Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers

摘要

The pharmacokinetic evaluation of guar gum-based colon-targeted tablets of mebendazole against an immediate release tablet was carried out in human volunteers. Six healthy volunteers participated in the study and a crossover design was followed. Mebendazole was administered at a dose of 50 mg both in immediate release tablet and colon-targeted tablets. On oral administration of colon-targeted tablets, mebendazole started appearing in the plasma at 5 h, and reached the peak concentration (C-max of 25.7+/-2.6 ng/ml) at 9.4+/-1.7 h (T-max) whereas the immediate release tablets produced peak plasma concentration (C-max of 37.2+/-6.8 ng/ml) at 3.4+/-0.9 h (T-max). Colon-targeted tablets showed delayed t(max) and absorption time, and decreased C-max and absorption rate constant when compared to the immediate release tablets. The results of the study indicated that the guar gum-based colon-targeted tablets of mebendazole did not release the drug in stomach and small intestine, but delivered the drug to the colon resulting in a slow absorption of the drug and making the drug available for local action in the colon. (C) 2002 Elsevier Science B.V. All rights reserved. [References: 19]