King J N, Mauron C, Voirol M J, Le Goff C, Hauffe S A
CIBA-GEIGY Animal Health, Centre de Recherches Agricoles, St. Aubin, Switzerland.
J Vet Pharmacol Ther. 1994 Jun;17(3):186-92. doi: 10.1111/j.1365-2885.1994.tb00232.x.
A high-performance liquid chromatographic method for the determination of the non-steroidal anti-inflammatory drug, oxindanac, in calf plasma is described. Recoveries over the concentration range 0.375 to 62.5 micrograms/ml were 90.2-107.8% with interassay coefficients of variation of 2.1-22.3%. The limit of detection was estimated as 0.10 micrograms/ml and the limit of quantification calculated to be 0.24 micrograms/ml in a 1 ml plasma sample. This method was used to establish the pharmacokinetics following intravenous (i.v.), intramuscular (i.m.) and oral (p.o.) administration to calves of oxindanac at a dose rate of 2 mg/kg. The elimination t1/2 was long (t1/2 21.2 h after i.v. injection) and absorption was rapid (t1/2a 0.072 h) and complete (F > 100%) following i.m. administration. Bioavailability was incomplete (F = 66.6%) following p.o. administration to calves that had been fed on milk, and Wagner-Nelson analysis revealed two absorption phases (t1/2's 0.20 and 1.9 h). Oxindanac produced long-lasting inhibition of serum TxB2 production, with mean Emax values (% inhibition) of 96.8, 94.1 and 81.3 following i.v., i.m. and p.o. administration, respectively. A single i.v. or i.m. injection of 2 mg/kg oxindanac will probably be active in calves for at least 36-48 h.
本文描述了一种用于测定犊牛血浆中非甾体抗炎药奥辛丹酸的高效液相色谱法。在0.375至62.5微克/毫升的浓度范围内,回收率为90.2 - 107.8%,批间变异系数为2.1 - 22.3%。在1毫升血浆样品中,检测限估计为0.10微克/毫升,定量限计算为0.24微克/毫升。该方法用于建立以2毫克/千克的剂量率对犊牛静脉内(i.v.)、肌肉内(i.m.)和口服(p.o.)给予奥辛丹酸后的药代动力学。消除半衰期较长(静脉注射后t1/2为21.2小时),肌肉注射后吸收迅速(t1/2a为0.072小时)且完全(F>100%)。对以牛奶为食的犊牛口服给药后,生物利用度不完全(F = 66.6%),Wagner-Nelson分析显示有两个吸收阶段(t1/2分别为0.20和1.9小时)。奥辛丹酸对血清TxB2的产生具有持久的抑制作用,静脉内、肌肉内和口服给药后的平均Emax值(抑制率%)分别为96.8、94.1和81.3。单次静脉注射或肌肉注射2毫克/千克的奥辛丹酸在犊牛体内可能至少36 - 48小时内有效。