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大鼠去甲烯酰亚胺的药代动力学评价

Pharmacokinetic evaluation of norendimide in rats.

作者信息

Koch H P, Pischek G, Czejka M, Ritschel W A

出版信息

Methods Find Exp Clin Pharmacol. 1982;4(8):581-5.

PMID:7169846
Abstract

Norendimide, the endo-isomer of the new psychoactive compound noreximide, was studied in rats upon I.V., P.O., and I.P. administration, and the pharmacokinetic parameters were determined from the concentration-time data. The one-compartment model was most appropriate for curve-fitting of all data. The elimination half-life is approximately 11 hours, and hence about 30% longer than that of the parent compound. The volume of distribution is about 85% of the body weight. Upon P.O. and I.P. administration the fraction of drug absorbed is 80% and 94%, respectively. A comparison with the previously reported pharmacokinetic data on noreximide indicates that both compounds, the parent drug and the analog, are completely absorbed and show some first-pass effect.

摘要

诺伦地米德是新型精神活性化合物诺雷西米德的内消旋异构体,通过静脉注射、口服和腹腔注射给药对大鼠进行了研究,并根据浓度-时间数据确定了药代动力学参数。单室模型最适合所有数据的曲线拟合。消除半衰期约为11小时,因此比母体化合物长约30%。分布容积约为体重的85%。口服和腹腔注射给药时,药物吸收分数分别为80%和94%。与先前报道的诺雷西米德药代动力学数据比较表明,母体药物及其类似物这两种化合物均被完全吸收并显示出一定的首过效应。

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