期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 66, 期 -, 页码 163-172出版社
ELSEVIER
DOI: 10.1016/j.ejps.2014.10.002
关键词
Bioequivalence; Dissolution; Similarity factor; Numerical convolution; First-order; Simulation
资金
- National Science and Technology Major Projects for Major New Drugs Innovation and Development (Beijing, China) [2012ZX09303014-001]
The present study examined the agreement between in vitro dissolution f2 similarity and in vivo bioequivalence criteria for BCS class II drugs. Dissolution test profiles were generated using the First-order model with varied dissolution parameters around the standard values of a reference profile. The in vivo curves were derived from in vitro dissolution profiles with the drug's pharmacokinetics parameters by numerical convolution method, The C-max, T-max, AUC(0-t) and AUC(0-infinity), obtained from in vivo test and reference concentration time curves were compared, and the CmaxR (C-max, ratio), T(max)Dif (Tin. difference), AUC(0-t)R (AUC(0-t) ratio) and AUC(0-infinity)R (AUC(0-infinity) ratio) were determined. The relationships between CmaxR, AUC(0-t)R, AUC(0-infinity)R, 12 and the First-order model parameters demonstrated that the Similarity Region 1 enclosed by the 12 contour line labeled 50 was completely within the Bioequivalence Region enclosed by the contour lines labeled 0.80 and 1.20 of AUC(0-t)R, AUC(0-infinity)R, and CmaxR, and the Similarity Region 2 enclosed by the 12 contour line labeled 35 was nearly overlapped with the Bioequivalence Region, but did not exactly match. The results indicate that the public standard for in vitro dissolution 12 similarity criterion (f2 >= 50) is probably slightly conservative and may be widened to an appropriate lower critical value. (C) 2014 Elsevier B.V. All rights reserved.
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