世界中医药

目的：测定通脉散瘀凝胶提取物及指标成分在不同溶剂中的平衡溶解度及不同pH下的表观油水分配系数，探索通脉散瘀凝胶提取物的溶解性能。方法：采用沉淀法测定提取物的溶解度，以指标成分法测定提取物在不同溶剂中的平衡溶解度以及在正辛醇/水和正辛醇/缓冲液中的表观油水分配系数。结果：37 ℃时提取物在乙醇中的平衡溶解度较大，在缓冲液中呈先减小后增大趋势；以指标成分来看，丹酚酸B和丹参素在pH缓冲液中溶解度先减小后增大，丹参酮ⅡA和隐丹参酮在pH 9时平衡溶解度达到最大；丹酚酸B和丹参素的油水分配系数随pH增大而减小，丹参酮ⅡA和隐丹参酮在pH8时lgP达到最大。结论：通脉散瘀提取物在醇类中的溶解度较大，可考虑在处方中加入适量乙醇提高溶解度；pH影响提取物的油水分配系数，可通过调节pH值来促进其经皮吸收。

English Summary:

To determine Tongmaisanyu gel extract and index components in different solvents' equilibrium solubility and apparent partition coefficient in different pH to explore the solvent performance of Tongmaisanyu extract. Methods:Taking the precipitation method for the determination of the solubility of the extract and equilibrium solubility of index components in different solvents as well as partition coefficient in n-octanol / water and n-octanol / buffer. Results:The equilibrium solubility of the extract in ethanol was higher at 37 ℃, and it decreased first and then increased in buffer; the solubility of salvianolic acid B and danshensu in pH buffer decreased first and then increased, and the equilibrium solubility of tanshinone ⅡA and cryptotanshinone was the highest at pH 9; the oil-water partition coefficient of salvianolic acid B and danshensu decreased with the increase of pH, and the lgP of tanshinone ⅡA and cryptotanshinone reached the maximum at pH8. Conclusion:Tongmaisanyu extract dissolves greater in alcohols, so adding an appropriate amount of ethanol in the formulation to increase the solubility may be favorable. And pH can affect the partition coefficient, so for percutaneous absorption may be promoted by adjusting the pH values.

查看全文查看/发表评论下载PDF阅读器