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强心剂不同制剂中茶碱和乙羟茶碱的人体药代动力学(作者译)

[Human pharmacokinetics of theophylline and etofylline from different formulations of a cardiotonic (author's transl)].

作者信息

Erking W, Lücker P W, Niebch G, Thiemer K, Wetzelsberger K

出版信息

Arzneimittelforschung. 1981;31(2):371-9.

PMID:7194656
Abstract

Serum concentrations of theophylline and etofylline were analysed by a specific HPLC-method in 6 volunteers after i.v. and p.o. administration of the cardiotonic Cordalin ampoules, drops and dragees. Maximum serum concentrations were reached by theophylline an etofylline at about the same time: 1.0-1.2 h after Cordalin drops; 2.3-2.6 h after Cordalin dragees. The half-life of serum elimination was 5.0-7.2 h for theophylline and 5.5-6.9 h for etofylline. The absolute bioavailability of the two oral formulations was calculated from the areas under the serum curves. For theophylline it is complete from the dragees and 78% from drops. Etofylline, too, is highly bioavailable: 94% from the dragees, 84% from drops. From the kinetic data the conclusion can be drawn that accumulation of theophylline and etofylline will be negligible after Cordalin if administered according to prescribed directions.

摘要

采用特定的高效液相色谱法对6名志愿者静脉注射和口服强心剂科达林安瓿剂、滴剂和糖衣丸剂后的血清茶碱和乙羟茶碱浓度进行了分析。茶碱和乙羟茶碱在大致相同的时间达到血清最高浓度:科达林滴剂给药后1.0 - 1.2小时;科达林糖衣丸剂给药后2.3 - 2.6小时。血清消除半衰期茶碱为5.0 - 7.2小时,乙羟茶碱为5.5 - 6.9小时。两种口服制剂的绝对生物利用度根据血清曲线下面积计算得出。对于茶碱,糖衣丸剂的生物利用度为100%,滴剂为78%。乙羟茶碱的生物利用度也很高:糖衣丸剂为94%,滴剂为84%。从动力学数据可以得出结论,如果按照规定的用法用量服用科达林,茶碱和乙羟茶碱的蓄积可以忽略不计。

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