Course of lectures on pharmaceutical chemistry. Pharmaceutical chemistry - Glushchenko N.N.

. 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 analysis methods 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. Wed-in the required level of quality is established using standard methods of 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. Wed-in (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

Subject and tasks of pharmaceutical chemistry.

pharmaceutical chemistry(FH) - a science that studies ways to get,

structures, physical and chemical properties medicinal substances; the relationship between their chemical structure and action on the body; methods of quality control of medicines and changes occurring during their storage. The problems facing it are solved with the help of physical, chemical and physico-chemical research methods used both for the synthesis and for the analysis of medicinal substances. PC is based on the theory and laws of related chemical sciences: inorganic, organic, analytical, physical and biological chemistry. It is closely related to pharmacology, biomedical and clinical disciplines.

Terminology in FH

The object of study of PC are pharmacological and medicinal products. The first of these is a substance or mixture of substances with established pharmacological activity, which is the object of clinical trials. After clinical trials and positive results means is approved by the Pharmacological and Pharmacopeial Committees for use and receives the name of the medicinal product. A medicinal substance is a substance that is an individual chemical compound or biological substance. A dosage form is a convenient state for use, given to a drug, in which the desired therapeutic effect is achieved. It includes powders, tablets, solutions, ointments, suppositories. A dosage form manufactured by a particular company and given a brand name is called a drug.

Sources of medicines

Medicinal substances by their nature are divided into inorganic and organic. They can be obtained from natural sources and synthetically. Rocks, gases, sea water, production wastes, etc. can be raw materials for obtaining inorganic substances. Organic medicinal substances are obtained from oil, coal, oil shale, gases, tissues of plants, animals, microorganisms, and other sources. In recent decades, the number of drugs obtained synthetically has increased dramatically.

Often, the complete chemical synthesis of many compounds (alkaloids, antibiotics, glycosides, etc.) is technically complex and new methods for obtaining drugs are used: semi-synthesis, biosynthesis, genetic engineering, tissue culture, etc. With the help of semi-synthesis, drugs are obtained from intermediates of natural origin, for example semi-synthetic penicillins, cephalosporins, etc. Biosynthesis is a natural synthesis final product living organisms based on natural intermediates.

The essence of genetic engineering is to change the genetic programs of microorganisms by introducing into their DNA genes encoding the biosynthesis of certain drugs, such as insulin. Tissue culture is the reproduction in artificial conditions of animal or plant cells, which become raw materials for the production of drugs. For the development of the latter, hydrobionts, plant and animal organisms of the seas and oceans are also used.

Classification of medicinal substances.

There are two types of classification a large number used medicinal substances: pharmacological and chemical. The first of them divides medicinal substances into groups depending on the mechanism of action on individual organs and systems of the body (central nervous, cardiovascular, digestive, etc.). This classification is convenient for use in medical practice. Its disadvantage is that in one group there may be substances with different chemical structures, which makes it difficult to unify the methods of their analysis.

According to the chemical classification, medicinal substances are divided into groups based on the commonality of their chemical structure and chemical properties regardless of pharmacological action. For example, pyridine derivatives have miscellaneous action on the body: nicotinamide is a vitamin PP, nicotinic acid diethylamide (cordiamin) stimulates the central nervous system, etc. Chemical classification is convenient because it allows you to identify the relationship between the structure and mechanism of action of medicinal substances, and also allows you to unify the methods of their analysis. In some cases, a mixed classification is used to take advantage of the pharmacological and chemical classification of drugs.

requirements for medicines.

The quality of the medicinal product is determined by its appearance, solubility, identification of its identity, degree of purity and quantitative determination of the content of the pure substance in the preparation. The complex of these indicators is the essence of pharmaceutical analysis, the results of which must comply with the requirements of the State Pharmacopoeia (SP).

The authenticity of the medicinal substance (confirmation of its identity) is established using chemical, physical and physico-chemical research methods. Chemical methods include reactions to the functional groups included in the structure of the drug, which are characteristic of a given substance: According to the Global Fund, they are reactions to aromatic primary amines, ammonium, acetates, benzoates, bromide, bismuth, ferrous and oxide iron, iodides, potassium, calcium, carbonates (bicarbonates), magnesium, arsenic, sodium, nitrates, nitrites, oxide mercury, salicylates, sulfates, sulfites, tartrates, phosphates, chlorides, zinc and citrates.

