of creating new highly effective drugs is carried out within the framework of subprogram 071 "Creation of new drugs by methods of chemical and biological synthesis."

Along with the traditional work on the screening of biologically active substances, the need to continue which is obvious, studies on the directed synthesis of new drugs are gaining more and more weight. Such works are based on the study of the mechanism of pharmacokinetics and drug metabolism; revealing the role of endogenous compounds in biochemical processes that determine one or another type of physiological activity; research possible ways inhibition or activation of enzyme systems. The most important basis for the creation of new drugs is the modification of the molecules of known drugs or natural biologically active substances, as well as endogenous compounds, taking into account their structural features and, in particular, the introduction of "pharmacophore" groups, the development of prodrugs. When developing drugs, it is necessary to achieve an increase in bioavailability and selectivity, regulation of the duration of action by creating transport systems in the body. For targeted synthesis, it is necessary to identify the correlation between the chemical structure, physicochemical properties, and biological activity of compounds, using computer technology to design drugs.

In recent years, the structure of diseases and the epidemiological situation have changed significantly, in highly developed countries the average life expectancy of the population has increased, and the incidence rate among the elderly has increased. These factors have determined new directions in the search for drugs. There was a need to expand the range of drugs for the treatment various kinds neuropsychiatric diseases (parkinsonism, depression, sleep disorders), cardiovascular diseases (atherosclerosis, arterial hypertension, ischemic heart disease, cardiac arrhythmias), diseases of the musculoskeletal system (arthritis, spinal diseases), lung diseases (bronchitis, bronchial asthma). Effective drugs for the treatment of these diseases can significantly affect the quality of life and significantly prolong the active period of people's lives, incl. old age. Moreover, the main approach in this direction is the search for mild drugs that do not cause drastic changes in the basic functions of the body, showing a therapeutic effect due to the influence on the metabolic links of the pathogenesis of the disease.

The main areas of search for new and modernization of existing vital drugs are:

* synthesis of bioregulators and metabolites of energy and plastic metabolism;

* identification of potential drugs during the screening of new products of chemical synthesis;

* synthesis of compounds with programmable properties (modification of the structure in the known series of drugs, resynthesis of natural phytosubstances, computer search for biologically active substances);

* stereoselective synthesis of eutomers and the most active conformations of socially significant drugs.

Development of methods for pharmaceutical and biopharmaceutical analysis. The solution of this important problem is possible only on the basis of fundamental theoretical studies of physical and chemical properties Drugs with a wide use of modern chemical and physico-chemical methods. The use of these methods should cover the entire process from the creation of new drugs to the quality control of the final product of production. It is also necessary to develop new and improved regulatory documentation for drugs and drug products, reflecting the requirements for their quality and ensuring standardization.

On the basis of scientific analysis by the method of expert assessments, the most promising areas of research in the field of pharmaceutical analysis were identified. An important place in these studies will be occupied by work on improving the accuracy of the analysis, its specificity and sensitivity, the desire to analyze very small amounts of drugs, including in a single dose, and also to perform the analysis automatically and in a short time. Undoubted importance is the reduction in labor intensity and the increase in the efficiency of analysis methods. It is promising to develop unified methods for the analysis of drug groups united by the relationship of the chemical structure based on the use of physicochemical methods. Unification creates great opportunities for increasing the productivity of the analytical chemist.

In the coming years, chemical titrimetric methods having a series positive aspects, in particular, the high accuracy of the determinations. It is also necessary to introduce into pharmaceutical analysis such new titrimetric methods as buretless and indicatorless titration, dielectrometric, biamperometric and other types of titration in combination with potentiometry, including in two-phase and three-phase systems.

In recent years, fiber optic sensors (without indicators, fluorescent, chemiluminescent, biosensors) have been used in chemical analysis. They make it possible to remotely study processes, allow determining the concentration without disturbing the state of the sample, and their cost is relatively low. Further development in pharmaceutical analysis will be kinetic methods, which are highly sensitive both in testing purity and quantification.

The laboriousness and low accuracy of biological test methods make it necessary to replace them with faster and more sensitive physicochemical methods. The study of the adequacy of biological and physicochemical methods for the analysis of drugs containing enzymes, proteins, amino acids, hormones, glycosides, antibiotics is a necessary way to improve pharmaceutical analysis. In the next 20-30 years, the leading role will be occupied by optical, electrochemical, and especially modern chromatographic methods, as they most fully meet the requirements of pharmaceutical analysis. Various modifications of these methods will be developed, for example, difference spectroscopy of the type of differential and derivative spectrophotometry. In the field of chromatography, along with gas-liquid chromatography (GLC), high-performance liquid chromatography(HPLC).

The quality of the resulting drugs depends on the degree of purity of the initial products, compliance with the technological regime, etc. Therefore, an important area of ​​research in the field of pharmaceutical analysis is the development of methods for quality control of the initial and intermediate products of drug production (step-by-step production control). This direction follows from the requirements that the OMP rules impose on the production of drugs. Automated methods of analysis will be developed in factory control and analytical laboratories. Significant opportunities in this regard are opened up by the use of automated flow-injection systems for step-by-step control, as well as GLC and HPLC for serial control of FPP. A new step has been taken towards the full automation of all analysis operations, which is based on the use of laboratory robots. Robotics has already found wide use in foreign laboratories, especially for sampling and other auxiliary operations.

