妥曲珠利在不同介质中的溶解度及其表观油水分配系数的测定  

Determination of Solubility in Different Media and Apparent Octanol-water Partition Coefficient of Toltrazuril

作　　者：蒋公建 周建瑜[3] 骆世军 雷元军 范建彪 魏世军 符华林[3] JIANG Gong-jian;ZHOU Jian-yu;LUO Shi-jun;LEI Yuan-jun;FAN Jian-biao;WEI Shi-jun;FU Hua-lin(Animal Husbandry Bureau of Wanzhou District,Wanzhou 404100,Chongqing,China;Pioneers Animals Pharmaceutical Co. Ltd. of Chongqing,Wanzhou 404100,Chongqing,China;Innovative Engineering Research Center of Veterinary Pharmaceutics,College of Veterinary Medicine,Sichuan Agricultural University,Chengdu 611130,China;Animal Husbandry and Veterinary Bureau of Kaizhou District,Kaizhou 405400,Chongqing,China)

机构地区：[1]重庆市万州区畜牧站,重庆万州404100 [2]重庆先锋动物药业有限公司,重庆万州404100 [3]四川农业大学动物医学院兽药创新制剂工程技术研究中心,成都611130 [4]重庆市开州区畜牧兽医局,重庆开州405400

出　　处：《四川农业大学学报》2017年第1期106-109,共4页Journal of Sichuan Agricultural University

基　　金：四川省三区人才支持计划(044z0106)

摘　　要：【目的】测定妥曲珠利的平衡溶解度和表观油水分配系数,为其体内吸收和剂型设计提供依据。【方法】采用平衡法测定妥曲珠利在水和有机溶剂中的溶解度,同时测定其在正辛醇-缓冲液中的表观油水分配系数。【结果】妥曲珠利在有机溶剂中的溶解度顺序为:丙酮>冰醋酸>乙醇>正丁醇>石油醚>环己烷,其在水中溶解度随pH增加逐渐增大,其表观油水分配系数受到pH的影响较大,在pH 5.8处表观油水分配系数最大,为118.49。【结论】妥曲珠利水溶性较差,其溶解度和表观油水分配系数受到pH的影响较大。【Objective】To determine the equilibrium solubility and apparent oil-water partitioncoefficient of toltrazuril,and provide basic data for it’s absorption in vivo and new formulationsdesign.【Methods】Equilibrium method was adopted to determine the solubility of toltrazuril in differentaqueous solution and organic solvents,and the apparent octanol-water partition coefficient oftoltrazuril in oil-buffer solution system was also explored.【Results】The order of the solubility oftoltrazuril in organic solvents was as follows:acetone>acetic acid>ethanol>n-butanol>petroleum ether>cyclohexane,and solubility in alkaline buffer was relatively higher;pH values had a great effect onthe apparent oil-water partition coefficient of toltrazuril,and the maximum coefficient existed in pH5.8buffer solution was118.49.【Conclusion】Toltrazuril had poor water solubility,and its apparented solubility in water and octanol-water partition coefficient were significantly affect by pH.

关 键 词：妥曲珠利 溶解度 表观分配系数 

分 类 号：R978.69[医药卫生—药品]