Physical methods for establishing the authenticity of a medicinal product include determining its: 1) physical properties: state of aggregation, color, smell, taste, crystal form or type of amorphous substance, hygroscopicity or degree of weathering in air, volatility, mobility and flammability, and 2) physical constants: melting (decomposition) and solidification temperatures, density, viscosity, solubility in water and other solvents , transparency and degree of turbidity, color, ash, insoluble in hydrochloric acid and sulfate and volatile substances and water.

Physical and chemical methods for studying authenticity consist in the use of instruments for chemical analysis: spectrophotometers, fluorometers, flame photometers, chromatography equipment, etc.

Impurities in medicines and their sources.

Many drugs contain certain impurities of foreign substances. Exceeding their level may cause unwanted action. The reasons for the ingress of impurities into medicinal substances may be insufficient purification of the feedstock, by-products of synthesis, mechanical contamination, impurities of the materials from which the equipment is made, and violation of storage conditions.

The GF requires either the complete absence of impurities, or allows the maximum permissible limit of them defined for a given drug, which does not affect the quality and therapeutic effect of the drug. Reference solutions are provided to determine the acceptable limit of HF impurities. The result of a reaction to a particular impurity is compared with the result of a reaction carried out with the same reagents and in the same volume with a reference, standard solution containing an acceptable amount of an impurity. Determining the degree of purity of a medicinal product includes testing for: chlorides, sulfates, ammonium salts, calcium, iron, zinc, heavy metals and arsenic.

region. State Pharmacopoeia of the USSR (SF USSR)

The GF of the USSR is a collection of obligatory national standards and regulations that regulate the quality of medicinal substances. It is based on the principles of Soviet health care and reflects modern achievements in the field of pharmacy, medicine, chemistry and other related sciences. The Soviet Pharmacopoeia is a national document, it reflects social entity Soviet health care, the level of science and culture of the population of our country. The State Pharmacopoeia of the USSR has a legislative character. Its requirements for medicines are mandatory for all enterprises and institutions. Soviet Union who manufacture, store, control the quality and use medicines.

The first edition of the Soviet Pharmacopoeia, called the VII edition of the State Pharmacopoeia of the USSR (SP VII), was put into effect in July 1926. To create it in 1923 in People's Commissariat health of the RSFSR, a special pharmacopoeial commission was formed under the chairmanship of prof. A. E. Chichibabina. The First Soviet Pharmacopoeia differed from previous editions in its increased scientific level, the desire for a possible replacement of medicines made from imported raw materials with domestically produced medicines. Higher requirements were imposed in GF VII not only for drugs, but also for products used for their manufacture.

Based on these principles, 116 articles for new drugs were included in GF VII and 112 articles were excluded. Significant changes have been made to the requirements for drug quality control. A number of new methods of chemical and biological standardization of drugs were provided, 30 general articles were included in the form of appendices, descriptions of some general reactions used to determine the quality of drugs, etc. The organoleptic control of many drugs was for the first time replaced by more objective physical and chemical methods, biological control methods were introduced.

Thus, in GF VII, priority was given to improving the quality control of medicines. This principle has found its further development in subsequent editions of the pharmacopoeias.

In 1949, the VIII edition was published, and in October 1961, the IX edition of the State Pharmacopoeia of the USSR. By this time, new groups of highly effective drugs (sulfonamides, antibiotics, psychotropic, hormonal and other drugs) had been created, which required the development of new methods of pharmaceutical analysis.

The X edition of the State Pharmacopoeia (SP X) was put into effect on July 1, 1969. It reflected the new achievements of the domestic pharmaceutical and medical science and industry.

The fundamental difference between GF IX and GF X is the transition to a new international terminology of drugs, as well as a significant update of both the nomenclature and methods of drug quality control.

In SP X, the requirements for the quality of medicines have been significantly increased, the methods of pharmacopoeial analysis have been improved, and the scope of physical and chemical methods has been expanded. Numerous general articles, reference tables and other materials included in SP X reflected the requirements necessary for assessing the qualitative and quantitative characteristics of medicines.