Further improvement will require methods for analyzing ready-made, including multicomponent, LF, including aerosols, eye films, multilayer tablets, and spansules. To this end, hybrid methods based on a combination of chromatography with optical, electrochemical and other methods will be widely used. The express analysis of individually manufactured dosage forms will not lose its significance, however, here chemical methods will increasingly be replaced by physicochemical ones. The introduction of simple and sufficiently accurate methods of refractometric, interferometric, polarimetric, luminescent, photocolorimetric analysis and other methods makes it possible to increase the objectivity and speed up the assessment of the quality of medicinal products manufactured in pharmacies. The development of such methods is of great relevance in connection with the problem of combating the falsification of drugs that has arisen in recent years. Along with legislative and legal norms, it is absolutely necessary to strengthen control over the quality of drugs of domestic and foreign production, incl. express methods.

An extremely important direction is the use of various methods of pharmaceutical analysis for the study chemical processes occurring during storage of drugs. Knowledge of these processes makes it possible to solve such actual problems, as the stabilization of drugs and drugs, the development of scientifically based storage conditions for drugs. The practical expediency of such studies is confirmed by their economic significance.

The task of biopharmaceutical analysis includes the development of methods for determining not only drugs, but also their metabolites in biological fluids and body tissues. To solve the problems of biopharmacy and pharmacokinetics, precise and sensitive physicochemical methods for the analysis of drugs in biological tissues and fluids are needed. The development of such methods is among the tasks of specialists working in the field of pharmaceutical and toxicological analysis.

Further development of pharmaceutical and biopharmaceutical analysis is closely related to the use of mathematical methods to optimize drug quality control methods. In various fields of pharmacy, information theory is already used, as well as such mathematical methods, as simplex optimization, linear, non-linear, numerical programming, multivariate experiment, pattern recognition theory, various expert systems.

Mathematical methods of planning an experiment make it possible to formalize the procedure for studying a particular system and, as a result, obtain its mathematical model in the form of a regression equation that includes all the most significant factors. As a result, optimization of the entire process is achieved and the most probable mechanism of its functioning is established.

Increasingly, modern methods of analysis are combined with the use of electronic computers. This led to the emergence at the intersection of analytical chemistry and mathematics of a new science - chemometrics. It is based on the wide use of methods of mathematical statistics and information theory, the use of computers and computers at various stages of choosing an analysis method, its optimization, processing and interpretation of results.

A very revealing characteristic of the state of research in the field of pharmaceutical analysis is the relative frequency of application of various methods. As of 2000, there has been a downward trend in the use of chemical methods (7.7% including thermochemistry). The same percentage of the use of IR spectroscopy and UV spectrophotometry methods. The largest number of studies (54%) were performed using chromatographic methods, especially HPLC (33%). Other methods account for 23% of the work performed. Therefore, there is a steady trend towards expanding the use of chromatographic (especially HPLC) and absorption methods to improve and unify methods for the analysis of drugs.

2. History of development of pharmaceutical chemistry

2.1 The main stages in the development of pharmacy

The creation and development of pharmaceutical chemistry are closely related to the history of pharmacy. Pharmacy originated in ancient times and had a huge impact on the formation of medicine, chemistry and other sciences.

The history of pharmacy is independent discipline, which is studied separately. To understand how and why pharmaceutical chemistry was born in the depths of pharmacy, how the process of its formation took place in independent science, we will briefly consider the individual stages in the development of pharmacy starting from the period of iatrochemistry.

The period of iatrochemistry (XVI - XVII centuries). During the Renaissance, alchemy was replaced by iatrochemistry (medical chemistry). Its founder Paracelsus (1493 - 1541) believed that "chemistry should serve not the extraction of gold, but the protection of health." The essence of the teachings of Paracelsus was based on the fact that the human body is a collection of chemicals and the lack of any of them can cause disease. Therefore, for healing, Paracelsus used chemical compounds of various metals (mercury, lead, copper, iron, antimony, arsenic, etc.), as well as herbal medicines.

Paracelsus conducted a study of the effect on the body of many substances of mineral and vegetable origin. He improved a number of instruments and apparatus for performing analysis. That is why Paracelsus is rightly considered one of the founders of pharmaceutical analysis, and iatrochemistry - the period of the birth of pharmaceutical chemistry.

Pharmacies in the XVI - XVII centuries. were original centers for the study of chemicals. Substances of mineral, plant and animal origin were obtained and studied in them. Here was opened whole line new compounds, the properties and transformations of various metals have been studied. This made it possible to accumulate valuable chemical knowledge and improve the chemical experiment. For 100 years of development of iatrochemistry, science has been enriched with a greater number of facts than alchemy for 1000 years.

