通过高效液相色谱保留时间测定淫羊藿次苷-Ⅱ与苷元的油水分配系数  

Determination of Partition Coefficients of Icariside-Ⅱ and Icaritin Based on the HPLC Retention Time

作　　者：李妍[1] 孙少平[1,2] 郑颖[1] 

机构地区：[1]中药质量研究国家重点实验室(澳门大学)澳门大学中华医药研究院 [2]黑龙江大学,哈尔滨150080

出　　处：《中国药学杂志》2012年第2期122-126,共5页Chinese Pharmaceutical Journal

基　　金：澳门科学技术发展基金(资助号:FDCT008/2007/A1);澳门大学科研基金(资助号:UL016/09-Y3/CMS/WYT01/ICMS)资助

摘　　要：目的利用化合物在高效液相色谱的保留时间测定强脂溶性化合物淫羊藿次苷-Ⅱ与苷元的油水分配系数。方法选取一系列结构相似的化合物作为参考物质,采用摇瓶法或通过数据库获得其油水分配系数(partition coefficient)的对数lgP。利用高效液相色谱法测定参考物质在不同浓度有机相条件下的保留时间,外推得到有机相浓度为零时的容量因子kw,建立参考物质lgkw与lgP的线性关系方程式。用同样方法得到检验物质槲皮素和芒柄花素以及待测物质淫羊藿次苷-Ⅱ和苷元的kw。利用参考物质的线性关系方程式计算得到上述4个化合物的lgP,并和采用摇瓶法测定的检验物质的lgP作比较。结果建立了lgkw与lgP的关系方程式:lgP=(1.532±0.091)lgkw-(1.805±0.301)(r2=0.959 0),摇瓶法测定检验物质的lgP在高效液相色谱法测定的lgP范围内,说明所选一系列化合物在高效液相系统和正辛醇-水系统的分配行为相似,可以利用其在高效液相色谱上的保留时间来测定其在正辛醇-水系统中的分配系数。计算淫羊藿次苷-Ⅱ与苷元的lgP分别为(5.114±0.712)和(6.074±0.769)。结论 HPLC可较准确、方便、快速的测定强脂溶性化合物(lgP>4)油水分配系数。OBJECTIVE The aim of the study is to measure partition coefficients of two highly hydrophobic compounds, icari- side- Ⅱ and icaritin, based on their retention time on HPLC. METHODS A series of compounds with similar structure were selected as the reference substances and their partition coefficients were determined by shake-flask method or obtained from the science finder database. The retention time of the above reference substances was determined under different concentrations of organic phase. Logkw was obtained by extrapolating to zero concentration of organic phase. A linear relationship between lgP and lgkw was established. Logkw of two substances for validation purpose （ quercetin and formononetin） and two substances to be measured （ icariside- Ⅱ and icaritin） were obtained by the same method. LogP of above four compounds was calculated from the linear regression equation obtained from the reference substances and compared with the lgP of validation substances determined by shake-flask method. RESULTS A linear re- gression equation between lgP and lgkw was established ： lgP = （ 1. 532 ± 0. 091 ） lgkw - （ 1. 805 ± 0. 301 ） , r2 = 0. 959 0. The lgP of validation substances determined by shake-flask method is within the range of lgP measured by HPLC method, indicating that the parti- tion of the selected compounds in HPLC system is similar to that in octanol-water system. Therefore, the partition coefficient could be determined using their retention time on HPLC. The calculated lgP value of icariside-Ⅱ and icaritin is （5. 114 ± 0. 712） and （6. 074 ±0. 769） , respectively. CONCLUSION HPLC is an accurate, convenient and rapid method to determine the partition coef- ficient of highly hydrophobic compounds （lgP 〉 4）.

关 键 词：油水分配系数 高效液相色谱法 容量因子 淫羊藿次苷-Ⅱ 淫羊藿苷元 

分 类 号：R944[医药卫生—药剂学]