The State Pharmacopoeia of the USSR X edition includes 4 parts: "Introductory part"; "Preparations" (private and group articles); "General methods of physico-chemical, chemical and biological research"; "Applications".

The "Introductory part" sets out the general principles of construction and the procedure for using SP X, the compilers, changes that distinguish SP X from SP IX, list A and list B of medicinal substances are indicated.

GF X contains 707 articles for medicinal substances (in GF IX there were 754) and 31 group articles (in GF IX there were 27). The nomenclature was updated by 30% due to the exclusion of drugs that were discontinued from production, as well as having limited use. The quality of the latter is established in accordance with the requirements of GF IX.

Compared to SP IX, the number of individual (synthetic and natural) drugs increased from 273 to 303, from 10 to 22 antibiotics, for the first time radioactive drugs were included in SP X. Among the drugs included in the GF X are new cardiovascular, psychotropic, ganglioblocking, antimalarial, anti-tuberculosis drugs, drugs for the treatment of malignant neoplasms, fungal diseases, new drugs for anesthesia, hormonal drugs, vitamins. Most of them were obtained for the first time in our country.

"Preparations" - the main part of SP X (pp. 39-740). 707 articles set out the requirements for the quality of medicines (quality standards). Each medicinal product, in accordance with the requirements of the pharmacopoeia, is subjected to physical properties testing, identity testing, purity testing and determination of the quantitative content of the drug. In GF X, the structure of articles reflecting the sequence of control is detailed. The "Properties" section has been replaced by two sections: "Description" and "Solubility". The description of authenticity reactions for 25 ions and functional groups is summarized in one general article, and references are given to it in private articles.

Changed the order of articles. For the first time in SP X, articles on finished dosage forms are located after articles on the corresponding medicinal product. In most articles of GF X there is a heading indicating the pharmacological action of the drug. Detailed information about the highest doses of drugs for various methods of administration.

In the third part of SP X "General methods of physico-chemical, chemical and biological research" is given short description methods used for pharmacopoeial analysis, provides information on reagents, titrated solutions and indicators.

"Appendices" to GF X contain reference tables atomic masses, densities, constants (solvents, acids, bases) and other quality indicators of drugs. This also includes tables of higher single and daily doses of poisonous and potent drugs for adults, children, and also for animals.

After the release of the 10th edition of the State Pharmacopoeia, the Ministry of Health of the USSR approved a number of new highly effective drugs for use in medical practice. Many of them were first developed by scientists of our country. At the same time, ineffective drugs were excluded, which were replaced by more modern drugs. Therefore, there is a need to create a new XI edition of the State Pharmacopoeia of the USSR, which is being prepared at the present time. Scientific institutions and enterprises of the USSR Ministry of Public Health, the Ministry of Medical Industry and other departments are involved in this work. The new State Pharmacopoeia will reflect modern achievements in the field of pharmaceutical analysis and improvement of the quality of medicines.

National and regional pharmacopoeias

Such large capitalist states as the USA, Great Britain, France, Germany, Japan, Italy, Switzerland and some others systematically produce national pharmacopoeias every 5-8 years. Published in 1924-1946. the pharmacopoeias of Greece, Chile, Paraguay, Portugal, Venezuela have already lost their significance.

Along with pharmacopoeias, in some countries, collections of official requirements for medicines such as the US National Formulary, the British Pharmaceutical Code are periodically published. They standardize the quality of new drugs that are not included in the pharmacopoeias or included in earlier editions of the pharmacopoeias.

The first experience of creating a regional pharmacopeia was carried out by the Scandinavian countries (Norway, Finland, Denmark and Sweden). The published Scandinavian pharmacopoeia since 1965 has acquired a legislative character for these countries.

Eight Western European states (Great Britain, Germany, France, Italy, Belgium, Luxembourg, the Netherlands and Switzerland), members of the EEC (European Economic Community), created in 1964 a pharmacopoeial commission. She prepared and in 1969 published the first, and in 1971 the second volume of the EEC Pharmacopoeia (in 1973, an addition to these editions was issued). In 1976, the EEC Pharmacopoeia was recognized by the Scandinavian countries, Iceland and Ireland. The EEC Pharmacopoeia is of a legislative nature, but does not replace the national pharmacopoeias of these countries.

