Characterization of azithromycin hydrates
Characterization of azithromycin hydrates
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DOI：
10.1016/s0928-0987(02)00087-8
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发表时间：
2002-08-01
影响因子：
4.6
通讯作者：
Panchagnula, R
中科院分区：
文献类型：
--
作者：
Gandhi, R;Pillai, O;Panchagnula, R
阿奇霉素 (AZI) 是一种大环内酯类抗生素，具有广泛的活性，以二水合物形式市售。进行这项研究是为了表征阿奇霉素水合物。使用商业二水合物样品从水/乙醇 (1:1) 混合物中制备一水合物。使用 DSC、TGA、KFT、XRD、HSM、SEM 和 FT-TR 表征水合物。 TGA 显示商业样品是二水合物，而由水/乙醇（1:1）制备的样品是一水合物。溶解度研究表明，在溶解度研究过程中，一水合物转化为二水合物，因此 MH 和 DH 的平衡溶解度没有显着差异。各种条件下的热分析表明脱水和熔化同时发生。发现无水 AZI 具有吸湿性，在室温下储存时会转化为 DH。分子模型研究揭示了水分子可能附着在 AZI 上的位点。 (C) 2002 Elsevier Science B.V. 保留所有权利。
Azithromycin (AZI) is a macrolide antibiotic with an expanded spectrum of activity that is commercially available as a dihydrate. This study was carried out to characterize hydrates of azithromycin. A commercial dihydrate sample was used to prepare monohydrate from water/ethanol (1:1) mixture. Hydrates were characterized using DSC, TGA, KFT, XRD, HSM, SEM and FT-TR. TGA showed that the commercial samples are dihydrate and the sample prepared from water/ethanol (1:1) was a monohydrate. Solubility studies revealed that monohydrate converted to dihydrate during solubility studies and as a result there was no significant difference in the equilibrium solubility of MH and DH. Thermal analysis under various conditions revealed that dehydration and melting took place simultaneously. Anhydrous AZI was found to be hygroscopic and converted to DH on storing at room temperature. Molecular modeling studies revealed the probable sites of attachment of water molecules to AZI. (C) 2002 Elsevier Science B.V. All rights reserved.