Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers.
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.
Krishnaiah
Y S R
YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, 530 003, India. krishnaiah112@rediffmail.com
Veer Raju
P
P
Dinesh Kumar
B
B
Satyanarayana
V
V
Karthikeyan
R S
RS
Bhaskar
P
P
D000293:Adolescent; D000328:Adult; D000465:Algorithms; D000969:Antinematodal Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D003106:Colon / Q000378:metabolism*; D016503:Drug Delivery Systems; D005685:Galactans; D006207:Half-Life; D006801:Humans; D008297:Male; D008351:Mannans; D008463:Mebendazole / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D053149:Plant Gums; D012995:Solubility; D013607:Tablets
D000969:Antinematodal Agents; D005685:Galactans; D008351:Mannans; D053149:Plant Gums; D013607:Tablets; D008463:Mebendazole; C007894:guar gum