Biowaiver extension potential to BCS Class III high solubility-low permeability drugs: Bridging evidence for metformin immediate-release tablet

Ching Ling Cheng, Lawrence X. Yu, Hwei Ling Lee, Chyun Yu Yang, Chang Sha Lue, Chen Hsi Chou

研究成果: Article同行評審

108 引文 斯高帕斯(Scopus)

摘要

The biopharmaceutics classification system (BCS) allows biowaiver for rapid dissolving immediate-release (IR) products of Class I drugs (high solubility and high permeability). The possibility of extending biowaivers to Class III high solubility and low permeability drugs is currently under scrutiny. In vivo bioequivalence data of different formulations of Class III drugs would support such an extension. The objective of this work was to demonstrate the bioequivalence of two marketed IR tablet products of a Class III drug, metformin hydrochloride, that are rapidly dissolving and have similar in vitro dissolution profiles. The effect of race on the systemic exposure of metformin was also explored. A randomized, open-label, two-period crossover study was conducted in 12 healthy Chinese male volunteers. Each subject received a single-dose of 500 mg of each product after an overnight fasting. The plasma concentrations of metformin were followed for 24 h. No significant formulation effect was found for the bioequivalence metrics: areas under concentration-time curve (AUC0-t, AUC0-∞) and maximal concentration (Cmax). The 90% confidence intervals for the ratio of means were found within the acceptance range of 80-125% for the log-transformed data. Based on these results, it was concluded that the two IR products are bioequivalent. The pharmacokinetic parameters of metformin in Chinese for both products were similar and were in good agreement with those reported for metformin IR tablets in other ethnic populations. This study serves as an example for supporting biowaiver for BCS Class III drugs.

原文English
頁(從 - 到)297-304
頁數8
期刊European Journal of Pharmaceutical Sciences
22
發行號4
DOIs
出版狀態Published - 2004 七月

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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