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[奎尼丁缓释制剂在健康志愿者体内的相对生物利用度及其对血压和心电图的影响(作者译)]

[Relative bioavailability and influence of a quinidine retard-formulation on blood-pressure and ECG in healthy volunteers (author's transl)].

作者信息

Knapp W, Lechleitner P

出版信息

Arzneimittelforschung. 1981;31(9):1482-6.

PMID:7197960
Abstract

In the present study on healthy volunteers plasma levels of (5-vinyl-2-quinuclidinyl)--(6-methoxy-4-quinolyl)-methanol (quinidine, Chinidinorm) and ECG were studied after administration of a single oral dose of 492 mg quinidine-base as quinidine-bisulfate in form of two slow-release formulations with different galenics. Both formulations show similar retard-characteristics. Serum concentration curve, area under the serum concentration curve, peak serum quinidine levels (1.44 mg/l for both formulations), apparent elimination rate constant (k2 = 0.0882 and 0.0805 h-1, respectively) and elimination half-life show no significant differences. Under the influence of quinidine there is a small but significant increase of the systolic blood pressure during peak serum quinidine levels. The ECG shows increased QT-duration, T-peak and R-peak. There are no significant differences between the two slow-release formulations.

摘要

在本项针对健康志愿者的研究中,以两种不同药剂学形式的硫酸奎尼丁给予单剂量492mg奎尼丁碱口服后,研究了(5-乙烯基-2-奎宁环基)-(6-甲氧基-4-喹啉基)-甲醇(奎尼丁,Chinidinorm)的血浆水平及心电图。两种制剂均显示出相似的缓释特性。血清浓度曲线、血清浓度曲线下面积、血清奎尼丁峰值水平(两种制剂均为1.44mg/l)、表观消除速率常数(分别为k2 = 0.0882和0.0805 h-1)及消除半衰期均无显著差异。在奎尼丁影响下,血清奎尼丁峰值水平时收缩压有小幅但显著升高。心电图显示QT间期、T波峰值和R波峰值增加。两种缓释制剂之间无显著差异。

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