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替马西泮在人和几种动物物种中的药代动力学及代谢情况。

Pharmacokinetics and metabolism of temazepam in man and several animal species.

作者信息

Schwarz H J

出版信息

Br J Clin Pharmacol. 1979;8(1):23S-29S. doi: 10.1111/j.1365-2125.1979.tb00451.x.

Abstract

1 Absorption, excretion and detoxification of temazepam were investigated in man, mouse, rat and dog. Considerable interspecies variation was apparent with respect to excretion and metabolite patterns in blood and urine. Animal species were exposed to equal or greater concentrations of all the metabolites occurring in man. 2 Pharmacokinetics of temazepam in man were investigated in a single dose study at two dose levels, and in a multiple dose study. The results of both studies were analyzed and interpreted with the help of compartmental models. Values were obtained for excretion pattern (0-infinity), half lives (1.95, 0.5, 10.0 and 1.9 h), amounts in all compartments, and for steady-state conditions. 3 The bioavailability of the hard gelatin capsule dosage form was compared with that of a suspension serving as the ideal dosage form, and found to be acceptable.

摘要
  1. 对替马西泮在人、小鼠、大鼠和犬体内的吸收、排泄及解毒情况进行了研究。在血液和尿液的排泄及代谢物模式方面,明显存在种间差异。动物物种接触到的所有代谢物浓度与人相同或更高。2. 在单剂量研究中的两个剂量水平以及多剂量研究中,对替马西泮在人体内的药代动力学进行了研究。两项研究的结果均借助房室模型进行了分析和解释。获得了排泄模式(0至无穷大)、半衰期(1.95、0.5、10.0和1.9小时)、所有房室中的含量以及稳态条件下的值。3. 将硬明胶胶囊剂型的生物利用度与作为理想剂型的混悬液进行了比较,结果发现该剂型是可接受的。

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