Valladares J E, Alberola J, Esteban M, Arboix M
Divisió de Farmacologia, Facultat de Veterinària, Universitat Autònoma de Barcelona, Bellaterra, Spain.
Vet Rec. 1996 Feb 24;138(8):181-3. doi: 10.1136/vr.138.8.181.
A study was carried out in dogs to define the pharmacokinetic profile of antimony and to define a better therapeutic protocol for the treatment of canine leishmaniasis. Six healthy beagle dogs received 100 mg/kg of N-methylglucamine antimoniate containing 27.2 per cent of antimony intravenously, intramuscularly and subcutaneously. After intravenous administration the plasma concentration of antimony decreased rapidly and after 240 minutes it was lower than the ED50 values suggested for Leishmania donovani. The pharmacokinetic parameters and bioavailability of antimony were calculated after each route of administration in each dog. The curves of plasma concentrations vs time were best described by a triexponential open model with a mean (sd) half life t1/2 alpha of 9.4 (4.4) min, a t1/2 beta of 45.3 (4.5) min and a t1/2 gamma of 618.0 (93.5) min. The mean volume of distribution at steady state was 0.25 (0.03) litres/kg and the total body clearance was 0.25 (0.04) litres/h/kg. The peak plasma concentration (Cmax) after intramuscular administration was 27.2 (3.1) micrograms/ml, and after subcutaneous administration it was 25.5 (4.5) micrograms/ml; they were reached after 73.6 (11.9) min and 85.6 (11.3) min, respectively. The bioavailabilities after intramuscular and subcutaneous administration were 91.7 (7.1) and 92.2 (7.1) per cent, respectively. More than 80 per cent of the antimony was excreted in the urine in the first nine hours.
在犬类中进行了一项研究，以确定锑的药代动力学特征，并确定治疗犬利什曼病的更好治疗方案。六只健康的比格犬分别通过静脉、肌肉和皮下注射接受了每千克体重100毫克含27.2%锑的葡甲胺锑酸盐。静脉给药后，锑的血浆浓度迅速下降，240分钟后低于杜氏利什曼原虫建议的半数有效剂量（ED50）值。在每只犬的每种给药途径后计算锑的药代动力学参数和生物利用度。血浆浓度与时间曲线最好用三指数开放模型描述，平均（标准差）半衰期t1/2α为9.4（4.4）分钟，t1/2β为45.3（4.5）分钟，t1/2γ为618.0（93.5）分钟。稳态时的平均分布容积为0.25（0.03）升/千克，全身清除率为0.25（0.04）升/小时/千克。肌肉注射后的血浆峰浓度（Cmax）为27.2（3.1）微克/毫升，皮下注射后为25.5（4.5）微克/毫升；分别在73.6（11.9）分钟和85.6（11.3）分钟达到。肌肉注射和皮下注射后的生物利用度分别为91.7（7.1）%和92.2（7.1）%。超过80%的锑在前九个小时内通过尿液排出。
