Sinclair Melissa D, Mealey Katrina L, Matthews Nora S, Peck Ken E, Taylor Tex S, Bennett Brad S
Department of Clinical Studies, Ontario Veterinary College, University of Guelph, Guelph, ON, Canada, N1G 2W1.
Am J Vet Res. 2006 Jun;67(6):1082-5. doi: 10.2460/ajvr.67.6.1082.
To determine the disposition of a bolus of meloxicam (administered IV) in horses and donkeys (Equus asinus) and compare the relative pharmacokinetic variables between the species.
5 clinically normal horses and 5 clinically normal donkeys.
Blood samples were collected before and after IV administration of a bolus of meloxicam (0.6 mg/kg). Serum meloxicam concentrations were determined in triplicate via high-performance liquid chromatography. The serum concentration-time curve for each horse and donkey was analyzed separately to estimate standard noncompartmental pharmacokinetic variables.
In horses and donkeys, mean +/- SD area under the curve was 18.8 +/- 7.31 microg/mL/h and 4.6 +/- 2.55 microg/mL/h, respectively; mean residence time (MRT) was 9.6 +/- 9.24 hours and 0.6 +/- 0.36 hours, respectively. Total body clearance (CL(T)) was 34.7 +/- 9.21 mL/kg/h in horses and 187.9 +/- 147.26 mL/kg/h in donkeys. Volume of distribution at steady state (VD(SS)) was 270 +/- 160.5 mL/kg in horses and 93.2 +/- 33.74 mL/kg in donkeys. All values, except VD(SS), were significantly different between donkeys and horses.
The small VD(SS) of meloxicam in horses and donkeys (attributed to high protein binding) was similar to values determined for other nonsteroidal anti-inflammatory drugs. Compared with other species, horses had a much shorter MRT and greater CL(T) for meloxicam, indicating a rapid elimination of the drug from plasma; the even shorter MRT and greater CL(T) of meloxicam in donkeys, compared with horses, may make the use of the drug in this species impractical.
确定静脉注射一剂美洛昔康后在马和驴(Equus asinus)体内的处置情况,并比较这两个物种之间的相对药代动力学变量。
5匹临床正常的马和5头临床正常的驴。
静脉注射一剂美洛昔康(0.6 mg/kg)前后采集血样。通过高效液相色谱法对血清中美洛昔康浓度进行三次测定。分别分析每匹马和每头驴的血清浓度 - 时间曲线,以估算标准的非房室药代动力学变量。
在马和驴中,曲线下面积的平均值±标准差分别为18.8±7.31μg/mL/h和4.6±2.55μg/mL/h;平均驻留时间(MRT)分别为9.6±9.24小时和0.6±0.36小时。马的总体清除率(CL(T))为34.7±9.21 mL/kg/h,驴为187.9±147.26 mL/kg/h。稳态分布容积(VD(SS))在马中为270±160.5 mL/kg,在驴中为93.2±33.74 mL/kg。除VD(SS)外,所有数值在驴和马之间均有显著差异。
美洛昔康在马和驴体内较小的VD(SS)(归因于高蛋白结合)与其他非甾体抗炎药所测定的值相似。与其他物种相比,马对美洛昔康的MRT更短,CL(T)更大,表明药物从血浆中消除迅速;与马相比,美洛昔康在驴体内更短的MRT和更大的CL(T)可能使该药物在该物种中的使用不切实际。