Davis J L, Messenger K M, LaFevers D H, Barlow B M, Posner L P
Department of Clinical Sciences, North Carolina State University, College of Veterinary Medicine, Raleigh, NC 27606, USA.
J Vet Pharmacol Ther. 2012 Feb;35(1):52-8. doi: 10.1111/j.1365-2885.2011.01284.x. Epub 2011 Mar 11.
The purpose of this study was to determine the pharmacokinetics of buprenorphine following intravenous (i.v.) and intramuscular (i.m.) administration in horses. Six horses received i.v. or i.m. buprenorphine (0.005 mg/kg) in a randomized, crossover design. Plasma samples were collected at predetermined times and horses were monitored for adverse reactions. Buprenorphine concentrations were measured using ultra-performance liquid chromatography with electrospray ionization mass spectrometry. Following i.v. administration, clearance was 7.97±5.16 mL/kg/min, and half-life (T(1/2)) was 3.58 h (harmonic mean). Volume of distribution was 3.01±1.69 L/kg. Following i.m. administration, maximum concentration (C(max)) was 1.74±0.09 ng/mL, which was significantly lower than the highest measured concentration (4.34±1.22 ng/mL) after i.v. administration (P<0.001). Time to C(max) was 0.9±0.69 h and T(1/2) was 4.24 h. Bioavailability was variable (51-88%). Several horses showed signs of excitement. Gut sounds were decreased 10±2.19 and 8.67±1.63 h in the i.v. and i.m. group, respectively. Buprenorphine has a moderate T(1/2) in the horse and was detected at concentrations expected to be therapeutic in other species after i.v. and i.m. administration of 0.005 mg/kg. Signs of excitement and gastrointestinal stasis may be noted.
本研究的目的是确定丁丙诺啡在马静脉注射（i.v.）和肌肉注射（i.m.）后的药代动力学。六匹马采用随机交叉设计接受静脉注射或肌肉注射丁丙诺啡（0.005mg/kg）。在预定时间采集血浆样本，并监测马匹的不良反应。使用超高效液相色谱-电喷雾电离质谱法测定丁丙诺啡浓度。静脉注射后，清除率为7.97±5.16mL/kg/min，半衰期（T(1/2)）为3.58小时（调和均值）。分布容积为3.01±1.69L/kg。肌肉注射后，最大浓度（C(max)）为1.74±0.09ng/mL，显著低于静脉注射后测得的最高浓度（4.34±1.22ng/mL）（P<0.001）。达到C(max)的时间为0.9±0.69小时，T(1/2)为4.24小时。生物利用度可变（51-88%）。几匹马出现兴奋迹象。静脉注射组和肌肉注射组的肠鸣音分别在10±2.19小时和8.67±1.63小时减弱。丁丙诺啡在马体内具有中等半衰期，在静脉注射和肌肉注射0.005mg/kg后，其浓度在其他物种中预期具有治疗作用。可能会注意到兴奋和胃肠停滞的迹象。