The period of the birth of the first chemical theories (XVII - XIX centuries). For the development of industrial production during this period, it was necessary to expand the scope of chemical research beyond the limits of atrochemistry. This led to the creation of the first chemical industries and to the formation of chemical science.

Second half of the 17th century - the period of the birth of the first chemical theory - the theory of phlogiston. With its help, they tried to prove that the processes of combustion and oxidation are accompanied by the release of a special substance - "phlogiston". The theory of phlogiston was created by I. Becher (1635-1682) and G. Stahl (1660-1734). Despite some erroneous assumptions, it was undoubtedly progressive and contributed to the development of chemical science.

In the struggle against the supporters of the phlogiston theory, the oxygen theory arose, which was a powerful impetus in the development of chemical thought. Our great compatriot M.V. Lomonosov (1711 - 1765), one of the first scientists in the world, proved the inconsistency of the phlogiston theory. Despite the fact that oxygen was not yet known, M.V. Lomonosov experimentally showed in 1756 that in the process of combustion and oxidation, it is not decomposition that occurs, but the addition of air "particles" to the substance. Similar results were obtained 18 years later in 1774 by the French scientist A. Lavoisier.

Oxygen was first isolated by the Swedish scientist, pharmacist K. Scheele (1742 - 1786), whose merit was also the discovery of chlorine, glycerin, a number of organic acids and other substances.

Second half of the 18th century was a period of rapid development of chemistry. A great contribution to the progress of chemical science was made by pharmacists, who made a number of remarkable discoveries that are important for both pharmacy and chemistry. So, the French pharmacist L. Vauquelin (1763 - 1829) discovered new elements - chromium, beryllium. Pharmacist B. Courtois (1777 - 1836) discovered iodine in seaweed. In 1807, the French pharmacist Seguin isolated morphine from opium, and his compatriots Pelletier and Caventu were the first to obtain strychnine, brucine, and other alkaloids from plant materials.

The pharmacist Mor (1806 - 1879) did a lot for the development of pharmaceutical analysis. He first used burettes, pipettes, pharmacy scales, which bear his name.

Thus, pharmaceutical chemistry, which originated in the period of iatrochemistry in the 16th century, received its further development in the 17th-18th centuries.

2.2 Development of pharmaceutical chemistry in Russia

The origins of Russian pharmacy. The emergence of pharmacy in Russia is associated with the widespread development of traditional medicine and quackery. Handwritten "healers" and "herbalists" have survived to this day. They contain information about numerous medicines of the plant and animal world. Green shops (XIII - XV centuries) were the first cells of the pharmacy business in Russia. The emergence of pharmaceutical analysis should be attributed to the same period, since there was a need to check the quality of drugs. Russian pharmacies in the XVI - XVII centuries. were a kind of laboratories for the manufacture of not only medicines, but also acids (sulfuric and nitric), alum, vitriol, sulfur purification, etc. Hence, pharmacies were the birthplace of pharmaceutical chemistry.

The ideas of alchemists were alien to Russia, here a genuine craft of making medicines immediately began to develop. Alchemists were involved in the preparation and quality control of medicines in pharmacies (the term "alchemist" has nothing to do with alchemy).

The training of pharmacists was carried out by the first medical school opened in Moscow in 1706. One of the special disciplines in it was pharmaceutical chemistry. Many Russian chemists were educated at this school.

The true development of chemical and pharmaceutical science in Russia is associated with the name of M.V. Lomonosov. On the initiative of M.V. Lomonosov, in 1748 the first scientific chemical laboratory was created, and in 1755 the first Russian university was opened. Together with the Academy of Sciences, these were centers of Russian science, including chemical and pharmaceutical sciences. M.V. Lomonosov owns wonderful words about the relationship between chemistry and medicine: "... A physician cannot be perfect without a satisfied knowledge of chemistry, and all shortcomings, all excesses and encroachments occurring in medical science from them; additions, aversions and corrections from one almost chemistry should hope."

One of the many successors of M.V. Lomonosov was an apothecary student, and then a prominent Russian scientist T.E. Lovits (1757 - 1804). He was the first to discover the adsorption capacity of coal and used it to purify water, alcohol, and tartaric acid; developed methods for obtaining absolute alcohol, acetic acid, grape sugar. Among the numerous works of T.E. Lovits, the development of a microcrystalloscopic method of analysis (1798) is directly related to pharmaceutical chemistry.

A worthy successor to M.V. Lomonosov was the greatest Russian chemist V.M. Severgin (1765-1826). Among his many works highest value for pharmacy have two books published in 1800: "A method for testing the purity and integrity of chemical products of medicinal products" and "A method for testing mineral water". Both books are the first domestic manuals in the field of research and analysis of medicinal substances. Continuing the thought of M.V. Lomonosov, V.M. Severgin emphasizes the importance of chemistry in assessing the quality of drugs: "Without knowledge in chemistry, drug testing cannot be undertaken." The author deeply scientifically selects for the study of drugs only the most accurate and accessible methods of analysis.The procedure and plan for the study of medicinal substances proposed by V.M. Severgin has not changed much and is now used in the preparation of the State Pharmacopoeia. chemical analysis in our country.