Regional pharmacopoeias contribute to the unification of the nomenclature and quality requirements for medicines obtained in different countries

Quality control of medicines in pharmacies

Intra-pharmacy drug quality control includes not only analytical control, but also a system of measures that ensure the correct storage, preparation and dispensing of drugs. It is based on strict adherence to the pharmaceutical and sanitary regime in the pharmacy. It is especially necessary to carefully follow the rules for storing medicines, the technology for preparing injection solutions, concentrates and eye drops.

For intra-pharmacy quality control of medicines, pharmacies should have analytical rooms or analytical tables equipped with the necessary instruments, reagents, reference and special literature. Intra-pharmacy control is carried out by pharmacists-analysts who are part of the staff of large pharmacies, as well as pharmacists-technologists, whose duties include checking the quality of medicines. They have an equipped workplace on the assistant's table or next to it. The head of the pharmacy and his deputies manage the quality control of medicines. They must own all types of intra-pharmacy control, and in small pharmacies themselves perform the functions of a pharmacist-analyst or pharmacist-technologist.

Direct analytical control in a pharmacy includes three main areas: quality control of medicinal substances coming from industry, quality control of distilled water and different kinds quality control of dosage forms manufactured in a pharmacy.

Medicinal substances entering the pharmacy from the industry, regardless of the presence of the OTC stamp, are controlled for identity. Preparations that rapidly change during storage are sent at least once a quarter for testing to control and analytical laboratories.

Systematic monitoring of the good quality of distilled water in a pharmacy ensures the quality of preparation of all liquid dosage forms. Therefore, distilled water is controlled in each cylinder for the absence of chlorides, sulfates and calcium salts. Even higher requirements are imposed on the water used for the preparation of injection solutions. Its absence of reducing agents, ammonia, carbon dioxide. At least once a quarter, the pharmacy sends distilled water for a complete analysis to the control and analytical laboratory, and twice a year to the sanitary and bacteriological laboratory to check the absence of microflora contamination.

All dosage forms manufactured in pharmacies are subject to intra-pharmacy control. There are several types of control: written, organoleptic, questionnaire, physical and chemical. Written, organoleptic, questioning and physical control is carried out, as a rule, by a pharmacist-technologist after the pharmacist has manufactured at least 5 medicines, and chemical control is carried out by a pharmacist-analyst.

All drugs manufactured in any pharmacy are subject to written control. The essence of written control is that the pharmacist, after preparing the medicine, writes down from memory on a special form the name and total weight of each ingredient or indicates the content of each concentrate taken. Then the form, together with the prescription, is submitted for verification to the pharmacist-technologist. The completed forms are stored in the pharmacy for 12 days.

Organoleptic control includes checking appearance(color, homogeneity of mixing), smell and taste of medicines, absence of mechanical impurities. All medicines prepared for internal use by children and selectively prepared for adults are checked for taste (excluding medicines containing ingredients related to list A).

Questioning control is carried out by a pharmacist-technologist. He names the ingredient, and in compound medicines the content of the first ingredient. After that, the pharmacist calls all the other ingredients and their amounts. If concentrates were used to make the medicine, the pharmacist lists them with an indication of the percentage. Questionnaire control is carried out immediately after the manufacture of medicines, if they are intended for injection or they contain list A drugs. If there is doubt about the quality of the manufactured medicine, questioning control is an additional type of control.

Physical control consists in checking the total volume (mass) of the prepared drug or the mass of its individual doses. Controlled 5-10% of the number of doses prescribed in the prescription, but not less than three doses. Physical control is carried out selectively, periodically throughout the working day. Together with physical control, the correctness check is carried out, the correctness of the design of drugs and the compliance of the packaging with the physical and chemical properties of the ingredients that make up the dosage form are carried out.

Chemical control includes qualitative and quantitative chemical analysis of medicines prepared in a pharmacy. quality chemical analysis subject all injection solutions (before they are sterilized); eye drops; each series of concentrates, semi-finished products and in-pharmaceutical preparations; medicines coming from the stock department to the assistant department; children's dosage forms; drugs containing list A drugs. Selectively control drugs made from individual impurities.

