de Sousa A B, Santos A C D, Schramm S G, Porta V, Górniak S L, Florio J C, de Souza Spinosa H
Departamento de Patologia, Faculdade de Medicina Veterinária e Zootecnia da Universidade de São Paulo, São Paulo, Brazil.
J Vet Pharmacol Ther. 2008 Feb;31(1):45-51. doi: 10.1111/j.1365-2885.2007.00916.x.
The aim of this trial was to implement a method to obtain a tool for analyses of tramadol and the main metabolite, o-desmethyltramadol (M1), in goat's plasma, and to evaluate the pharmacokinetics of these substances following intravenous (i.v.) and oral (p.o.) administration in female goats. The pharmacokinetics of tramadol and M1 were examined following i.v. or p.o. tramadol administration to six female goats (2 mg/kg). Average retention time was 5.13 min for tramadol and 2.42 min for M1. The calculated parameters for half-life, volume of distribution and total body clearance were 0.94+/-0.34 h, 2.48+/-0.58 L/kg and 2.18+/-0.23 L/kg/h following 2 mg/kg tramadol HCl administered intravenously. The systemic availability was 36.9+/-9.1% and half-life 2.67+/-0.54 h following tramadol 2 mg/kg p.o. M1 had a half-life of 2.89+/-0.43 h following i.v. administration of tramadol. Following p.o., M1 was not detectable.
本试验的目的是实施一种方法，以获得一种用于分析山羊血浆中曲马多及其主要代谢物O-去甲基曲马多（M1）的工具，并评估这些物质在雌性山羊静脉注射（i.v.）和口服（p.o.）给药后的药代动力学。对六只雌性山羊（2mg/kg）静脉注射或口服曲马多后，检测了曲马多和M1的药代动力学。曲马多的平均保留时间为5.13分钟，M1为2.42分钟。静脉注射2mg/kg盐酸曲马多后，计算得出的半衰期、分布容积和全身清除率参数分别为0.94±0.34小时、2.48±0.58L/kg和2.18±0.23L/kg/h。口服2mg/kg曲马多后，系统利用率为36.9±9.1%，半衰期为2.67±0.54小时。静脉注射曲马多后，M1的半衰期为2.89±0.43小时。口服后，未检测到M1。