The works of the Russian scientist A.P. Nelyubin (1785 - 1858) are rightly called the "Encyclopedia of Pharmaceutical Knowledge". He first formulated scientific foundations pharmacy, performed a number of applied research in the field of pharmaceutical chemistry; improved methods for obtaining salts of quinine, created devices for obtaining ether and for testing arsenic. A.P. Nelyubin conducted extensive chemical studies of Caucasian mineral waters.

Until the 40s of the XIX century. in Russia there were many chemists who made a great contribution to the development of pharmaceutical chemistry with their work. However, they worked separately, there were almost no chemical laboratories, there was no equipment and scientific chemical schools.

The first chemical schools and the creation of new chemical theories in Russia. The first Russian schools of chemistry, founded by A.A. Voskresensky (1809-1880) and N.N. Zinin (1812-1880), played important role in the training of personnel, in the creation of laboratories, had a great influence on the development of the chemical sciences, including pharmaceutical chemistry. A.A. Voskresensky carried out with his students a number of studies directly related to pharmacy. They isolated the alkaloid theobromine, and studied the chemical structure of quinine. The outstanding discovery of N.N. Zinin was the classical reaction of the transformation of aromatic nitro compounds into amino compounds.

D.I.Mendeleev wrote that A.A.Voskresensky and N.N.Zinin are "the founders of the independent development of chemical knowledge in Russia". World fame was brought to Russia by their worthy successors D.I. Mendeleev and A.M. Butlerov.

D.I. Mendeleev (1834 - 1907) is the creator of the Periodic Law and Periodic system elements. The great importance of the Periodic Law for all chemical sciences is well known, but it also contains a deep philosophical meaning, since it shows that all elements form a single connected general pattern system. In its multifaceted scientific activity DIMendeleev also paid attention to pharmacy. Back in 1892, he wrote about the need to "set up factories and laboratories in Russia for the production of pharmaceutical and hygienic preparations" in order to free them from imports.

The works of A.M. Butlerov also contributed to the development of pharmaceutical chemistry. A.M. Butlerov (1828 - 1886) received urotropin in 1859; studying the structure of quinine, discovered quinoline. He synthesized sugary substances from formaldehyde. However, world fame brought him the creation (1861) of the theory of the structure of organic compounds.

The periodic system of elements by D.I. Mendeleev and the theory of the structure of organic compounds by A.M. Butlerov had a decisive influence on the development of chemical science and its connection with production.

Research in the field of chemotherapy and chemistry of natural substances. AT late XIX Bv in Russia, new studies of natural substances were carried out. As early as 1880, long before the works of the Polish scientist Funk, the Russian physician N.I. Lunin suggested that in addition to protein, fat, and sugar, food contained "substances indispensable for nutrition." He experimentally proved the existence of these substances, which were later called vitamins.

In 1890, the book by E. Shatsky "Teaching about plant alkaloids, glucosides and ptomains" was published in Kazan. It deals with the alkaloids known at that time in accordance with their classification according to the producing plants. Methods for the extraction of alkaloids from plant materials are described, including the apparatus proposed by E. Shatsky.

In 1897, K. Ryabinin's monograph "Alkaloids (Chemical and Physiological Essays)" was published in St. Petersburg. In the introduction, the author points out the urgent need "to have in Russian such an essay on alkaloids, which, with a small volume, would give an accurate, essential and comprehensive concept of their properties." The monograph has a short introduction describing general information about the chemical properties of alkaloids, as well as sections that give summary formulas, physical and chemical properties, reagents used for identification, and information on the use of 28 alkaloids.

Chemotherapy originated at the turn of the 20th century. due to the rapid development of medicine, biology and chemistry. Both domestic and foreign scientists have contributed to its development. One of the creators of chemotherapy is the Russian doctor D.JI. Romanovsky. In 1891, he formulated and experimentally confirmed the foundations of this science, pointing out that it is necessary to look for a "substance" that, when introduced into a diseased organism, will cause the least harm to the latter and cause the greatest destructive effect in the pathogenic agent. This definition has retained its meaning to this day.

Extensive research in the field of the use of dyes and organoelement compounds as medicinal substances was carried out by the German scientist P. Ehrlich (1854 - 1915) at the end of the 19th century. He was the first to propose the term "chemotherapy". On the basis of the theory developed by P. Ehrlich, called the principle of chemical variation, many scientists, including Russians (O.Yu. Magidson, M.Ya. Kraft, M.V. Rubtsov, A.M. Grigorovsky), created a large number of chemotherapeutic drugs with antimalarial activity.

The creation of sulfanilamide preparations, which marked the beginning of a new era in the development of chemotherapy, is associated with the study of the azo dye prontosil, discovered in search of drugs for the treatment of bacterial infections (G. Domagk). The discovery of prontosil was a confirmation of the continuity of scientific research - from dyes to sulfonamides.

