Binding of Sulfamethazine to β-cyclodextrin and Methyl-β-cyclodextrin
Binding of Sulfamethazine to β-cyclodextrin and Methyl-β-cyclodextrin
复制标题
DOI：
10.1208/s12249-013-9958-9
复制
发表时间：
2013-04
影响因子：
3.3
通讯作者：
A. Zoppi;Alicia Delrivo;V. Aiassa;M. Longhi
中科院分区：
文献类型：
--
作者：
A. Zoppi;Alicia Delrivo;V. Aiassa;M. Longhi
制备了β-环糊精（βCD）和甲基-β-环糊精（MβCD）与磺胺二甲嘧啶（SMT）的复合物，采用不同的实验方法对其进行了表征，并通过相溶解度分析评价了βCD和MβCD对药物溶解度的影响。药物的相溶解度图显示水溶性增加，计算出以下亲和常数：βCD为40.4 ± 0.4（pH 2.0）和29.4 ± 0.4（pH 8.0）M−1，MβCD为56 ± 1（水）、39 ± 3（pH 2.0）和39 ± 5（pH 8.0）M−1。根据1H NMR和2D NMR谱，络合模式涉及包含在MβCD空腔中的SMT的芳环。采用傅里叶变换红外光谱、扫描电子显微镜和热分析等手段对固相冷冻干燥法制备的配合物进行了表征。在本研究中获得的无定形复合物可能是有用的，在制备药物剂型的SMT。
β-cyclodextrin (βCD) and methyl-β-cyclodextrin (MβCD) complexes with sulfamethazine (SMT) were prepared and characterized by different experimental techniques, and the effects of βCD and MβCD on drug solubility were assessed via phase-solubility analysis. The phase-solubility diagram for the drug showed an increase in water solubility, with the following affinity constants calculated: 40.4 ± 0.4 (pH 2.0) and 29.4 ± 0.4 (pH 8.0) M−1 with βCD and 56 ± 1 (water), 39 ± 3 (pH 2.0) and 39 ± 5 (pH 8.0) M−1 with MβCD. According to 1H NMR and 2D NMR spectroscopy, the complexation mode involved the aromatic ring of SMT included in the MβCD cavity. The complexes obtained in solid state by freeze drying were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, and thermal analysis. The amorphous complexes obtained in this study may be useful in the preparation of pharmaceutical dosage forms of SMT.