Increasing the bioavalilability of mebendazole I. Influence of croscarmellose on dissolution rate, extent and mechanism in simulated gastric medium

 

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Article Title: Increasing the bioavalilability of mebendazole I. Influence of croscarmellose on dissolution rate,   extent and mechanism in simulated gastric medium
Authors: Ghafil F., Anuta V., Sarbu I., Toderescu C.D., Mircioiu I.
Affiliation: 1 Ministry of Health-Iraq,  2Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia, Bucharest, Romania 3 Faculty of Pharmacy, “Titu Maiorescu“ University, Bucharest, Romania
Abstract: ABSTRACT: The objective of the research presented in the paper was the obtaining of mebendazole tablets with increased bioavailability. Five solid formulations containing croscarmellose, an internally cross-linked sodium carboxymethylcellulose as superdisintegrant in 1%, 2 %, 3 %, 4 % and 5 % concentrations were prepared by direct compression and characterized in accordance with USP specifications. For the mebendazole quantitative analysis a HPLC method with UV detection was developed and validated. The effect of croscarmellose on rate, extent and mechanism of release of mebendazole from resulted formulations was studied. In vitro release kinetics was evaluated using USP Apparatus 2, in acidic medium (0.1N HCl) containing 1% sodium lauryl sulfate (SLS). The release of mebendazole was complete within 120 minutes. Rate and extent of release increased with croscarmellose concentration. The release mechanism was diffusion controlled, application of Higuchi law being excellent both in pre and post-disintegration phases. Peppas and Weibull models proved to be also applicable.
Keywords: mebendazole tablets, croscarmellose, bioavailability, diffusion controlled release
*Correspondence: Valentina Anuta, “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, 6 Traian Vuia Street, Bucharest, Romania, email: vali_anuta@yahoo.com