Modern chemotherapy has a huge arsenal of drugs, among which the most important place is occupied by antibiotics. First discovered in 1928 by the Englishman A. Fleming, the antibiotic penicillin was the ancestor of new chemotherapeutic agents effective against pathogens of many diseases. The works of A. Fleming were preceded by research by Russian scientists. In 1872, V.A. Manassein established the absence of bacteria in the culture liquid when growing green mold (Pénicillium glaucum). A.G. Polotebnov experimentally proved that the cleansing of pus and wound healing occur faster if a mold is applied to it. The antibiotic effect of mold was confirmed in 1904 by veterinarian M.G. Tartakovsky in experiments with the causative agent of chicken plague.

The research and production of antibiotics has led to the creation of a whole branch of science and industry, revolutionized the field of drug therapy for many diseases.

Thus, conducted by Russian scientists at the end of the XIX century. research in the field of chemotherapy and chemistry of natural substances laid the foundation for obtaining new effective drugs in subsequent years.

2.3 Development of pharmaceutical chemistry in the USSR

The formation and development of pharmaceutical chemistry in the USSR took place in the early years of Soviet power in close connection with chemical science and production. The domestic schools of chemists created in Russia, which had a huge impact on the development of pharmaceutical chemistry, have been preserved. Suffice it to mention the major schools of organic chemists A.E. Favorsky and N.D. Zelinsky, the researcher of terpene chemistry S.S. geochemistry, N.S. Kurnakova - in the field of physical and chemical research methods. The center of science in the country is the Academy of Sciences of the USSR (now - NAS).

Like other applied sciences, pharmaceutical chemistry can develop only on the basis of fundamental theoretical research that was conducted at the research institutes of chemical and biomedical profile of the USSR Academy of Sciences (NAS) and the USSR Academy of Medical Sciences (now AMN). Scientists of academic institutions are directly involved in the creation of new drugs.

Back in the 30s, the first research in the field of chemistry of natural biologically active substances was carried out in the laboratories of A.E. Chichibabin. These studies were further developed in the works of I. L. Knunyants. Together with O.Yu.Magidson, he was the creator of the technology for the production of the domestic antimalarial drug akrikhin, which made it possible to free our country from importing antimalarial drugs.

An important contribution to the development of the chemistry of drugs with a heterocyclic structure was made by N.A. Preobrazhensky. Together with his colleagues, he developed and introduced into production new methods for obtaining vitamins A, E, PP, synthesized pilocarpine, studied coenzymes, lipids and other natural substances.

V.M. Rodionov had a great influence on the development of research in the field of chemistry of heterocyclic compounds and amino acids. He was one of the founders of the domestic industry of fine organic synthesis and chemical-pharmaceutical industry.

A very great influence on the development of pharmaceutical chemistry was exerted by the studies of the school of A.P. Orekhov in the field of alkaloid chemistry. Under his leadership, methods were developed for the isolation, purification and determination of the chemical structure of many alkaloids, which then found application as medicines.

On the initiative of M.M. Shemyakin, the Institute of Chemistry of Natural Compounds was established. Here fundamental research is being carried out in the field of chemistry of antibiotics, peptides, proteins, nucleotides, lipids, enzymes, carbohydrates, steroid hormones. On this basis, new drugs have been created. The Institute laid the theoretical foundations of a new science - bioorganic chemistry.

The studies carried out by GV Samsonov at the Institute of Macromolecular Compounds made a great contribution to solving the problems of purification of biologically active compounds from accompanying substances.

Close ties connect the Institute of Organic Chemistry with research in the field of pharmaceutical chemistry. During the years of the Great Patriotic War here such preparations as Shostakovsky's balm, phenamine, and later promedol, polyvinylpyrrolidone, etc. were created. obtaining vitamin B and its analogues. Work has been carried out in the field of the synthesis of anti-tuberculosis antibiotics and the study of the mechanism of their action.

Research in the field of organoelement compounds carried out in the laboratories of A.N. Nesmeyanov, A.E. Arbuzov and B.A. Arbuzov, M.I. Kabachnik, I.L. These studies were the theoretical basis for the creation of new drugs, which are organoelement compounds of fluorine, phosphorus, iron and other elements.

At the Institute of Chemical Physics, N.M. Emanuel was the first to express the idea of ​​the role of free radicals in suppressing the function of a tumor cell. This allowed the creation of new anticancer drugs.

The development of pharmaceutical chemistry was also greatly facilitated by the achievements of the domestic medical and biological sciences. The work of the school of the great Russian physiologist I.P. Pavlov, the work of A.N. Bach and A.V. Palladin in the field of biological chemistry, etc., had a huge impact.

at the Institute of Biochemistry. A.N.Bakh, under the leadership of V.N.Bukin, developed methods for the industrial microbiological synthesis of vitamins B12, B15, etc.

Fundamental research in the field of chemistry and biology carried out at the institutes of the National Academy of Sciences creates a theoretical basis for the development of targeted synthesis of medicinal substances. Of particular importance are studies in the field of molecular biology, which provides a chemical interpretation of the mechanism biological processes occurring in the body, including under the influence of drugs.

