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大鼠体内吲哚美辛的药代动力学与镇痛效果之间的关系

Relationship between pharmacokinetics and the analgesic effect of indomethacin in the rat.

作者信息

Suzuki T, Suganuma T, Shimizu R, Aoki M, Hanano M

机构信息

Department of Pharmaceutical Science, College of Pharmacy, Nihon University, Chiba, Japan.

出版信息

Biol Pharm Bull. 1997 Apr;20(4):438-42. doi: 10.1248/bpb.20.438.

DOI:10.1248/bpb.20.438
PMID:9145226
Abstract

The relationship between the pharmacokinetic properties and the analgesic effect of indomethacin (IDM) was evaluated on a carrageenin-induced inflammation model in the rat. Rats were administered the drug in one of two ways: intravenous (i.v.) IDM bolus or i.v. IDM infusion. The analgesic activity was measured by Randall-Selitto test. No correlation was observed between the analgesic effect and the plasma IDM concentration after i.v. bolus administration of IDM. However, in the case of infusion, IDM produced a dose-dependent analgesic effect. In this paper, we demonstrated that the plasma concentration of IDM maintained by i.v. infusion had a prolonged analgesic effect on the carrageenin-induced inflammation model.

摘要

在大鼠角叉菜胶诱导的炎症模型上评估了吲哚美辛(IDM)的药代动力学性质与镇痛效果之间的关系。大鼠通过以下两种方式之一给药:静脉注射(i.v.)IDM推注或静脉输注IDM。通过Randall-Selitto试验测量镇痛活性。静脉推注IDM后,未观察到镇痛效果与血浆IDM浓度之间存在相关性。然而,在输注的情况下,IDM产生剂量依赖性镇痛作用。在本文中,我们证明了静脉输注维持的IDM血浆浓度对角叉菜胶诱导的炎症模型具有延长的镇痛作用。

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