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Abstract
Abstract: Present study describes the synthesis and pharmacological characteristics of the 18-glycyrrhizic acid com-plex with nifedipine, molecular composition 1:4. The study showed that complex decreases arterial pressure at the dose of nifedipine 10 times smaller than the therapeutic dose. Antiarrhythmic effect of nifedipine in this complex was obtained at the dosage 29 times lower than that ensuring antihypertensive action. Keywords: Nifedipine, Glycyrrhizic acid, Drug delivery, Complexation. INTRODUCTION Nifedipine, dimethyl ether 2,6-dimethyl-4-(2'-nitrophenyl)- 1,4-dihydropyridine-3,5-dicarboxylate, one of the commonly used 1,4-dihydropyridine derivatives, is a selective slow calcium channel blocker. Its prevalence as an enteral antihypertensive agent can be explained both by pharmacological properties, which garner attention of practi-cal cardiologists again, and by technological availability of the pharmacon substance. As for the drug formulations for intravenous administration for acute care applications, some problems arise in their usage. In particular, administration of the recommended injection forms of the drug requires spe-cial precaution because the pharmacon solvent contains ethanol. Therefore, developing water-soluble forms of nifedipine suitable for parenteral administration is still a challenging problem. It is known that the use of carbohydrate-containing me-tabolites of microbial and plant origin for formation of pharmacon complexes is a rather promising approach to de-veloping novel drug carriers for known drugs. Cyclodextrins (CD) appear to be the highest in the list of the most exten-sively studied and practically used agents. Complexation of pharmacons using CD ensures im-proved water solubility of pharmacons, which frequently enhances their biovitality as well. In complexes with CD pharmacons are shown to have an elongated therapeutic ef-fect and enhanced resistance to early unwanted metabolism in the gastrointestinal tract. Complexes with CD are known for more than 70 phar-macons with different types of activity. Twenty CD com-plex-based drugs are produced commercially, including 7 preparations for injections [1-3]. The complexes of nifedip-ine with hydroxypropylmethyl cellulose [4, 5], with
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