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Pharmacokinetic evaluation of guar gum-based colon-targeted oral drug delivery systems of metronidazole in healthy volunteers.
Eur J Drug Metab Pharmacokinet. 2003 Oct-Dec; 28(4):287-94.EJ

Abstract

The present study was carried out to find the in vivo performance of guar gum-based colon-targeted tablets of metronidazole as compared to an immediate release tablets in human volunteers. Six healthy volunteers participated in the study and a crossover design was used. Blood samples were obtained at different time intervals and the plasma concentration of metronidazole was estimated by reverse phase HPLC. The immediate release tablets of metronidazole produced peak plasma concentration (Cmax of 2990 +/- 574.6 ng/mL) within 2.8 +/- 0.6 h. On oral administration of colon-targeted tablets, metronidazole started appearing in the plasma between 5 h and 8 h, and reached the peak concentration (Cmax of 1940.0 +/- 528.4 ng/mL) at 11.1 +/- 2.1 h (Tmax). The AUC(0-infinity) and t(1/2) of metronidazole were unaltered on administering the drug as a colon-targeted tablet indicating that the extent of absorption and elimination were not affected by targeting the drug to the colon. However, colon-targeted tablets showed delayed tmax and absorption time (ta), decreased Cmax and decreased absorption rate constant as compared to immediate release tablets. This in turn indicated that metronidazole was delivered to the colon resulting in a slow absorption of the drug and making it available for local action in the colon.

Authors+Show Affiliations

Krishnaiah YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530 003, India.
Veer Raju P
No affiliation info available
Dinesh Kumar B
No affiliation info available
Jayaram B
No affiliation info available
Rama B
No affiliation info available
Raju V
No affiliation info available
Bhaskar P
No affiliation info available

MeSH

AdolescentAdultAntiprotozoal AgentsArea Under CurveChromatography, High Pressure LiquidColonDrug Delivery SystemsExcipientsFemaleGalactansHalf-LifeHumansIntestinal AbsorptionMaleMannansMetronidazolePlant GumsSolubilityTablets

Pub Type(s)

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

Language

eng

PubMed ID

14743970

Citation

Krishnaiah, Y S R., et al. "Pharmacokinetic Evaluation of Guar Gum-based Colon-targeted Oral Drug Delivery Systems of Metronidazole in Healthy Volunteers." European Journal of Drug Metabolism and Pharmacokinetics, vol. 28, no. 4, 2003, pp. 287-94.
Krishnaiah YS, Veer Raju P, Dinesh Kumar B, et al. Pharmacokinetic evaluation of guar gum-based colon-targeted oral drug delivery systems of metronidazole in healthy volunteers. Eur J Drug Metab Pharmacokinet. 2003;28(4):287-94.
Krishnaiah, Y. S., Veer Raju, P., Dinesh Kumar, B., Jayaram, B., Rama, B., Raju, V., & Bhaskar, P. (2003). Pharmacokinetic evaluation of guar gum-based colon-targeted oral drug delivery systems of metronidazole in healthy volunteers. European Journal of Drug Metabolism and Pharmacokinetics, 28(4), 287-94.
Krishnaiah YS, et al. Pharmacokinetic Evaluation of Guar Gum-based Colon-targeted Oral Drug Delivery Systems of Metronidazole in Healthy Volunteers. Eur J Drug Metab Pharmacokinet. 2003 Oct-Dec;28(4):287-94. PubMed PMID: 14743970.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetic evaluation of guar gum-based colon-targeted oral drug delivery systems of metronidazole in healthy volunteers. AU - Krishnaiah,Y S R, AU - Veer Raju,P, AU - Dinesh Kumar,B, AU - Jayaram,B, AU - Rama,B, AU - Raju,V, AU - Bhaskar,P, PY - 2004/1/28/pubmed PY - 2004/9/21/medline PY - 2004/1/28/entrez SP - 287 EP - 94 JF - European journal of drug metabolism and pharmacokinetics JO - Eur J Drug Metab Pharmacokinet VL - 28 IS - 4 N2 - The present study was carried out to find the in vivo performance of guar gum-based colon-targeted tablets of metronidazole as compared to an immediate release tablets in human volunteers. Six healthy volunteers participated in the study and a crossover design was used. Blood samples were obtained at different time intervals and the plasma concentration of metronidazole was estimated by reverse phase HPLC. The immediate release tablets of metronidazole produced peak plasma concentration (Cmax of 2990 +/- 574.6 ng/mL) within 2.8 +/- 0.6 h. On oral administration of colon-targeted tablets, metronidazole started appearing in the plasma between 5 h and 8 h, and reached the peak concentration (Cmax of 1940.0 +/- 528.4 ng/mL) at 11.1 +/- 2.1 h (Tmax). The AUC(0-infinity) and t(1/2) of metronidazole were unaltered on administering the drug as a colon-targeted tablet indicating that the extent of absorption and elimination were not affected by targeting the drug to the colon. However, colon-targeted tablets showed delayed tmax and absorption time (ta), decreased Cmax and decreased absorption rate constant as compared to immediate release tablets. This in turn indicated that metronidazole was delivered to the colon resulting in a slow absorption of the drug and making it available for local action in the colon. SN - 0378-7966 UR - https://www.unboundmedicine.com/medline/citation/14743970/Pharmacokinetic_evaluation_of_guar_gum_based_colon_targeted_oral_drug_delivery_systems_of_metronidazole_in_healthy_volunteers_ DB - PRIME DP - Unbound Medicine ER -