王艳宏++刘书博++关枫++陈大忠
摘要：目的 测定麻黄-附子药对提取物中麻黄类生物碱平衡溶解度和表观油水分配系数，为经皮给药研究提供依据。方法 采用70%乙醇提取、D101大孔吸附树脂纯化方法，制备麻黄-附子药对提取物。采用沉淀法联合HPLC，测定麻黄-附子药对提取物中主要有效成分麻黄碱和伪麻黄碱在各类溶剂中的平衡溶解度。采用摇瓶法，测定麻黄-附子药对中麻黄碱和伪麻黄碱在正辛醇-水中的表观油水分配系数。结果 提取物在甲醇和乙腈中的溶解度较大，麻黄碱和伪麻黄碱在pH 7.4磷酸盐缓冲液中的溶解度最大。麻黄碱、伪麻黄碱在正辛醇-水中的表观油水分配系数分别为0.101（lgP=-0.99）、0.076（lgP=-1.12）。提取物中麻黄生物碱类成分的油水分配系数受pH值影响较大。结论 提取物在极性大的溶剂中溶解性较好，适宜的pH值可在一定范围内改善其有效成分的水溶性和脂溶性，从而有利于透皮吸收。
关键词：麻黄-附子药对；麻黄类生物碱；平衡溶解度；表观油水分配系数；高效液相色谱法
DOI：10.3969/j.issn.1005-5304.2017.01.022
中图分类号：R284.1 文献标识码：A 文章编号：1005-5304（2017）01-0091-04
Investigation of Dissolvability of Ephedra Alkaloid in Compatibility Ephedrae Herba- Aconiti Lateralis Radix Praeparata WANG Yan-hong， LIU Shu-bo， GUAN Feng， CHEN Da-zhong （Heilongjiang University of Chinese Medicine， Harbin 150040， China）
Abstract： Objective To determine equilibrium solubility and apparent oil/water partition coefficient of ephedra alkaloid in the compatibility Ephedrae Herba-Aconiti Lateralis Radix Praeparata； To provide a basis for transdermal delivery. Methods The extract was prepared by 70% ethyl alcohol and D101 macroporous absorbent resins. Dissolvability of its main effective components （ephedrine and pseudoephedrine） in the compatibility Ephedrae Herba-Aconiti Lateralis Radix Praeparata was determined by precipitation method and HPLC method； the oil/water partition coefficient of ephedrine and pseudoephedrine in n-octanol-water buffer solution system were determined by shaking flask method. Results The extract had optimum solubility in methyl alcohol and acetonitrile， and ephedrine and pseudoephedrine had optimum solubility in buffered solution of pH 7.4. Oil/water partition coefficient of ephedrine and pseudoephedrine in n-octanol-water system was 0.101 with lgP=-0.99 and 0.076 with lgP=-1.12. Oil-water partition coefficients of ephedrine and pseudoephedrine in the extract were affected by pH. Conclusion The extract has optimum solubility in high polar solvents. Ephedrine and pseudoephedrine have certain fatsoluble and water-soluble in suitable pH， which was beneficial for transdermal absorption.
Key words： compatibility Ephedrae Herba-Aconiti Lateralis Radix Praeparata； ephedra alkaloid； equilibrium solubility； apparent oil/water partition coefficient； HPLC
麻黄-附子为临床常用药对，在《伤寒论》的麻黄附子汤、麻黄附子细辛汤、麻黄附子甘草汤、乌头汤等方剂中均有应用。麻黄辛温，具有发汗解表、宣肺平喘、利水消肿功效；附子辛热，具有回阳救逆、
基金项目：国家自然科学基金（81473359）；黑龙江省科技厅青年基金项目（QC07C107）；黑龙江省自然科学基金（H201472）；黑龙江省教育厅科学技术研究项目（11531357）
通讯作者：陈大忠，E-mail：799378826@qq.comendprint
