Chiralcel OJ-H手性色谱柱-HPLC法同时分离4种H_1受体拮抗药的对映体  

Simultaneous Separation of 4 Kinds of H_1-Receptor Antagonist Enantiomers by Chiralcel OJ-H Chiral Column-HPLC

作　　者：李尚颖 陈默 张耀文 隋晓璠 孙苓苓 国梦然 LI Shangying;CHEN Mo;ZHANG Yaowen;SUI Xiaofan;SUN Lingling;GUO Mengran(Liaoning Institute for Drug Control,Shenyang 110036,China;College of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]辽宁省药品检验检测院,沈阳110036 [2]沈阳药科大学药学院,沈阳110016

出　　处：《中国药房》2018年第23期3189-3193,共5页China Pharmacy

基　　金：国家自然科学基金资助项目(No.81502993)

摘　　要：目的:建立拆分盐酸西替利嗪、盐酸异丙嗪、特非那定和马来酸非尼拉敏4种H1受体拮抗药对映体的方法。方法:采用高效液相色谱法(HPLC),选择Chiralcel OJ-H手性色谱柱,检测波长为230 nm,柱温为室温,流速为1.0 mL/min,进样量为20μL;以保留时间、选择因子和分离度为指标,考察流动相中酸碱添加剂(二乙胺)、有机改性剂的种类(乙醇、异丙醇)及其占比、甲醇等对4种药物对映体分离的影响。结果:流动相考察结果为盐酸西替利嗪和盐酸异丙嗪的流动相为正己烷-乙醇(90∶10,V/V);特非那定的流动相为正己烷-甲醇-乙醇-二乙胺(89∶9.9∶1∶0.1,V/V/V/V);马来酸非尼拉敏对映体的流动相为正己烷-甲醇-乙醇-二乙胺(98∶2∶0.5∶0.1,V/V/V/V)。在此条件下,4种药物的对映体均达到完全分离,分离度分别为4.36、3.76、1.55、1.71。结论:建立的Chiralcel OJ-H手性色谱柱-HPLC法对这4种H1受体拮抗药的选择性良好,可用于其对映体的手性分离。OBJECTIVE：To establish a method for separating of 4 kinds of H1-receptor antagonist enantiomers as cetirizine hydrochloride, promethazine hydrochloride, terfenadine and pheniramine maleate. METHODS： HPLC method was adopted. Chiralcel OJ-H chiral column was selected. Detection wavelength was set at 230 nm;column temperature was room temperature; flow rate was 1.0 mL/min;sample size was 20 μL. Using retention time,selective factors and separation rate as indexes,the influence of acid-base additives （diethylamine）,type and ratio of organic modifiers （ethanol,isopropanol）,methanol on the separation of 4 kinds of enantiomers in mobile phase were investigated. RESULTS：The results of mobile phase investigation was the mobile phase of cetirizine hydrochloride and promethazine hydrochloride was n-hexane and ethanol （90 ∶ 10,V/V）. Mobile phase of terfenadine was n-hexane-methanol-ethanol-diethylamine（89 ∶ 9.9 ∶ 1 ∶ 0.1,V/V/V/V）. Mobile phase of pheniramine maleate enantiomers was n-hexane-methanol-ethanol-diethylamine （98 ∶ 2 ∶ 0.5 ∶ 0.1,V/V/V/V）. Under the condition,4 kinds of drug enantiomers were separated completely,with separate rate of 4.36,3.76,1.55,1.71. CONCLUSIONS：Established Chiralcel OJ-H chiral column-HPLC is selective for these 4 kinds of H1-receptor antagonists,and can be used for the chiral separation of the enationmers.

关 键 词：CHIRALCEL OJ-H手性色谱柱 高效液相色谱法 H1受体拮抗药 盐酸西替利嗪 盐酸异丙嗪 特非那定 马来酸非尼拉敏 对映体 

分 类 号：R917[医药卫生—药物分析学]