消旋维拉帕米两种不同剂型单剂量给药后S-维拉帕米的血浆浓度。

Plasma concentrations of S-verapamil after single doses of two different galenic formulations of racemic verapamil.

作者信息

Harder S, Siewert M, Thürmann P, Blume H, Rietbrock N, Siewert B

机构信息

Department of Clinical Pharmacology, University Hospital, Frankfurt/Main, Fed. Rep. of Germany.

出版信息

Arzneimittelforschung. 1993 May;43(5):520-2.

PMID:8328995

Abstract

The results of enantioselective analysis of verapamil (CAS 52-53-9) in plasma samples obtained at tmax after single dose applications of a 80 mg fast dissoluting (IR) tablet, a controlled release (CR) formulation (240 mg) and an intravenous injection of 5 mg verapamil are reported. The mean fraction of S-verapamil obtained in samples containing the Cmax of racemic verapamil was somewhat smaller after application of the IR-form than observed with the CR formulation. (IR = 15.8 +/- 3.8%; CR = 18.8 +/- 2.0%; p < 0.01), after the intravenous application the mean S-fraction was 32.8 +/- 1.4%. In vitro dissolution tests of the two oral preparations prove that the isomers were released as racemate.

摘要

报道了单次服用80mg速溶（IR）片、控释（CR）制剂（240mg）以及静脉注射5mg维拉帕米后，在达峰时间（tmax）采集的血浆样本中维拉帕米（CAS 52 - 53 - 9）对映体选择性分析的结果。含有外消旋维拉帕米Cmax的样本中，服用IR制剂后获得的S - 维拉帕米平均比例，比CR制剂的略小。（IR = 15.8 +/- 3.8%；CR = 18.8 +/- 2.0%；p < 0.01），静脉注射后，S - 比例平均为32.8 +/- 1.4%。两种口服制剂的体外溶出试验证明，异构体以消旋体形式释放。