左旋氨氯地平溶析结晶工艺的研究  

Study on Solventing-out Crystallization Process of Levoamlodipine

作　　者：卢定强[1,2] 常亚军[1] 凌岫泉[1] 贾静[1] 党安旺[1] 

机构地区：[1]南京工业大学药学院,南京210009 [2]江苏省药物研究所,南京210009

出　　处：《中国现代应用药学》2010年第11期1006-1009,共4页Chinese Journal of Modern Applied Pharmacy

基　　金：国家自然科学基金(20876076)

摘　　要：目的研究利用溶析结晶法提纯左旋氨氯地平的工艺。方法采用差重法测定正庚烷-二氯甲烷混合溶剂的溶解度,研究了左旋氨氯地平溶析结晶的温度、反溶剂的含量及导入方式、搅拌转速对左旋氨氯地平的纯度和收率的影响。结果左旋氨氯地平在正庚烷-二氯甲烷溶液中的溶解度随着正庚烷浓度的升高而减小,确定了最佳结晶条件为温度：25℃;正庚烷/二氯甲烷质量比为1.5~1.75;搅拌速度：300 r.min·1。结论该结晶工艺得到的产品纯度和收率较高,其工艺具有操作简易、易于工业化等特点,同时也为氨氯地平单一对映体制备成各种剂型开辟良好的前景。OBJECTIVE To study the solventing-out crystallization process of levoamlodipine.METHODS The gravimetric method was used to measure the solubility of levoamlodipine in the mixture of n-heptane and dichloromethane.It is studied the effect factors on the purity and the yield of levoamlodipine crystallization which included the temperature,the quantity of anti-solvent,the flow rate of n-heptane introduced into levoamlodipine dichloromethane solution and the rotary speed.RESULTS The solubility of levoamlodipine in the mixture increased remarkably during the reduction of the n-heptane＇s ratio at the fixed temperatures.The optimized condition was temperatures： 25 ℃;the mass ratio of n-heptane to dichloromethane： 1.5？1.75;rate of rotation： 300 r.min？1.CONCLUSION The product obtained from the crystallization process has the higher purity and yield.The technology has the advantages such as simple operation,easy-to-industrialization and so on.What is more,it is opening up good prospects for preparation of the single amlodipine enantiomer of a variety of formulation.

关 键 词：左旋氨氯地平 溶析结晶 纯度 收率 

分 类 号：R916.691[医药卫生—药学]