| 第 50 卷第 1 期 |  | Vol. 50 No. 1 | | 2020 年 2 月 | Feb 2020 |
|
所屬欄目：醫藥及中間體
不同晶型二氫高紅霉素的制備及穩定性研究 |
| 金 勇，湯 旗，單繼雷，周志奎，侯仲軻
（浙江國邦藥業(yè)有限公司，浙江 紹興 312369） |
| 摘 要：以紅霉素亞胺醚為原料，采用Pt／C做催化劑，在甲醇中進(jìn)行催化加氫反應，反應結束后，回收部分甲醇，用10%氫氧化鈉水溶液調pH值10~12；35℃以上結晶得到了二氫高紅霉素一水合物，30℃以下得到了二氫高紅霉素二水合物。對兩種晶型進(jìn)行長(cháng)期穩定性實(shí)驗和加速穩定性實(shí)驗研究，結果表明一水合物的有關(guān)物質(zhì)穩定性?xún)?yōu)于二水合物。 |
| 關(guān)鍵詞：二氫高紅霉素；大環(huán)內酯類(lèi)藥物；晶型；穩定性實(shí)驗 |
| 中圖分類(lèi)號：TQ465 文獻標識碼：A 文章編號：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 |
|
作者簡(jiǎn)介：金 勇（1980-），男，江西萍鄉人，高級工程師，碩士，研究方向：醫藥化工（E-mail：jiny02@163.com）。
|
收稿日期：2020-01-20
|
|