格列吡嗪油水分配系数和平衡溶解度的测定

Determination of equilibrium solubility and partition coefficient of glipizide

目的测定格列吡嗪的平衡溶解度和油水分配系数,为设计格列吡嗪新剂型提供基础。方法采用HPLC法测定格列吡嗪在水、不同缓冲盐溶液中的质量浓度;采用摇瓶-紫外分光光度法测定格列吡嗪在正辛醇-水、缓冲液体系中的表观油水分配系数。结果37℃下格列吡嗪在水中的平衡溶解度为7.79mg·L-1,随着pH值增大,格列吡嗪的平衡溶解度增大。格列吡嗪在正辛醇-水体系中的油水分配系数lgP=1.63,随着缓冲盐溶液的pH值增大,格列吡嗪在正辛醇-缓冲盐溶液体系中的油水分配系数减小。结论建立的方法可以准确测定格列吡嗪的平衡溶解度和表观油水分配系数,并借此解析其体内动态。

Objective To determine the equilibrium solubility and the partition coefficient of glipizide for designing new formulations.Method The equilibrium solubility of glipizide in various media was detected by HPLC, and a shake flask-ultraviolent spectrophotometry method was applied to determine the partition coefficient of glipizide in n-octanol-water-buffer solutions of different pH.Result The equilibrium solubility of glipizide was 7.79 mg·L-1 in water at 37 ℃ and increased with the pH increase of the buffer solution.lg P of glipizide was 1.63 in n-octanol-water system and decreased with increasing the pH of the buffer solution.Conclusion The methods described in this paper can be used to determine the equilibrium solubility and the partition coefficient of glipizide, and help to predict the intracoporal process.