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目的:研究斑蝥素的理化性质,为其动力学性质及新剂型设计提供依据。方法:采用高效液相色谱法(HPLC)测定不同溶剂中斑蝥素的平衡溶解度;采用摇瓶法测定正辛醇-水及缓冲液体系中的油水分配系数;以及测定斑蝥素在酸、碱、氧化性和还原性溶液中的稳定性等。结果:斑蝥素在25℃下水中的平衡溶解度为40.5μg·m L~(-1),在乙腈中溶解度最大(36 927.6μg·m L~(-1)),在缓冲液中溶解度较小,且加入多数表面活性剂后能增加斑蝥素的溶解度,以氢化大豆卵磷脂增溶能力最强;斑蝥素的表观油水分配系数为2.541 2(lg P=0.405 0);斑蝥素在酸、碱、氧化性和还原性溶液中均不稳定。结论:本文建立的测定方法简单可行。斑蝥素几乎不溶于水,且p H值影响平衡溶解度和表观油水分配系数。斑蝥素属于低溶解度、低渗透性和低生物利用度药物。
Objective: To study the physicochemical properties of cantharidin, and provide the basis for its kinetic properties and new formulation design. Methods: The equilibrium solubility of cantharidin in different solvents was determined by high performance liquid chromatography (HPLC). The oil-water partition coefficient in n-octanol-water and buffer system was determined by shake flask method. Oxidative and reducing solution stability and so on. Results: The equilibrium solubility of cantharidin in water was 40.5μg · m L -1 at 25 ℃ and 36 927.6μg · m L -1 in acetonitrile. The solubility of cantharidin in buffer was low , And the addition of most surfactants can increase the solubility of cantharidin to hydrogenate soy lecithin strongest solubilization; cantharidin apparent oil and water partition coefficient of 2.541 2 (lg P = 0.405 0); cantharidin in acid, Base, oxidizing and reducing solution are not stable. Conclusion: The method established in this paper is simple and feasible. Cantharidin is hardly soluble in water, and the p H value affects equilibrium solubility and apparent oil-water partition coefficient. Cantharidin is a drug of low solubility, low permeability and low bioavailability.