第 50 卷第 1 期 Vol. 50 No. 1 2020 年 2 月 Feb 2020

所属栏目：医药及中间体 不同晶型二氢高红霉素的制备及稳定性研究

金 勇，汤 旗，单继雷，周志奎，侯仲轲 （浙江国邦药业有限公司，浙江 绍兴 312369）

摘　要：以红霉素亚胺醚为原料，采用Pt／C做催化剂，在甲醇中进行催化加氢反应，反应结束后，回收部分甲醇，用10%氢氧化钠水溶液调pH值10~12；35℃以上结晶得到了二氢高红霉素一水合物，30℃以下得到了二氢高红霉素二水合物。对两种晶型进行长期稳定性实验和加速稳定性实验研究，结果表明一水合物的有关物质稳定性优于二水合物。

关键词：二氢高红霉素；大环内酯类药物；晶型；稳定性实验

中图分类号：TQ465　　文献标识码：A　　文章编号：1009-9212（2020）01-0032-004

Stability of 9-Deoxo-9a-aza-9a-homoerythromycin A with Different Crystallization

JIN Yong, TANG Qi, SHANG Ji-lei, ZHOU Zhi-kui, HOU Zhong-ke (Zhejiang Goubang Pharmaceutical Co., Ltd., Shaoxing 312369, China)

Abstract：6,9-Iminoether was hydrogenated using Pt/C as catalyst in methanol. After the hydrogenation reaction was completed, part of methanol was distilled out from the reaction mixture. Finally, the pH of the residue is adjusted to a value of between 10~12 using 10% aqueous sodium hydroxide solution. The monohydrate of 9-deoxo-9a-aza-9a-homoerythromycin A is obtained by controlling the crystallization temperatureabove 35℃while the dihydrate of 9-deoxo-9a-aza-9a-homoerythromycin A was obtained by controlling the crystallization temperature blow 30℃. Expermental datafromaccelerated stability testing showed that the stability of monohydrate was better than that of dihydrate.

Key words：9-deoxo-9a-aza-9a-homoerythromycin A; macrolide antibiotic; crystallization; stability experiment

作者简介：金 勇（1980-），男，江西萍乡人，高级工程师，硕士，研究方向：医药化工（E-mail：jiny02@163.com）。

收稿日期：2020-01-20