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戊四氮在犬体内的药代动力学研究。

Pharmacokinetic studies of pentylenetetrazol in dogs.

作者信息

Jun H W

出版信息

J Pharm Sci. 1976 Jul;65(7):1038-41. doi: 10.1002/jps.2600650720.

Abstract

Pharmacokinetic profiles of pentylenetetrazol in the dog were studied following rapid intravenous and oral administrations of a convulsant dose (15-20 mg/kg). Plasma level-time curves after a rapid intravenous injection showed biexponential decline, indicating that the disposition of this drug in the dog follows a two-compartment body model. Pharmacokinetic parameters were calculated from the intravenous data. After oral administration of the solution dose, the peak plasma level appeared at about 30 min postdose, indicating that the absorption occurs rapidly. Areas under the oral plasma level-time curves s howed that the drug was absorbed completely and that the first-pass metabolism effect was minimal. The ligation studies of the kidney and the liver suggested that the main elimination pathway of this drug was biotransformation in the liver. The average plasma half-life was 1.4 hr. At steady state, the volume of distribution was approximately equivalent to the volume of the total body water.

摘要

在犬类中,以惊厥剂量(15 - 20毫克/千克)快速静脉注射和口服戊四氮后,研究了其药代动力学特征。快速静脉注射后的血浆浓度-时间曲线呈双指数下降,表明该药物在犬体内的处置遵循二室模型。药代动力学参数根据静脉注射数据计算得出。口服溶液剂量后,血浆浓度峰值出现在给药后约30分钟,表明吸收迅速。口服血浆浓度-时间曲线下面积显示药物被完全吸收,且首过代谢效应最小。肾脏和肝脏的结扎研究表明,该药物的主要消除途径是肝脏中的生物转化。平均血浆半衰期为1.4小时。在稳态时,分布容积大约相当于总体液量。

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