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人用药物制剂在马体内的处置。I. 直肠给药的吲哚美辛。

Disposition of human drug preparations in the horse. I. Rectally administered indomethacin.

作者信息

Delbeke F T, Debackere M, Vynckier L

机构信息

Labo voor Farmacologie en Toxicologie, Faculteit Diergeneeskunde, Rijksuniversiteit Gent, Belgium.

出版信息

J Vet Pharmacol Ther. 1991 Jun;14(2):145-9. doi: 10.1111/j.1365-2885.1991.tb00816.x.

Abstract

A high-performance liquid chromatographic method to measure urinary indomethacin levels is described. In 0.5 ml urine, 1 micrograms/ml of indomethacin could be detected. Alkaline hydrolysis of urine resulted in the decomposition of indomethacin. When two suppositories of Indocid corresponding to 200 mg indomethacin were administered rectally to four horses the drug was rapidly absorbed and remained detectable in urine from 1 to 12 h. The excretion rate peaked after 2-3 h while the maximal concentration ranged from 18.5 to 80.6 micrograms/ml. Only 8 to 16% of the indomethacin dose was eliminated in urine after 12 h. A fraction of the dose was excreted as the glucuronide conjugate.

摘要

描述了一种用于测量尿中吲哚美辛水平的高效液相色谱法。在0.5毫升尿液中,可检测到1微克/毫升的吲哚美辛。尿液的碱性水解导致吲哚美辛分解。当给四匹马直肠给药相当于200毫克吲哚美辛的两枚消炎痛栓时,药物迅速吸收,在1至12小时的尿液中仍可检测到。排泄率在2 - 3小时后达到峰值,而最大浓度范围为18.5至80.6微克/毫升。12小时后,仅8%至16%的吲哚美辛剂量经尿液排出。一部分剂量以葡萄糖醛酸结合物的形式排泄。

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