To perform a qualitative analysis, the drop method is mainly used, using tables of the most characteristic reactions.

Oh practical work it is necessary to study the basics of general pharmaceutical chemistry and methods for studying the qualitative and quantitative studies of substances most commonly found in veterinary practice.

The list of medicines subject to quantitative analysis depends on the availability of a pharmacist-analyst in the pharmacy. If it is in the state of the pharmacy, then all drugs for injection are subjected to quantitative analysis (before sterilization); eye drops (containing silver nitrate, atropine sulfate, dicaine, ethylmorphine pilocarpine hydrochloride); solutions of atropine sulfate for internal use; all concentrates, semi-finished products and in-pharmaceutical preparations. The remaining drugs are analyzed selectively, but daily by each pharmacist. First of all, they control medicines used in pediatric and ophthalmic practice, as well as those containing preparations of list A. Perishable medicines (solutions of hydrogen peroxide, ammonia and formaldehyde, lime water, ammonia-anise drops) are analyzed at least once a quarter.

If there is no pharmacist-analyst, but there are two or more pharmacists in the pharmacy staff, then injection solutions (before sterilization) containing novocaine, atropine sulfate, calcium chloride, sodium chloride, glucose are subjected to quantitative analysis; eye drops containing silver nitrate, atropine sulfate, pilocarpine hydrochloride; all concentrates; solutions of hydrochloric acid. Perishable medicines from these pharmacies are sent for testing to control and analytical laboratories.

Qualitative and quantitative analysis in category VI pharmacies with one pharmacist in the state and in pharmacy points of the first group are subject to injection solutions containing novocaine and sodium chloride; eye drops containing atropine sulfate and silver nitrate.

The procedure for assessing the quality of drugs manufactured in pharmacies and the norms of permissible deviations in the manufacture of drugs are established by order of the Ministry of Health of the USSR No. 382 dated September 2, 1961. To assess the quality of manufactured drugs, the terms are used: “satisfies” or “does not satisfy” the requirements of the USSR GF, FS , VFS or instructions of the Ministry of Health of the USSR.

Features of pharmaceutical analysis.

Pharmaceutical analysis is one of the main branches of pharmaceutical chemistry. It has its own specific features that distinguish it from other types of analysis. They consist in the fact that substances of various chemical nature are subjected to research: inorganic, organoelement, radioactive, organic compounds from simple aliphatic to complex natural biologically active substances. The range of concentrations of analytes is extremely wide. The objects of pharmaceutical research are not only individual medicinal substances, but also mixtures containing a different number of components. The number of medicines used is increasing every year. This leads to the need for both the development of new methods of analysis and the unification of already known ones.

The continuous increase in the requirements for the quality of medicines dictates the need for continuous improvement of pharmaceutical analysis. Moreover, the requirements are growing both for the good quality of medicinal substances and for the quantitative content. This necessitates the widespread use of not only chemical, but also more sensitive physical and chemical methods for assessing the quality of drugs.

The requirements for pharmaceutical analysis are high. It must be sufficiently specific and sensitive, accurate in relation to the standards stipulated by the USSR GF, VFS, FS and other scientific and technical documentation, carried out in short periods of time using minimum quantities tested drugs and reagents.

Pharmaceutical analysis, depending on the tasks, includes various forms of drug quality control: pharmacopoeial analysis, step-by-step control of the production of medicines, analysis of individual dosage forms, express analysis in a pharmacy, and biopharmaceutical analysis.

Integral part pharmaceutical analysis is pharmacopoeial analysis. It is a set of methods for the study of drugs and dosage forms set forth in the State Pharmacopoeia or other regulatory and technical documentation (VFS, FS). Based on the results obtained during the pharmacopoeial analysis, a conclusion is made on the compliance of the medicinal product with the requirements of the USSR GF or other regulatory and technical documentation. In case of deviation from these requirements, the drug is not allowed to be used.

