苯基布他松制剂在马体内的肌肉注射生物利用度。

The intramuscular bioavailability of a phenylbutazone preparation in the horse.

作者信息

Landuyt J, Delbeke F T, Debackere M

机构信息

Laboratory of Veterinary Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Ghent, Belgium.

出版信息

J Vet Pharmacol Ther. 1993 Dec;16(4):494-500. doi: 10.1111/j.1365-2885.1993.tb00216.x.

DOI:10.1111/j.1365-2885.1993.tb00216.x

PMID:8126767

Abstract

The plasma concentrations of phenylbutazone (PBZ) and its major metabolites, oxyphenbutazone (OPBZ) and gamma-OH-phenylbutazone (OHPBZ) were determined for up to 72 h in six horses, following intravenous (i.v.) and intramuscular (i.m.) administration of 4 g phenylbutazone, 20 ml Phenylarthrite Ventoquinol (Vetoquinol Spécialités Pharmaceutiques Vétérinaires, Magny-Vernois, 70200 Lure, France). After i.v. dosing the plasma disposition was best described by a two-compartment open model. The hydroxylated metabolites OPBZ and OHPBZ were present in detectable concentrations for 72 h and 48 h, respectively. After 36 h the OPBZ concentrations exceeded plasma PBZ concentrations. The plasma disposition following i.m. injection could be described by a one-compartment open model. The hydroxylated metabolites OPBZ and OHPBZ were present in detectable concentrations for 72 h and 36 h, respectively. Only after 72 h was the concentration of OPBZ in plasma higher than the concentration of PBZ. The mean i.m. bioavailability of phenylbutazone was calculated to be 91.7 +/- 10.1%.

摘要

在六匹马静脉注射（i.v.）和肌肉注射（i.m.）4克保泰松、20毫升Phenylarthrite Ventoquinol（法国Vetoquinol Spécialités Pharmaceutiques Vétérinaires公司，马格尼 - 韦尔努瓦，70200吕尔）后，测定了长达72小时的保泰松（PBZ）及其主要代谢物羟基保泰松（OPBZ）和γ-OH-保泰松（OHPBZ）的血浆浓度。静脉给药后，血浆处置情况最好用二室开放模型描述。羟基化代谢物OPBZ和OHPBZ分别在72小时和48小时内以可检测浓度存在。36小时后，OPBZ浓度超过血浆PBZ浓度。肌肉注射后的血浆处置情况可用一室开放模型描述。羟基化代谢物OPBZ和OHPBZ分别在72小时和36小时内以可检测浓度存在。仅在72小时后，血浆中OPBZ的浓度才高于PBZ的浓度。保泰松的平均肌肉注射生物利用度经计算为91.7±10.1%。