Increasing the bioavalilability of mebendazole II. Influence of Croscarmellose on dissolution rate, extent and mechanism in simulated intestinal medium
November 17, 2014
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| Article Title: | Increasing the bioavalilability of mebendazole II. Influence of Croscarmellose on dissolution rate, extent and mechanism in simulated intestinal medium | ||
| Authors: | Ghafil F., Anuta V., Sarbu I.,Toderescu C.D., Mircioiu I. | ||
| Affiliation: | 2 1 Ministry of Health-Iraq Faculty 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: Objective of the research was the developing of tablets with increased rate and extent of release of mebendazole in intestine in order to improve its bioavailability and pharmacokinetic profile. Three solid formulations containing 1%, 2% and 3 % croscarmellose sodium, with superdisintegrant properties were prepared. For the quantitative assay of mebendazole a HPLC-UV method was developed and validated. Bioavailability was estimated by means of the in-vitro release kinetics using USP Apparatus 2, in Fasting State Simulated Intestinal Fluid (FaSSIF). Release of mebendazole in FaSSIF was poor (less than 10 % within 2 hours). Dissolution could be described by Higuchi law and Peppas law in both the swelling phase and post-errosion-disintegration phase, suggesting a diffusion controlled release. Both rate and extent of release increased with concentration of croscarmellose predicting a better bioavailability of mebendazole from the croscarmellose containing tablets. | ||
| Keywords: | mebendazole, croscarmellose, in vitro release, FaSSIF, intestinal suprasaturation | ||
| *Correspondence: | Valentina Anuta, “Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, 6 Traian Vuia Street, Bucharest, Romania, email: vali_anuta@yahoo.com |
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