市售地尔硫䓬制剂的生物不等效性。

Bioinequivalence of marketed diltiazem preparations.

作者信息

Joshi M V, Gokhale P C, Pohujani S M, Dalvi S S, Karandikar S M, Kshirsagar N A

机构信息

Department of Pharmacology, Seth GS Medical College, Parel, Bombay, India.

出版信息

Eur J Clin Pharmacol. 1990;39(2):189-90. doi: 10.1007/BF00280058.

DOI:10.1007/BF00280058

PMID:2253673

Abstract

A bioequivalence study of three brands of regular diltiazem--Angizem (A), Dilzem (B) and Herbesser (C) has been carried out in 5 healthy, male volunteers. After a single oral dose of 60 mg of each preparation, the mean AUC (0-8 h) and Cmax of preparation B was significantly higher than of brands A and C. The tmax of A and B was significantly lower than of C. B had a higher dissolution rate in vitro (98.8% dissolved in 45 min) than A and C. Thus, there was bioinequivalence of the three brands of diltiazem, due partly to differences in dissolution and perhaps in part to a first pass effect.

摘要

对5名健康男性志愿者进行了三种品牌常规地尔硫䓬——安其敏（A）、地尔心（B）和恬尔心（C）的生物等效性研究。在单次口服每种制剂60毫克后，制剂B的平均AUC（0 - 8小时）和Cmax显著高于品牌A和C。A和B的tmax显著低于C。B在体外的溶出率更高（45分钟内溶解98.8%），高于A和C。因此，三种品牌的地尔硫䓬存在生物不等效性，部分原因是溶出差异，也可能部分归因于首过效应。