Performing a pharmacopoeial analysis allows you to establish the authenticity of the drug, its good quality, to determine the quantitative content of the pharmacologically active substance or ingredients that make up the dosage form. While each of these steps has a specific purpose, they cannot be considered in isolation. They are interrelated and complement each other. For example, melting point, solubility, pH of an aqueous solution, etc. are criteria for both the authenticity and the good quality of the medicinal substance.

SP X describes the methods of appropriate tests in relation to one or another pharmacopoeial preparation. Many of these methods are identical. To summarize a large amount of private information on pharmacopoeial analysis, the main criteria for pharmaceutical analysis and the general principles of testing for authenticity, good quality and quantitative determination of medicinal substances will be considered. In separate sections, the state of and prospects for the use of physicochemical and biological methods in the analysis of drugs are considered.

PHARMACY (Greek φαρμακεία use of drugs) is a complex of sciences and practical knowledge, including the 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 possibility 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, qualitative 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, 3 S, 4 R, 5 S)-5 -((1 R, 2 R, 5 R, 6 R)-3, 5 international classification, based on diamino-2 -((2 R, 3 S, 4 R, 5 S)-3 -amino-6 of which (aminomethyl)-4, 5 -dihydroxytetrahydro-2 H is a specific system for the formation of drug terminology.The principle of this -pyran-2 -yloxy)-6 -hydroxycyclohexyloxy)-4 system INN - INN ( International Nonproprietary Names - International hydroxy-2 -(hydroxymethyl)tetrahydrofuran Nonproprietary Names) lies in -3 -yloxy)tetrahydro-2 H-pyran-3, 4 -diol that its group affiliation is tentatively given in the name of the drug. 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 grouped into groups of narcotic drugs, hypnotics and sedatives, local anesthetics, analgesics, diuretics, etc. Chemical classification - drugs are grouped according to the common chemical structure and chemical properties. At the same time, in each chemical group of drugs there may be substances with different physiological activity. 9

Contemporary Issues 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 the synthesis of which new drugs with a different mechanism are needed actions Synthesis of compounds with programmable properties (modified processes in the known series of drugs, lead to the emergence of new structures in the evolution of microorganisms; resynthesis of natural phytosubstances, diseases; side effects, which has 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 man was completely dependent on outside world. In search of relief from illness and suffering, he used various remedies from his environment, the first of which appeared during the gathering period and were of plant 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. 14

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. 15

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 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 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 fight pathogens was a French pharmacist, Ernest Forunio (1872 -1949 B early works proposes the use of bismuth and arsenic compounds for the treatment of syphilis. His research "paved the way" for sulfonamide compounds and chemical substances 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 introduce the new discovery into production. The serum became available in 1895 (!), and the lives of thousands of children were saved. Inoculation of horses with diphtheria was the first step of many in the production of antidotes. The development of a polio vaccine in 1955 was a kind of culmination in this field. 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 advances in 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 " Medicines "M. D. Mashkovsky https: //vk. com/nspu_pc 23

is a science based on the general laws of chemical sciences, studying issues related to medicinal substances: their composition and structure, obtaining 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 the 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 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 with the help of these sciences physical and chemical methods of drug analysis and calculations in pharmaceutical analysis are carried out, 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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Information on the specialty

The Department of Organic Chemistry of the Faculty of Chemistry and Technology trains graduates in the specialty 04.05.01 "Fundamental and Applied Chemistry", specializations "Organic Chemistry" and "Pharmaceutical Chemistry". The staff of the department - highly qualified teachers and researchers: 5 doctors of science and 12 candidates of chemical sciences.

Professional activity alumni

Graduates are preparing for the following types of professional activities: research, research and production, teaching, design and organizational and managerial. A specialist chemist in the specialty "Fundamental and Applied Chemistry" will be ready to solve the following professional tasks: planning and setting up work, which includes the study of the composition, structure and properties of substances and chemical processes, creation and development of new promising materials and chemical technologies, solution of fundamental and applied problems in the field of chemistry and chemical technology; report preparation and scientific publications; scientific and pedagogical activity in a university, in a secondary specialized educational institution, in high school. Successful students engaged in scientific work can take an internship, take part in scientific conferences, olympiads and competitions of various levels, as well as present the results scientific work for publication in Russian and foreign scientific journals. Students have at their disposal chemical laboratories equipped with modern equipment and a computer class with the necessary literature and access to full-text electronic databases.

