INCREASING THE BIOAVALILABILITY OF MEBENDAZOLE II. INFLUENCE OF CROSCARMELLOSE ON DISSOLUTION RATE, EXTENT AND MECHANISM IN SIMULATED INTESTINAL MEDIUM

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 properti...

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Bibliographic Details
Published in:Studia Universitatis "Vasile Goldiș". Seria ș̦tiințele vieții 2017-01, Vol.27 (1), p.39-46
Main Authors: Ghafil, Firas, Anuta, Valentina, Sarbu, Iulian, Toderescu, Corina Dalia, Mircioiu, Ion
Format: Article
Language:English
Subjects:
Bioavailability
Chromatography
Classification
Controlled release
Dissolution
Drug delivery systems
Experiments
High-performance liquid chromatography
International conferences
Intestine
Mebendazole
Methods
Pharmaceutical industry
Quantitative analysis
Sodium
Tablets
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Summary: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
ISSN:1584-2363
1842-7963