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时间依赖性动力学I:卡马西平在猴子体内的指数自诱导

Time-dependent kinetics I: Exponential autoinduction of carbamazepine in monkeys.

作者信息

Pitlick W H, Levy R H

出版信息

J Pharm Sci. 1977 May;66(5):647-9. doi: 10.1002/jps.2600660511.

Abstract

The pharmacokinetics of carbamazepine were studied during a week-long infusion of the drug in 60% polyethylene glycol 400 solution in three rhesus monkeys. Serum concentrations approached steady state within 8-16 hr and then rapidly declined, within 72 hr, to a new asymptotic level approximately 46% of the maximum steady-state concentration. Serum concentrations remained at that level during the rest of the experimental period. The decline from the maximum value to the asymptotic steady state was exponential. It is postulated that the decline in the steady-state concentration is due to autoinduction by carbamazepine of its own metabolism.

摘要

在三只恒河猴中,研究了卡马西平在60%聚乙二醇400溶液中为期一周的输注过程中的药代动力学。血清浓度在8 - 16小时内接近稳态,然后在72小时内迅速下降至新的渐近水平,约为最大稳态浓度的46%。在实验期的其余时间内,血清浓度保持在该水平。从最大值下降到渐近稳态呈指数下降。据推测,稳态浓度的下降是由于卡马西平自身代谢的自诱导作用。

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