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速可巴比妥在兔体内的药代动力学

Pharmacokinetics of secobarbital in rabbit.

作者信息

Somani S M, McDonald R H, Schumacher D P

出版信息

Arch Int Pharmacodyn Ther. 1975 Jun;215(2):301-17.

PMID:1164094
Abstract

The pharmacokinetic study of secobarbital in the rabbit utilizing gas chromatography (GC) indicated a correlation between blood levels and brain tissue levels; and that the distribution of the drug appears to be more complex than a first order process is suggested by the compartmental simulation midel. The liver and kidney which eliminate the drug into bile and urine, respectively, tend to follow first order elimination kinetics more closely than those which act as depots for drug storage such as muscle and fat. The two dose levels of secobarbital indicate the same relationship with blood and tissues, therefore an increase or decrease in the dosage has no effect on the pharmacokinetics of secobarbital. The termination of action of secobarbital is due to the combination of rapid uptake by liver and its disposition there and a slower uptake by muscle. Computer simulation of secobarbital distribution has strongly suggested the elimination of this drug in bile and that the rebound rise in liver amy be due to enterohepatic circulation.

摘要

利用气相色谱法(GC)对家兔进行的司可巴比妥药代动力学研究表明,血药浓度与脑组织浓度之间存在相关性;房室模拟模型表明,该药的分布似乎比一级过程更为复杂。分别将药物排泄到胆汁和尿液中的肝脏和肾脏,比肌肉和脂肪等作为药物储存库的器官更倾向于遵循一级消除动力学。司可巴比妥的两个剂量水平与血液和组织的关系相同,因此剂量的增加或减少对司可巴比妥的药代动力学没有影响。司可巴比妥作用的终止是由于肝脏对其快速摄取并在肝脏中进行处置,以及肌肉摄取较慢共同作用的结果。司可巴比妥分布的计算机模拟有力地表明该药可经胆汁排泄,肝脏中药物浓度的反弹升高可能是由于肠肝循环所致。

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