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正常受试者中青霉胺的动力学。

Penicillamine kinetics in normal subjects.

作者信息

Bergstrom R F, Kay D R, Harkcom T M, Wagner J G

出版信息

Clin Pharmacol Ther. 1981 Sep;30(3):404-13. doi: 10.1038/clpt.1981.180.

Abstract

The kinetic characteristics of penicillamine are reported in four fasting subjects after four oral doses each. On late test days, tow of the subjects received an additional single dose 30 min after a large breakfast. On subject originally included in the study had to drop out because of gastrointestinal disturbances following each of two single doses of penicillamine. The fasting plasma levels of penicillamine observed in this study displayed an unusual double peak in the plasma levels after single doses. Individual subjects had consistent plasma level patterns for each of the four single doses but there was marked intersubject variability in patterns and kinetic parameters. The half-life of unchanged penicillamine ranged from 1.66 to 3.15 hr and the apparent plasma clearance ranged from 530 to 2300 ml/min. The administration of penicillamine following a large breakfast caused a reduction in the area under the penicillamine plasma concentration-time curve corresponding to a decrease in the extent of absorption of unchanged penicillamine.

摘要

对四名受试者在禁食状态下各口服四剂青霉胺后的动力学特征进行了报告。在试验后期,其中两名受试者在丰盛早餐后30分钟额外服用了一剂青霉胺。该研究最初纳入的一名受试者因服用两剂单剂量青霉胺后均出现胃肠道不适而退出。本研究中观察到的青霉胺空腹血浆水平在单剂量给药后呈现出异常的双峰。四名受试者各自的单剂量血浆水平模式具有一致性,但受试者之间的模式和动力学参数存在显著差异。未变化的青霉胺半衰期为1.66至3.15小时,表观血浆清除率为530至2300毫升/分钟。丰盛早餐后服用青霉胺导致青霉胺血浆浓度-时间曲线下面积减小,这与未变化的青霉胺吸收程度降低相对应。

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