中成药2017，Vol.39Issue(10)：2034-2038,5.DOI:10.3969/j.issn.1001-1528.2017.10.009
马钱子总碱中2种成分的平衡溶解度、油水分配系数、体外透皮特性
Equilibrium solubilities, oil-water partition coefficients and in vitro skin permeation features of two constituents in total alkaloids from Strychni Semen
摘要
Abstract
AIM To investigate the equilibrium solubilities,oil-water partition coefficients and in vitro skin permeation features of brucine and strychnine in total alkaloids from Strychni Semen.METHODS Saturated dissolution method was applied to determining the equilibrium solubilities of two constituents in ethanol (10％,20％,30％,60％,90％,anhydrous ethanol),trichloromethane,n-octanol and surfactants (0.5％ tween,0.5％ sodium deoxycholate,0.5％ oleic acid).Shake-flask method was adopted in detecting their oil-water partition coefficients in PBS (pH 2.5,4.0,5.0,5.8,6.8,7.0,7.4,9.0).Modified Franz diffusion cell method was used for evaluating their in vitro skin permeation features in PBS,20％ ethanol and anhydrous ethanol.RESULTS Both brucine and strychnine showed the highest equilibrium solubilities in trichloromethane and the lowest equilibrium solubilities in surfactants.The equilibrium solubility of strychnine was higher than that of brucine in ethanol (＞ 20％) or PBS (pH ＜ 8.0),which reached the highest in 60％ ethanol and pH 2.5 PBS,respectively.The similar oil-water partition coefficients of two constituents,proportional to pH value,reached the highest at pH9.0.And they exhibited the highest accumulated transdermal absorptivities in anhydrous ethanol and pH 9.0 PBS,respectively.CONCLUSION Solvent type has obvious effects on the equilibrium solubilities,oil-water partition coefficients and in vitro skin permeation features of both brucine and strychnine.This study can provide a reference for the bioavailability improvement of transdermal drug delivery and development of related preparations.关键词
马钱子总碱/马钱子碱/士的宁/平衡溶解度/油水分配系数/体外透皮特性Key words
total alkaloids from Strychni Semen/brucine/strychnine/equilibrium solubilities/oil-water partition coefficients/in vitro skin permeation features分类
医药卫生引用本文复制引用
王艳宏,齐笑,关枫,冯宇飞,李永吉,陈大忠..马钱子总碱中2种成分的平衡溶解度、油水分配系数、体外透皮特性[J].中成药,2017,39(10):2034-2038,5.基金项目
国家自然科学基金项目(81473359) （81473359）
黑龙江省科技厅青年基金项目(QC07C107) （QC07C107）
黑龙江省教育厅科学技术研究项目(11531357) （11531357）
