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依托度酸直肠给药后的药代动力学研究;“体外”释放动力学

Pharmacokinetic study of etodolac after rectal administration; "in vitro" release kinetics.

作者信息

Cadorniga R, Herrero R, Barcia E, Molina I T, Guitierrez J A, Fabregas J L, Martinez-Tobed A

机构信息

Department of Pharmacy, Faculty of Pharmacy, University of Madrid, Spain.

出版信息

Eur J Drug Metab Pharmacokinet. 1991;Spec No 3:389-96.

PMID:1840326
Abstract

The present study describes the pharmacokinetic behaviour of a new dosage form of etodolac not available in the Spanish market: suppositories. Rectal administration was chosen as an alternative for the oral route. The dose used was 200 mg. The pharmacokinetic parameters of the drug are estimated by means of two possible methods i.e., model-independent and model-dependent. The results obtained are compared and discussed. At the same time, an "in vitro" study of the release kinetics of etodolac from the suppository was performed using a continuous flow system without fluid recirculation or accumulating reservoir. The dissolution media used were buffered aqueous solutions at pH 6.5 and 7.4. The results obtained show that the release of the drug from the supposity could be a limiting factor for its absorption.

摘要

本研究描述了一种西班牙市场上没有的依托度酸新剂型(栓剂)的药代动力学行为。选择直肠给药作为口服途径的替代方法。使用的剂量为200毫克。通过两种可能的方法,即非模型依赖法和模型依赖法来估计药物的药代动力学参数。对所得结果进行了比较和讨论。同时,使用无流体再循环或累积储库的连续流动系统对依托度酸从栓剂中的释放动力学进行了“体外”研究。使用的溶出介质是pH值为6.5和7.4的缓冲水溶液。所得结果表明,药物从栓剂中的释放可能是其吸收的一个限制因素。

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