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美哌隆在人体中的肠胃外给药和口服给药的药代动力学

Pharmacokinetics of parenteral and oral melperone in man.

作者信息

Borgström L, Larsson H, Molander L

出版信息

Eur J Clin Pharmacol. 1982;23(2):173-6. doi: 10.1007/BF00545974.

Abstract

The pharmacokinetics of melperone (Buronil, Ferrosan, Sweden) was studied after administration of various parenteral and oral doses to man. After parenteral administration, the data could be fitted to a two-compartment model, but after oral dosing the distribution phase could not be separated from the elimination phase, and so an one-compartment model gave the best fit. The half-lives were about 3-4 h, except after intramuscular injection, when the half-life was about 6 h. The bioavailability of oral doses was about 60% of the intravenous injection. After the highest oral dose of 100 mg, the pharmacokinetics, expressed as AUC or Cmax, showed non-linearity, possibly due to saturation of the hepatic elimination system.

摘要

在给人体注射不同剂量的胃肠外给药和口服给药后,研究了美哌隆(Buronil,Ferrosan,瑞典)的药代动力学。胃肠外给药后,数据可拟合为二室模型,但口服给药后,分布相无法与消除相分离,因此单室模型拟合效果最佳。半衰期约为3 - 4小时,但肌肉注射后半衰期约为6小时。口服剂量的生物利用度约为静脉注射的60%。口服最高剂量100毫克后,以AUC或Cmax表示的药代动力学显示出非线性,这可能是由于肝脏消除系统饱和所致。

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