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In vivo pharmacokinetics in human volunteers: oral administered guar gum-based colon-targeted 5-fluorouracil tablets.
Eur J Pharm Sci. 2003 Aug; 19(5):355-62.EJ

Abstract

The objective of the present study is to compare the guar gum-based colon-targeted tablets of 5-fluorouracil against an immediate release tablet by in vitro dissolution and in vivo pharmacokinetic studies in human volunteers. Twelve healthy volunteers participated in the study. 5-Fluorouracil was administered at a dose of 50 mg both in immediate release tablet and colon-targeted tablet. On oral administration of colon-targeted tablets, 5-fluorouracil started appearing in the plasma at 6 h, and reached the peak concentration (C(max) of 216+/-15 ng/ml) at 7.6+/-0.1 h (T(max)), whereas the immediate release tablets produced peak plasma concentration (C(max) of 278+/-21 ng/ml) at 0.6+/-0.01 h (T(max)). The AUC(0- infinity) for 5-fluorouracil from colon-targeted tablet and immediate release tablet were found to be 617+/-39 and 205+/-21 ng/ml/h, respectively. Colon-targeted tablets showed delayed t(max), delayed absorption time (t(a)), decreased C(max) and decreased absorption rate constant when compared to the immediate release tablets. The results of the study indicated that the guar gum-based colon-targeted formulation did not release the drug in stomach and small intestine, but delivered it to the colon resulting in a slow absorption of the drug and making it available for local action in colon.

Authors+Show Affiliations

Krishnaiah YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, 530 003, India. krishnaysr112@rediffmail.com
Satyanarayana V
No affiliation info available
Dinesh Kumar B
No affiliation info available
Karthikeyan RS
No affiliation info available
Bhaskar P
No affiliation info available

MeSH

AdolescentAdultAntimetabolites, AntineoplasticArea Under CurveChromatography, High Pressure LiquidColonDrug Delivery SystemsExcipientsFemaleFluorouracilGalactansHalf-LifeHumansIntestinal AbsorptionMaleMannansPlant GumsSolubilityTablets

Pub Type(s)

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

Language

eng

PubMed ID

12907286

Citation

Krishnaiah, Y S R., et al. "In Vivo Pharmacokinetics in Human Volunteers: Oral Administered Guar Gum-based Colon-targeted 5-fluorouracil Tablets." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 19, no. 5, 2003, pp. 355-62.
Krishnaiah YS, Satyanarayana V, Dinesh Kumar B, et al. In vivo pharmacokinetics in human volunteers: oral administered guar gum-based colon-targeted 5-fluorouracil tablets. Eur J Pharm Sci. 2003;19(5):355-62.
Krishnaiah, Y. S., Satyanarayana, V., Dinesh Kumar, B., Karthikeyan, R. S., & Bhaskar, P. (2003). In vivo pharmacokinetics in human volunteers: oral administered guar gum-based colon-targeted 5-fluorouracil tablets. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 19(5), 355-62.
Krishnaiah YS, et al. In Vivo Pharmacokinetics in Human Volunteers: Oral Administered Guar Gum-based Colon-targeted 5-fluorouracil Tablets. Eur J Pharm Sci. 2003;19(5):355-62. PubMed PMID: 12907286.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vivo pharmacokinetics in human volunteers: oral administered guar gum-based colon-targeted 5-fluorouracil tablets. AU - Krishnaiah,Y S R, AU - Satyanarayana,V, AU - Dinesh Kumar,B, AU - Karthikeyan,R S, AU - Bhaskar,P, PY - 2003/8/9/pubmed PY - 2004/3/9/medline PY - 2003/8/9/entrez SP - 355 EP - 62 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 19 IS - 5 N2 - The objective of the present study is to compare the guar gum-based colon-targeted tablets of 5-fluorouracil against an immediate release tablet by in vitro dissolution and in vivo pharmacokinetic studies in human volunteers. Twelve healthy volunteers participated in the study. 5-Fluorouracil was administered at a dose of 50 mg both in immediate release tablet and colon-targeted tablet. On oral administration of colon-targeted tablets, 5-fluorouracil started appearing in the plasma at 6 h, and reached the peak concentration (C(max) of 216+/-15 ng/ml) at 7.6+/-0.1 h (T(max)), whereas the immediate release tablets produced peak plasma concentration (C(max) of 278+/-21 ng/ml) at 0.6+/-0.01 h (T(max)). The AUC(0- infinity) for 5-fluorouracil from colon-targeted tablet and immediate release tablet were found to be 617+/-39 and 205+/-21 ng/ml/h, respectively. Colon-targeted tablets showed delayed t(max), delayed absorption time (t(a)), decreased C(max) and decreased absorption rate constant when compared to the immediate release tablets. The results of the study indicated that the guar gum-based colon-targeted formulation did not release the drug in stomach and small intestine, but delivered it to the colon resulting in a slow absorption of the drug and making it available for local action in colon. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/12907286/In_vivo_pharmacokinetics_in_human_volunteers:_oral_administered_guar_gum_based_colon_targeted_5_fluorouracil_tablets_ DB - PRIME DP - Unbound Medicine ER -