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Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of tinidazole in healthy human volunteers.
Drug Deliv. 2003 Oct-Dec; 10(4):263-8.DD

Abstract

The aim of the present investigation was to determine the in vivo availability of guar gum-based colon-targeted tablets of tinidazole in comparison with immediate release tablets of tinidazole in human volunteers. Six healthy volunteers participated in the study, and a cross-over design was used. The plasma concentration of tinidazole was estimated by HPLC. The pharmacokinetic parameters were calculated from the plasma concentration of tinidazole versus time data. The immediate release tablets of tinidazole produced a peak plasma concentration (Cmax of 3239 +/- 428 ng/ml) at 1.04 +/- 0.32 hr (Tmax), whereas colon-targeted tablets produced peak plasma concentration (Cmax of 2158 +/- 78 ng/ml) at 14.9 +/- 1.6 hr. The delayed Tmax, decreased Cmax, and Ka, and unaltered bioavailability and elimination half-life of tinidazole from guar gum-based colon-targeted tinidazole tablets, in comparison with the immediate tablets, indicated that the drug was not released in the stomach and small intestine but delivered to the colon. Slow absorption of the drug from the less absorptive colon might result in the availability of the drug for local action in the colon. The guar gum-based colon-targeted tablets of tinidazole may be useful in providing an effective and safe therapy of intestinal amoebiasis.

Authors+Show Affiliations

Krishnaiah YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India. krishnaysr112@rediffmail.com
Muzib YI
No affiliation info available
Bhaskar P
No affiliation info available
Satyanarayana V
No affiliation info available
Latha K
No affiliation info available

MeSH

AdultArea Under CurveColonDrug Delivery SystemsDrug Evaluation, PreclinicalGalactansHumansMaleMannansPlant GumsTabletsTinidazole

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

14612342

Citation

Krishnaiah, Y S R., et al. "Pharmacokinetic Evaluation of Guar Gum-based Colon-targeted Drug Delivery Systems of Tinidazole in Healthy Human Volunteers." Drug Delivery, vol. 10, no. 4, 2003, pp. 263-8.
Krishnaiah YS, Muzib YI, Bhaskar P, et al. Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of tinidazole in healthy human volunteers. Drug Deliv. 2003;10(4):263-8.
Krishnaiah, Y. S., Muzib, Y. I., Bhaskar, P., Satyanarayana, V., & Latha, K. (2003). Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of tinidazole in healthy human volunteers. Drug Delivery, 10(4), 263-8.
Krishnaiah YS, et al. Pharmacokinetic Evaluation of Guar Gum-based Colon-targeted Drug Delivery Systems of Tinidazole in Healthy Human Volunteers. Drug Deliv. 2003 Oct-Dec;10(4):263-8. PubMed PMID: 14612342.
* 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 tinidazole in healthy human volunteers. AU - Krishnaiah,Y S R, AU - Muzib,Y Indira, AU - Bhaskar,P, AU - Satyanarayana,V, AU - Latha,K, PY - 2003/11/13/pubmed PY - 2004/7/23/medline PY - 2003/11/13/entrez SP - 263 EP - 8 JF - Drug delivery JO - Drug Deliv VL - 10 IS - 4 N2 - The aim of the present investigation was to determine the in vivo availability of guar gum-based colon-targeted tablets of tinidazole in comparison with immediate release tablets of tinidazole in human volunteers. Six healthy volunteers participated in the study, and a cross-over design was used. The plasma concentration of tinidazole was estimated by HPLC. The pharmacokinetic parameters were calculated from the plasma concentration of tinidazole versus time data. The immediate release tablets of tinidazole produced a peak plasma concentration (Cmax of 3239 +/- 428 ng/ml) at 1.04 +/- 0.32 hr (Tmax), whereas colon-targeted tablets produced peak plasma concentration (Cmax of 2158 +/- 78 ng/ml) at 14.9 +/- 1.6 hr. The delayed Tmax, decreased Cmax, and Ka, and unaltered bioavailability and elimination half-life of tinidazole from guar gum-based colon-targeted tinidazole tablets, in comparison with the immediate tablets, indicated that the drug was not released in the stomach and small intestine but delivered to the colon. Slow absorption of the drug from the less absorptive colon might result in the availability of the drug for local action in the colon. The guar gum-based colon-targeted tablets of tinidazole may be useful in providing an effective and safe therapy of intestinal amoebiasis. SN - 1071-7544 UR - https://www.unboundmedicine.com/medline/citation/14612342/Pharmacokinetic_evaluation_of_guar_gum_based_colon_targeted_drug_delivery_systems_of_tinidazole_in_healthy_human_volunteers_ DB - PRIME DP - Unbound Medicine ER -