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ACTA Pharmaceutica Sciencia
2009 , Vol 51 , Num 2
IN-VITRO RELEASE AND PHARMACOLOGICAL STUDY OF SYNTHESIZED VALPROIC ACID-DEXTRAN CONJUGATE
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, U.P., India
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The valproic acid - dextran conjugate was synthesized by preparing valproic acid acyl imidazole with N, N carbonyldiimidazole and in- situ condensation with dextran of molecular weight 110,000. The degree of substitution was estimated to be 16% and molecular weight was determined by viscometery method. In-vitro hydrolysis study of valproic acid dextran conjugate was performed in different buffer solutions (pH 1.2, 7.4 and 9.0). The hydrolysis followed first order kinetics and a faster hydrolysis was observed at pH 9 compared to pH 7.4. The conjugate was evaluated for anticonvulsant, hepatotoxicity and ulcerogenic activities. The results showed a remarkable reduction in hepatotoxicity and ulcerogenicity along with comparable anti-convulsant activity as parent drug valproic acid.
Keywords :
MACROMOLECULAR PRODRUG, CHARACTERIZATION, IN-VITRO HYDROLYSIS, HEPATOTOXICITY, ULCEROGENIC ACTIVITIES