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.
出处
《中国药物与临床》
CAS
2012年第8期984-986,共3页
Chinese Remedies & Clinics
基金
国家自然科学基金(30572367)
关键词
延胡索乙素
溶解度
色谱法
高压液相
Tetrahydropalmatine
Solubility
Chromatography, high pressure liquid
