延胡索乙素在不同溶剂中平衡溶解度及其油水分配系数的测定  

Assessment of equilibrium solubility in various solvents and oil/water partition coefficient for tetrahydropalmatine

作　　者：梁卓[1] 孙艺丹[1] 王锐利[1] 田青平[1] 张淑秋[1] 

机构地区：[1]山西医科大学药学院,太原030001

出　　处：《中国药物与临床》2012年第8期984-986,共3页Chinese Remedies & Clinics

基　　金：国家自然科学基金(30572367)

摘　　要：目的测定延胡索乙素在各种溶剂中的平衡溶解度以及在正辛醇-水中的表观油水分配系数,为延胡索乙素经皮给药制剂的制备提供实验基础。方法采用紫外分光光度法测定延胡索乙素在不同pH缓冲液中的平衡溶解度;采用高效液相色谱(HPLC)方法,测定不同介质中延胡索乙素的平衡溶解度;采用摇瓶法测定延胡索乙素的表观油水分配系数。结果 32℃延胡索乙素在pH7.4缓冲液中的平衡溶解度为32.47mg/L,在酸性缓冲液中溶解度增大;32℃延胡索乙素在油酸、吐温80中有较好的增溶能力,其溶解度分别为22165.21mg/L、69653.86mg/L;延胡索乙素的表观油水分配系数为3.12。结论延胡索乙素水溶性差,在油酸和吐温80中有较好的增溶能力。Objective To determine the equilibrium solubility of tetrahydropalmatine in various solvents and its apparent oil/water partition coefficient in n-octanol/water mixture, thus offering experimental basis for preparation of tetrahydropalmatine transdermal delivery medication. Methods Ultraviolet spectrophotometry and high-performance liquid chromatography were employed to determine the equilibrium solubility of tetrahydropalmatine in buffer solutions of pH values and various media, respectively. And the apparent oil/water partition coefficient was determined by shaking the flask. Results Tetrahydropalmatine was associated with an equilibrium solubility of 32.47 mg/L in pH 7.4 buffer solution at 32 ℃, and the figure might increase in acidic buffer solutions. Tetrahydropalmatine yielded preferable solubility in oleic acid （22 165.21 mg/L） and Tween 80 （69 653.86 mg/L） at 32℃. The apparent oil/water partition coefficient of of 3.12 was determined for tetrahydropalmatine. Conclusion Tetrahydropalmatine is featured of high solubility in oleic acid and Tween 80 yet low solubility in water.

关 键 词：延胡索乙素 溶解度 色谱法 高压液相 

分 类 号：R283[医药卫生—中药学]