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Biowaiver extension potential to BCS Class III high solubility-low permeability drugs: bridging evidence for metformin immediate-release tablet.
Eur J Pharm Sci. 2004 Jul; 22(4):297-304.EJ

Abstract

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-infinity) 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.

Authors+Show Affiliations

Department of Pharmacy, Chia-Nan University of Pharmacy and Science, Tainan, Taiwan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

15196586

Citation

Cheng, Ching-Ling, et al. "Biowaiver Extension Potential to BCS Class III High Solubility-low Permeability Drugs: Bridging Evidence for Metformin Immediate-release Tablet." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 22, no. 4, 2004, pp. 297-304.
Cheng CL, Yu LX, Lee HL, et al. Biowaiver extension potential to BCS Class III high solubility-low permeability drugs: bridging evidence for metformin immediate-release tablet. Eur J Pharm Sci. 2004;22(4):297-304.
Cheng, C. L., Yu, L. X., Lee, H. L., Yang, C. Y., Lue, C. S., & Chou, C. H. (2004). Biowaiver extension potential to BCS Class III high solubility-low permeability drugs: bridging evidence for metformin immediate-release tablet. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 22(4), 297-304.
Cheng CL, et al. Biowaiver Extension Potential to BCS Class III High Solubility-low Permeability Drugs: Bridging Evidence for Metformin Immediate-release Tablet. Eur J Pharm Sci. 2004;22(4):297-304. PubMed PMID: 15196586.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biowaiver extension potential to BCS Class III high solubility-low permeability drugs: bridging evidence for metformin immediate-release tablet. AU - Cheng,Ching-Ling, AU - Yu,Lawrence X, AU - Lee,Hwei-Ling, AU - Yang,Chyun-Yu, AU - Lue,Chang-Sha, AU - Chou,Chen-Hsi, PY - 2003/08/07/received PY - 2004/03/17/revised PY - 2004/03/29/accepted PY - 2004/6/16/pubmed PY - 2005/4/23/medline PY - 2004/6/16/entrez SP - 297 EP - 304 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 22 IS - 4 N2 - 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-infinity) 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. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/15196586/Biowaiver_extension_potential_to_BCS_Class_III_high_solubility_low_permeability_drugs:_bridging_evidence_for_metformin_immediate_release_tablet_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928098704000958 DB - PRIME DP - Unbound Medicine ER -