Specialists will:

• master the skills of a chemical experiment, basic synthetic and analytical methods for obtaining and studying chemicals and reactions;
• represent the main chemical, physical and technical aspects of chemical industrial production taking into account raw materials and energy costs;
• have the skills to work on modern educational and scientific equipment when conducting chemical experiments;
• have experience in working on serial equipment used in analytical and physico-chemical studies (gas-liquid chromatography, infrared and ultraviolet spectroscopy);
• own the methods of registration and processing of the results of chemical experiments.
• Possess the skills of planning, staging and conducting chemical experiments in the field of fine organic synthesis to obtain substances with desired useful properties

Students acquire knowledge in the field of fundamentals of inorganic chemistry, organic chemistry, physical and colloidal chemistry, analytical chemistry, planning of organic synthesis, chemistry of alicyclic and framework compounds, catalysis in organic synthesis, chemistry of organoelement compounds, pharmaceutical chemistry, modern methods analysis and quality control of medicines, basics of medicinal chemistry, basics of technology of pharmaceuticals, basics of pharmaceutical analysis. During practical exercises students gain skills in working in a modern chemical laboratory, master methods for obtaining and analyzing new compounds. Students have the skills to work on a gas-liquid chromatograph, infrared spectrophotometer, ultraviolet spectrophotometer. Students pass in-depth study foreign language(within 3 years).

In the process of learning, students master the methods of working on the analytical equipment of the Department of Organic Chemistry:

Chromato-mass spectrometer Finnigan Trace DSQ

NMR spectrometer JEOL JNM ECX-400 (400 MHz)

HPLC/MS with TOF mass spectrometer high resolution with ESI and DART ionization source, with diode array and fluorimetric detectors

Reveleris X2 Preparative Flash Chromatography System with UV and ELSD Detectors

Shimadzu IR Affinity-1 FT-IR Spectrometer

Waters Liquid Chromatograph with UV and Refractometric Detectors

TA Instruments DSC-Q20 Differential Scanning Calorimeter

Automatic C,H,N,S analyzer EuroVector EA-3000

Scanning spectrofluorimeter Varian Cary Eclipse

Automatic polarimeter AUTOPOL V PLUS

OptiMelt Automatic Melting Pointer

High Performance Computing Station

The training process provides for familiarization and chemical-technological practices in the laboratories of enterprises:

• CJSC "All-Russian Research Institute of Organic Synthesis of NK";
• JSC "Middle Volga Research Institute for Oil Refining" NK Rosneft;
• CJSC "TARKETT";
• Samara CHPP;
• OAO Syzransky Refinery Rosneft Oil Company;
• JSC "Giprovostokneft";
• OJSC Aviation Bearings Plant;
• OOO Novokuibyshevsky Plant of Oils and Additives, Rosneft Oil Company;
• CJSC "Neftekhimiya"
• LLC "Pranafarm"
• OOO "Ozon"
• JSC Electroshield
• FSUE GNPRKTS
• TsSKB-Progress
• OJSC "Baltika"
• PJSC SIBUR Holding, Togliatti

Successful students engaged in scientific work can undergo internships, take part in scientific conferences, olympiads and competitions of various levels, as well as submit the results of scientific work for publication in Russian and foreign scientific journals. Specialists who have received training in the specialty "Fundamental and Applied Chemistry" are in demand in the laboratories of state scientific centers and private companies, in research and analytical laboratories of various industries (chemical, food, metallurgical, pharmaceutical, petrochemical and gas production), in forensic laboratories; in customs laboratories; diagnostic centers; sanitary and epidemiological stations; environmental control organizations; certification testing centers; enterprises of the chemical industry, ferrous and non-ferrous metallurgy; in educational institutions of the secondary system vocational education; departments of labor protection and industrial sanitation; meteorological stations.

Qualification "Chemist. Chemistry teacher" with a specialization in "Organic Chemistry" or "Pharmaceutical Chemistry". Enrollment by USE results: chemistry, mathematics and Russian language. Duration of study: 5 years (full-time). Possible admission to graduate school.