A great contribution to the creation of new drugs is made by research institutes of the Academy of Medical Sciences. Extensive synthetic and pharmacological research is carried out by the institutes of the National Academy of Sciences together with the Institute of Pharmacology of the Academy of Medical Sciences. This partnership has made it possible to develop theoretical foundations directed synthesis of a number of drugs. Synthetic chemists (N.V. Khromov-Borisov, N.K. Kochetkov), microbiologists (Z.V. Ermolyeva, G.F. Gause and others), pharmacologists (S.V. Anichkov, V.V. Zakusov, M.D. Mashkovsky, G.N. Pershin and others) created original medicinal substances.

On the basis of fundamental research in the field of chemical and biomedical sciences, pharmaceutical chemistry developed in our country and became an independent branch. Already in the first years of Soviet power, pharmaceutical research institutes were created.

In 1920, the Scientific Research Chemical and Pharmaceutical Institute was opened in Moscow, which in 1937 was renamed VNIHFI named after V.I. S. Ordzhonikidze. Somewhat later, such institutes (NIHFI) were created in Kharkov (1920), Tbilisi (1932), Leningrad (1930) (in 1951 LenNIKhFI was merged with the chemical-pharmaceutical educational institute). AT post-war years NIHFI was formed in Novokuznetsk.

VNIHFI is one of the largest research centers in the field of new drugs. The scientists of this institute solved the iodine problem in our country (O.Yu. Magidson, A.G. Baichikov and others), developed methods for obtaining antimalarial drugs, sulfonamides (O.Yu. Magidson, M.V. Rubtsov and others. ), anti-tuberculosis drugs (S.I. Sergievskaya), arsenic-organic drugs (G.A. Kirchhoff, M.Ya. Kraft, etc.), steroid hormonal drugs (V.I. Maksimov, N.N. Suvorov, etc.) , carried out major studies in the field of chemistry of alkaloids (A.P. Orekhov). Now this institute is called the "Center for the Chemistry of Medicinal Products" - VNIKhFI im. S. Ordzhonikidze. Scientific personnel are concentrated here, coordinating activities for the creation and implementation of new medicinal substances into the practice of chemical and pharmaceutical enterprises.

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PHARMACY (Greek φαρμακεία the use of medicines) is a complex of sciences and practical knowledge, including issues of research, procurement, research, storage, manufacture and distribution of medicinal and therapeutic and prophylactic agents. PHARMACY "Pharmaceutical Chemistry" VV Chupak-Belousov is a complex of scientific and practical disciplines studying the problems of creation, safety, research, storage, PHARMACEUTICAL CHEMISTRY TOXICOLOGICAL CHEMISTRY of manufacturing, dispensing and marketing of medicines, as well as the search for natural sources of medicinal substances. TECHNOLOGY OF DOSAGE FORMS PHARMACOGNOSIS Wikipedia ECONOMY AND ORGANIZATION OF PHARMACEUTICAL BUSINESS 3

Toxicological chemistry is a science that studies methods for isolating toxic substances from various objects, as well as methods for detecting and quantifying these substances. Pharmacognosy is a science that studies medicinal plant materials and the possibilities of creating new medicinal substances from it. The technology of dosage forms (pharmaceutical technology) is a field of knowledge that studies the methods of preparing medicines. The economics and organization of the pharmaceutical business is a field of knowledge that deals with solving the problems of storing medicines, as well as organizing a control and analytical service. 4

Pharmaceutical chemistry is a science that, based on the general laws of chemical sciences, explores the methods of obtaining, structure, physical and chemical properties of medicinal substances, the relationship between their chemical structure and effects on the body, quality control methods and changes that occur during storage. "Pharmaceutical chemistry" V. G. Belikov is the science of the chemical properties and transformations of medicinal substances, methods for their development and production, quality and quantitative analysis. Wikipedia 5

Objects of pharmaceutical chemistry Medicinal substances (MS) - (substances) individual substances of plant, animal, microbial or synthetic origin with pharmacological activity. Substances are intended for obtaining medicines. Medicines (PM) are inorganic or organic compounds with pharmacological activity, obtained by synthesis, from plant materials, minerals, blood, blood plasma, organs, tissues of a human or animal, as well as using biological technologies. Dosage form (DF) is a state that is convenient for use, in which the desired therapeutic effect is achieved. Medicinal preparations (MP) are dosed drugs in a specific LF, ready for use. "Pharmaceutical chemistry" V. G. Belikov 6

The relationship of pharmaceutical chemistry with other chemical disciplines PHARMACEUTICAL CHEMISTRY Methods of development and methods for obtaining drugs Inorganic chemistry Quality assurance of drugs Properties of drugs Organic chemistry Physical chemistry Analytical chemistry Biochemistry 7

