Franquelo C, Toledo A, Manubens J, Cristòfol C, Valladares J E, Arboix M
Divisiò de Farmacologia, Facultat de Veterinària, UAB, Bellaterra, Spain.
Vet Rec. 2000 Oct 21;147(17):477-80. doi: 10.1136/vr.147.17.477.
An aqueous solution and a lipid emulsion of bupivacaine were administered epidurally in doses of 1.8 mg/kg to six beagle dogs following a randomised two-phase crossover design. The aqueous solution was absorbed rapidly and the mean (sd) peak venous plasma concentration of bupivacaine, 1.4 (0.4) microg/ml, was detected after five minutes. After administration of the lipid emulsion, the peak plasma concentration of bupivacaine, 0.6 (0.2) microg/ml, was detected after 30 minutes. The mean (sd) t1/2beta of the aqueous preparation was 149.1 (32.6) minutes, and of the lipid emulsion 119.2 (34.0) minutes. Both preparations had a similar bioavailability. The mean time to the onset of motor block after the administration of the aqueous solution, 2.3 (2.2) minutes, was significantly shorter (P=0.028) than after the administration of the lipid emulsion, 9.4 (1.9) minutes, and the duration of the motor block induced by the lipid emulsion, 217.6 (26.2) minutes, was significantly longer (P=0.043) than for the aqueous solution, 158 (48.8) minutes. During anaesthesia, the plasma concentrations of bupivacaine ranged between 1.3 and 0.2 microg/ml. Non-significant changes in systolic blood pressure and heart rate were observed which coincided with the peak plasma concentrations of bupivacaine.
按照随机双阶段交叉设计,对6只比格犬硬膜外给予布比卡因水溶液和脂质乳剂,剂量均为1.8mg/kg。布比卡因水溶液吸收迅速,给药5分钟后检测到布比卡因的平均(标准差)静脉血浆峰浓度为1.4(0.4)μg/ml。给予脂质乳剂后,30分钟时检测到布比卡因的血浆峰浓度为0.6(0.2)μg/ml。水溶液制剂的平均(标准差)β半衰期为149.1(32.6)分钟,脂质乳剂为119.2(34.0)分钟。两种制剂的生物利用度相似。给予水溶液后运动阻滞开始的平均时间为2.3(2.2)分钟,显著短于给予脂质乳剂后的9.4(1.9)分钟(P=0.028);脂质乳剂诱导的运动阻滞持续时间为217.6(26.2)分钟,显著长于水溶液的158(48.8)分钟(P=0.043)。麻醉期间,布比卡因的血浆浓度在1.3至0.2μg/ml之间。观察到收缩压和心率无显著变化,且与布比卡因的血浆峰浓度一致。