DOSAGE FORM DEVELOPMENT BASED ON AMIDES OF 5-BROMNICOTINIC ACID AND STUDY OF PHYSICAL AND MECHANICAL CHARACTERISTICS OF THE TABLET MASS
Abstract and keywords
Abstract:
According to the WHO report on statistics of cardiovascular diseases in 34 countries of the world, fatal outcomes from heart and vascular pathologies occupy one of the first places. Accordingly, the search for new effective drugs for the treatment of cardiovascular diseases today remains an urgent task. In the Decree of the President of the Russian Federation on the national goals and strategic objectives of Russia's development, a large block of tasks is devoted to the problems of medicine. The tasks are set to increase life expectancy. In addition, mortality rates for cardiovascular diseases should be reduced to 450 cases per 100 thousand population. A large number of drugs are based on nicotinic acid, isonicotinic acid and their derivatives. Nicotinic acid has a pronounced vasodilatory effect on peripheral vessels and brain vessels, but the use of its derivatives is primarily due to less pronounced side effects. For effective treatment of heart disease, drugs are used in the form of liquid and solid dosage forms. The former allows to obtain the fastest therapeutic effect, and the latter is convenient for prophylactic use. Previous works of the authors showed the possibility of practical synthesis of amides of 5-bromnicotinic acid on the basis of some amines of aliphatic and aromatic series, studied their physical properties and biological activity. In the process of work the solid dosage form - tablet was selected, calculations of optimal amount of active substance were carried out, selection of auxiliary components was carried out. As auxiliary components selected: microcrystalline cellulose, potato starch, calcium stearate. The technological process of tablet manufacturing includes several stages, one of the main stages is pressing. The technological characteristics - strength and density of samples depending on the pressing pressure of powdered material containing biologically active substances were studied, tablets were obtained by pressing method and pressing modes were selected.

Keywords:
BIOLOGICALLY ACTIVE SUBSTANCE, DOSAGE FORM, PHYSICAL AND MECHANICAL CHARACTERISTICS, 5-BROMNICOTINIC ACID DERIVATIVES
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