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单次口服给药后各种奎尼丁制剂在人体中的相对生物利用度

[Relative bioavailability of various quinidine preparations in man after a single oral dose].

作者信息

Terhaag B, Gieszinger U

出版信息

Pharmazie. 1982 Dec;37(12):848-50.

PMID:7163373
Abstract

The bioavailability of quinidine sulfate in different preparations (quinidine in capsules as reference; Quinidine longo; Qunidine longo with either quinidine in the cover or in the nucleus, Quinidine Duriles) was investigated in 8 healthy volunteers in plasma and urine in a crossover design. There are no differences in the AUCo infinitey and in the eliminated amount in urine after infinit time. Quinidine longo possesses two maxima at 0.8 +/- 0.1 h and at 3.1 +/- 0.2 h. These maxima are caused by the liberation from the cover and the nucleus. The quotients of retardation (RD = ratio of the duration at 1/2 Cpmax, RC = ratio of 1/2 Cpmax, quinidine sulfate as reference) is calculated for Quinidine longo: RD = 1.42 +/- 0.14, RC = 0.75 +/- 0,05 and for Quinidine Duriles: RD = 1.79 +/- 0.21, RC = 0.52 +/- 0.07. The effect of retardation of Quinidine longo is not so much as that of Quinidine Duriles. However there are no statistic differences for RD in contrast to RC between these two retard-preparations.

摘要

采用交叉设计,在8名健康志愿者中研究了不同制剂(以胶囊中的奎尼丁为对照;长效奎尼丁;长效奎尼丁的包衣或内核中含有奎尼丁的制剂,杜氏奎尼丁)中硫酸奎尼丁在血浆和尿液中的生物利用度。曲线下面积(AUCo∞)和无限时间后尿液中的消除量没有差异。长效奎尼丁在0.8±0.1小时和3.1±0.2小时有两个峰值。这些峰值是由包衣和内核中的释放引起的。计算了长效奎尼丁的延迟商(RD = 1/2 Cpmax持续时间的比值,RC = 1/2 Cpmax的比值,以硫酸奎尼丁为对照):RD = 1.42±0.14,RC = 0.75±0.05,杜氏奎尼丁的RD = 1.79±0.21,RC = 0.52±0.07。长效奎尼丁的延迟作用不如杜氏奎尼丁。然而,与这两种缓释制剂的RC相比,RD没有统计学差异。

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