第 44 卷第 1 期 Vol. 44 No. 1 2014 年 2 月 Feb 2014

所属栏目：医药及中间体 阿奇霉素一水晶型与二水晶型的制备与转化

金 勇，乔 伟，王兆刚，侯仲轲* （浙江国邦药业有限公司，浙江 绍兴 312369）

摘　要：阿奇霉素存在2种不同的晶型：一水晶型和二水晶型，可通过控制结晶过程中的条件来制备。阿奇霉素二水晶型比一水晶型更稳定，一水晶型在一定的条件下转化为二水晶型。一水晶型是动力学控制的稳定状态，而二水晶型是热力学控制的稳定状态。制备方法的区别以20 g阿奇霉素粗品、50 mL丙酮投料量为例，一水晶型制备初次加水5 mL，养晶温度54~56℃，养晶0.5 h；二水晶型制备初次加水10 mL，养晶温度38~42℃，养晶2 h。

关键词：阿奇霉素；一水晶型；二水晶型；制备；转化

中图分类号：R974　　文献标识码：A　　文章编号：1009-9212（2014）01-0016-03

Preparation and Transformation of Azithromycin in the forms of Monohydrate and Dihydrate

IN Yong，QIAO Wei，WANG Zhao-gang，HOU Zhong-ke* （Zhejiang Guobang Pharmaceutical Co.，Ltd.，Shaoxing 312369，China）

Abstract：Azithromycin is a macrolide antibiotic with two crystalline forms of monohydrate and dihydrate. They can be prepared by changing the crystallization conditions. The dynamically stable monohydrate can be converted to the thermodynamically stable dihydrate in crystallization process. For example，20 g of azithromycin was dissolved in 50 mL of acetone. The monohydrate was prepared under conditions that the first amount of water was 5 mL，the temperature and the time of crystal growing was 54~56℃ and 0.5 h. The dihydrate was prepared under conditions that the first amount of water was 10 mL，the temperature and the time of crystal growing was 38~42℃ and 2 h.

Key words：azithromycin；monohydrate；dihydrate；preparation； transformation

作者简介：金 勇（1980-），男，江西萍乡人，工程师，硕士，研究方向：化学工程。

收稿日期：2014-01-24