Name of drugs The Commission on International Names of WHO, in order to streamline and (2 RS, 3 S, 4 S, 5 R) -5 -amino-2 - (aminomethyl) -6 unify drug names in all countries of the world, has developed - ((2 R, 3S, 4R, 5S)-5 -((1R, 2R, 5R, 6R)-3, 5 international classification, based on diamino-2 - ((2 R, 3 S, 4 R, 5 S) -3 -amino-6 which is based on (aminomethyl) -4, 5 -dihydroxytetrahydro-2 H a certain system for the formation of drug terminology. The principle of this is pyran-2 -yloxy)-6 -hydroxycyclohexyloxy)-4 system INN - INN (International Nonproprietary Names - International hydroxy-2 -(hydroxymethyl)tetrahydrofuran Nonproprietary Names) is -3 -yloxy)tetrahydro-2 H-pyran-3, 4 -diol that in the name of the drug its group affiliation is tentatively given. This is achieved for IUPAC name by including in the name parts of words corresponding to the pharmacotherapeutic group to which this drug belongs. Members of WHO are required to recognize the names of substances recommended by WHO as INNs and prohibit their registration as trademarks or trade names of Neomycin. INN name 8

Classification of drugs Pharmacological classification - all drugs are divided into groups depending on their effect on systems, processes and executive organs (for example, heart, brain, intestines, etc.). In accordance with this, drugs are combined into groups of narcotic drugs, hypnotics and sedatives, local anesthetics, analgesics, diuretics, etc. Chemical classification- Drugs are grouped according to the commonality of the chemical structure and chemical properties. At the same time, in each chemical group of drugs there may be substances with different physiological activity. nine

Modern Problems of Pharmaceutical Chemistry Creation and Research of New Drugs Despite the huge arsenal of drugs, the problem of finding new highly effective drugs The main directions of the search for new and modernization of existing drugs remains relevant. The role of drugs is constantly growing in modern medicine, which is due to a number of reasons: Synthesis of bioregulators and metabolites of energy and plastic metabolism A number of serious diseases are not yet cured by drugs Identification of potential drugs during the screening of new chemical products Long-term use of a number of drugs forms tolerant pathologies to combat synthesis who need new drugs with a different mechanism of action Synthesis of compounds with programmable properties (modified processes in the known series of drugs, lead to the emergence of new structures of the evolution of microorganisms resynthesis of natural phytosubstances, diseases, for the treatment of computer search for biologically active substances) which need effective drugs Some of the drugs used cause side effects effects in having a stereoselective synthesis of eutomers (an enantiomer of a chiral drug, due to which pharmacological activity is necessary) and the most active conformations to create safer drugs of socially significant drugs 10

Modern problems of pharmaceutical chemistry Development of methods for pharmaceutical and biopharmaceutical analysis Promising areas of search in this area Only The solution of this important problem is possible on the basis of fundamental theoretical studies of the physical and chemical properties of drugs Work to improve the accuracy of analysis, its specificity, sensitivity and with the widespread use of modern chemical and physical and chemical methods. rapidity, as well as automation of individual stages or the entire analysis. The use of these methods should cover the entire process from the creation of new drugs to quality control and increase the cost-effectiveness of analysis methods. Reducing the labor intensity of the final production product. It is also necessary to develop new and improved regulatory documentation for drugs and drug products. It is promising to develop quality and provide for the analysis of drug groups, reflecting the requirements for their unified standardization methods. united by kinship of chemical structure based on the use of physicochemical methods 11

Raw material base of pharmaceutical chemistry Vegetable raw materials (leaves, flowers, seeds, fruits, bark, plant roots) and products of their processing (fatty and essential oils, juices, gums, resins); Animal raw materials (organs, tissues, glands of slaughtered cattle); Fossil organic raw materials (oil and products of its distillation, products of coal distillation; products of basic and fine organic synthesis); Inorganic minerals (mineral rocks and products of their processing by the chemical industry and metallurgy); 12

History of Pharmaceutical Chemistry The emergence of pharmacy is lost in the depths of the primitive era. Primitive was completely dependent on the outside world. In search of relief from illness and suffering, he used various remedies from his environment, the first of which appeared during the period of gathering and had vegetable origin: belladonna, poppy, tobacco, wormwood, henbane. With the development of agriculture, the domestication of animals and the transition to cattle breeding, new plants with healing properties were discovered: hellebore, centaury and many others. The manufacture of tools and household items from native metals, the development of pottery led to the manufacture of dishes that made it possible to prepare medicinal potions. During this period, medicines of mineral origin were introduced into the practice of healing, which they learned to extract from rocks, oil, and coal. thirteen

History of Pharmaceutical Chemistry With the advent of writing, the first medical texts appear containing descriptions of medicines, methods of their preparation and use. Currently, more than 10 ancient Egyptian papyri are known, in one way or another devoted to medicine. The most famous of these is the Ebers Papyrus ("The Book of the Preparation of Medicines for All Parts of the Body"). This is the largest of the papyri and dates back to 1550 BC. e. and contains about 900 recipes for the treatment of diseases of the gastrointestinal tract, lungs, eyes, ears, teeth, joints. fourteen

History of Pharmaceutical Chemistry Theophrastus - The Father of Botany Theophrastus (circa 300 BC), one of the greatest early Greek philosophers and naturalists, is often referred to as the "father of botany". His observations and writings regarding the medicinal qualities and characteristics of herbs are extremely accurate, even in the light of modern knowledge. In his hands he holds a branch of belladonna. fifteen

