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目的:测定田蓟苷在不同缓冲溶液和表面活性剂溶液中的平衡溶解度及在正辛醇-水/磷酸缓冲盐中表观油水分配系数(Papp),为今后新剂型的选择和制备提供参考。方法:通过高效液相色谱法测定田蓟苷在不同溶剂和表面活性剂溶液中的浓度,采用摇瓶法测定田蓟苷在正辛醇-水/磷酸缓冲盐中油水分配系数。结果:田蓟苷在37℃纯水中的平衡溶解度为1.57mg·L~(-1),在甲醇、乙酸乙酯及三氯甲烷有机溶液中溶解性较好;在酸性缓冲溶液中的平衡溶解度较水中有明显增加,在碱性缓冲液中随pH的增高平衡溶解度逐渐减小。在32 g·L~(-1)的十二烷基硫酸钠溶液中平衡溶解度提高到188.65 mg·L~(-1)。田蓟苷的油水分配系数为14.63(lg P=1.17),且随溶液pH的增高逐渐增加。结论:田蓟苷为疏水性药物,脂溶性较强。制剂时,可加入适当浓度的十二烷基硫酸钠助溶。同时,提高其制剂的溶出度可能会提高其生物利用度。
OBJECTIVE: To determine the equilibrium solubility of silymarin in different buffer solutions and surfactant solutions and the apparent oil-water partition coefficient (Papp) in n-octanol-water / phosphate buffered saline, to provide reference for the future selection and preparation of new dosage forms . Methods: The concentration of thymidine in different solvents and surfactant solutions was determined by high performance liquid chromatography (HPLC). The partition coefficient of thymidine in n-octanol-water / phosphate buffer was determined by shake flask method. Results: The equilibrium solubility of thymidine in pure water at 37 ℃ was 1.57 mg · L -1, and its solubility in organic solvents such as methanol, ethyl acetate and trichloromethane was better. The balance of thymidine in acidic buffer solution Solubility than in water significantly increased in alkaline buffer pH equilibrium solubility gradually decreases. The equilibrium solubility increased to 188.65 mg · L -1 in 32 g · L -1 sodium dodecyl sulfate solution. The thymidine oil-water partition coefficient was 14.63 (lg P = 1.17), and gradually increased with increasing pH of the solution. Conclusion: Silymarin is a hydrophobic drug with strong liposolubility. Preparation, can be added to the appropriate concentration of sodium lauryl sulfate to dissolve. At the same time, increasing the dissolution rate of their formulations may increase their bioavailability.