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Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers.
J Control Release. 2003 Feb 14; 88(1):95-103.JC

Abstract

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.

Authors+Show Affiliations

Krishnaiah YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, 530 003, India. krishnaiah112@rediffmail.com
Veer Raju P
No affiliation info available
Dinesh Kumar B
No affiliation info available
Satyanarayana V
No affiliation info available
Karthikeyan RS
No affiliation info available
Bhaskar P
No affiliation info available

MeSH

AdolescentAdultAlgorithmsAntinematodal AgentsArea Under CurveChromatography, High Pressure LiquidColonDrug Delivery SystemsGalactansHalf-LifeHumansMaleMannansMebendazolePlant GumsSolubilityTablets

Pub Type(s)

Clinical Trial
Controlled Clinical Trial
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

12586507

Citation

Krishnaiah, Y S R., et al. "Pharmacokinetic Evaluation of Guar Gum-based Colon-targeted Drug Delivery Systems of Mebendazole in Healthy Volunteers." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 88, no. 1, 2003, pp. 95-103.
Krishnaiah YS, Veer Raju P, Dinesh Kumar B, et al. Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers. J Control Release. 2003;88(1):95-103.
Krishnaiah, Y. S., Veer Raju, P., Dinesh Kumar, B., Satyanarayana, V., Karthikeyan, R. S., & Bhaskar, P. (2003). Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers. Journal of Controlled Release : Official Journal of the Controlled Release Society, 88(1), 95-103.
Krishnaiah YS, et al. Pharmacokinetic Evaluation of Guar Gum-based Colon-targeted Drug Delivery Systems of Mebendazole in Healthy Volunteers. J Control Release. 2003 Feb 14;88(1):95-103. PubMed PMID: 12586507.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of mebendazole in healthy volunteers. AU - Krishnaiah,Y S R, AU - Veer Raju,P, AU - Dinesh Kumar,B, AU - Satyanarayana,V, AU - Karthikeyan,R S, AU - Bhaskar,P, PY - 2003/2/15/pubmed PY - 2003/11/13/medline PY - 2003/2/15/entrez SP - 95 EP - 103 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 88 IS - 1 N2 - 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. SN - 0168-3659 UR - https://www.unboundmedicine.com/medline/citation/12586507/Pharmacokinetic_evaluation_of_guar_gum_based_colon_targeted_drug_delivery_systems_of_mebendazole_in_healthy_volunteers_ DB - PRIME DP - Unbound Medicine ER -