| 第 44 卷第 1 期 |  | Vol. 44 No. 1 | | 2014 年 2 月 | Feb 2014 |
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所屬欄目：醫藥及中間體
阿奇霉素一水晶型與二水晶型的制備與轉化 |
| 金 勇，喬 偉，王兆剛，侯仲軻*
（浙江國邦藥業(yè)有限公司，浙江 紹興 312369） |
| 摘 要：阿奇霉素存在2種不同的晶型：一水晶型和二水晶型，可通過(guò)控制結晶過(guò)程中的條件來(lái)制備。阿奇霉素二水晶型比一水晶型更穩定，一水晶型在一定的條件下轉化為二水晶型。一水晶型是動(dòng)力學(xué)控制的穩定狀態(tài)，而二水晶型是熱力學(xué)控制的穩定狀態(tài)。制備方法的區別以20 g阿奇霉素粗品、50 mL丙酮投料量為例，一水晶型制備初次加水5 mL，養晶溫度54~56℃，養晶0.5 h；二水晶型制備初次加水10 mL，養晶溫度38~42℃，養晶2 h。 |
| 關(guān)鍵詞：阿奇霉素；一水晶型；二水晶型；制備；轉化 |
| 中圖分類(lèi)號：R974 文獻標識碼：A 文章編號：1009-9212（2014）01-0016-03 |
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| 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 |
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作者簡(jiǎn)介：金 勇（1980-），男，江西萍鄉人，工程師，碩士，研究方向：化學(xué)工程。
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收稿日期：2014-01-24
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