DEVELOPMENT OF THE PHARMACEUTICAL INDUSTRY

DEVELOPMENT OF THE PHARMACEUTICAL INDUSTRY

Development of new drugs is one of the strategic directions of development of pharmaceutical industry of the Republic of Tajikistan. When creating new generation drugs, scientists focus on achieving high bioavailability, targeted delivery, low toxicity, as well as regulated release of pharmacologically active component from the dosage form. Achievement of these requirements for modern innovative drugs can be achieved by microencapsulation with the help of cyclodextrins.

Cyclodextrins (CD, CD), molecules of natural origin, were discovered in 1891 by Villiers A. while studying the metabolic products of Bacillus amylobacter, and were first named "cellulosins". In 1903, F. Schardinger reported the preparation of two different crystalline cellulosin-like products, which he called α- and β-dextrins. Further studies led to the development of an optimal method of synthesis and also proved the cyclic structure of dextrins, which was the basis for renaming them as cyclodextrins (CDs). By 1953, K. Freudenberg et al. obtained the first patent for the use of CDs in drug manufacturing technology. However, low synthesis volumes and high production costs hampered the widespread use of CDs in practice. In the late 70s of the XX century it became possible to synthesize highly purified CDs and their derivatives, which stimulated the growth of their use in various fields: agroindustry, cosmetology, pharmacology, chemistry and others.

Due to their structure, CDs are capable of forming water-soluble inclusion complexes with various organic substrates. The incorporation of a guest molecule into the CD cavity promotes the acquisition of new physicochemical properties, among which the most obvious is the increase in water solubility. The different influence of aqueous and nonaqueous media on molecular complexation suggests the possibility of changing the selectivity of CDs and the use of solvent to obtain molecular complexes with a given stability and energy of reactions of their formation. This assumption is based on the understanding of the role of the solvent not only as a medium, but also as a participant of chemical interactions.

CDs are widely used in pharmaceuticals to prepare various dosage forms of poorly water-soluble compounds. CDs are able to form inclusion complexes by placing various drug substances in the cavities of their molecules and selectively deliver them to human cells, tissues and organs. Such a method allows to reduce the side effect of drugs and enhance the effect of their main effect. Cyclodextrins, known for more than 100 years, have found their active application only in recent decades. Their ability to form inclusion complexes with increased solubility, stability, bioavailability and other properties of guest molecules has forced to reconsider the possibility of using previously unaccepted compounds and expand the range of application of already known drugs. In this regard, studies of complexation of CD with drugs are of great practical importance.


Kabirov J.N. - c.ch.s., assistant at the department of pharmaceutical and toxicological chemistry

Translated Ismoilov R.


22.02.2024 512
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