The History of Pharmaceutical Chemistry Dioscorides In the evolution of all successful and enduring systems of knowledge, there comes a point when a great deal of observation and intense research transcends the level of trade or profession and acquires the status of science. Dioscorides (1st century AD) strongly influenced this transition in pharmacy. He carefully described the rules for the collection of medicines, their storage and use. In the Renaissance, scholars again turn to his texts. sixteen

History of Pharmaceutical Chemistry During the Middle Ages in Western civilization, the remnants of knowledge about pharmacy and medicine were preserved in monasteries. The monks collected herbs in the vicinity of the monasteries and transferred them to their own herbal gardens. They were engaged in the preparation of medicines for the sick and wounded. Many manuscripts have been preserved in reprinting or translation in monastic libraries. Such gardens can still be found in monasteries in many countries. 17

History of pharmaceutical chemistry Avicenna (Ibn Sina) 980 - 1037 The most prominent representative of the philosophers of the Arabian period. He made a significant contribution to pharmacy and medicine. The pharmaceutical teachings of Avicenna were accepted as an authority in the West until the 17th century. The treatise "Canon of Medicine" is an encyclopedic work in which the prescriptions of ancient physicians are comprehended and revised in accordance with the achievements of Arabic medicine. In the "Canon" Ibn Sina suggested that diseases can be caused by some tiny creatures. He was the first to draw attention to the contagious nature of smallpox, to distinguish between cholera and plague, to describe leprosy, separating it from other diseases, and to study a number of other diseases. Ibn Sina also removes attention from the description of medicinal raw materials, medicines, methods of their manufacture and use. eighteen

History of pharmaceutical chemistry The period of iatrochemistry (XVI-XVII centuries) The founder of iatrochemistry is the German physician and alchemist Philip Aureol Theophrastus Bombast von Hohenheim (1493-1541), who went down in history under the pseudonym Paracelsus, shared the ancient Greek doctrine of the four elements. Paracelsus' medicine was based on the mercury-sulphur theory. He taught that living organisms consist of the same mercury, sulfur, salts and a number of other substances that form all other bodies of nature; when a person is healthy, these substances are in balance with each other; disease means the predominance or, conversely, the lack of one of them. To restore balance, Paracelsus used in medical practice many medicinal preparations of mineral origin - compounds of arsenic, antimony, lead, mercury, etc. - in addition to traditional herbal preparations. Paracelsus argued that the task of alchemy is the manufacture of medicines: “Chemistry is one of the pillars on which medical science must rely. The task of chemistry is not at all to make gold and silver, but to prepare medicines. nineteen

History of pharmaceutical chemistry The period of the birth of the first chemical theories (XVII-XIX centuries) c. n. 17th century – phlogiston theory (I. Becher, G. Stahl) c. n. 18th century - refutation of the theory of phlogiston. Oxygen theory (M. V. Lomonosov, A. Lavoisier) 1804 - German pharmacologist Friedrich Serturner isolated the first alkaloid (Morphine) from opium in 1818-1820. – Pelletier and Caventon isolate strychnine, brucine, develop methods for separating quinine and cinchonine isolated from cinchona bark XIX – American and European Pharmaceutical Associations are formed 20

History of pharmaceutical chemistry One of the successful researchers in the development of new chemical compounds, specially created to combat pathogens was a French pharmacist, Ernest Forunio (1872 -1949 In his early work, he proposes the use of bismuth and arsenic compounds for the treatment of syphilis. His research "paved the way" for sulfonylamide compounds and chemicals with antihistamine properties. In 1894 Behring and Roux announced the effectiveness of antibodies against diphtheria.Pharmaceutical scientists in Europe and the United States immediately began to put the new discovery into production.The serum became available in 1895 (!), and the lives of thousands of children were saved.Vaccination of horses with diphtheria was the first one of many steps in the development of antidotes, a field that culminated with the development of a polio vaccine in 1955. 21

History of pharmaceutical chemistry Modern period The second quarter of the 20th century marked the heyday of the era of antibiotics. Penicillin is the first antibiotic that was isolated in 1928 by Alexander Fleming from a strain of the fungus Penicillium notatum. In 1940-1941, H. W. Flory (bacteriologist), E. Cheyne (biochemist) and N. W. Heatley (biochemist) worked on the isolation and industrial production of penicillin, and also used it for the first time to treat bacterial infections. In 1945, Fleming, Florey and Cheyne were awarded Nobel Prize in Physiology or Medicine "for the discovery of penicillin and its curative effects in various infectious diseases» . Using the latest technical achievements each of the branches of science, pharmaceutical chemistry develops and manufactures the newest and best medicines. Today, pharmaceutical production uses methods and highly qualified personnel from every branch of science to do this. 22

Literature "Pharmaceutical Chemistry", ed. V. G. Belikova “Pharmaceutical chemistry. Course of lectures, ed. V. V. Chupak-Belousova “Fundamentals of Medicinal Chemistry” V. G. Granik “Synthesis of Basic Medicines” R. S. Vartanyan “ Medical chemistry» V. D. Orlov, V. V. Lipson, V. V. Ivanov “Medications” M. D. Mashkovsky https: //vk. com/nspu_pc 23