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磺胺甲噁唑/羟丙基-β-环糊精包合物的制备与表征。

Sulfamethoxazole:hydroxypropyl-β-cyclodextrin complex: preparation and characterization.

机构信息

Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina.

出版信息

J Pharm Biomed Anal. 2012 Apr 7;63:74-9. doi: 10.1016/j.jpba.2012.01.011. Epub 2012 Feb 2.

Abstract

A complex of sulfamethoxazole (SMX) and hydroxypropyl-β-cyclodextrin (HP-β-CD) was developed and characterized in order to investigate their interactions in aqueous solution and the solid state. The SMX solubility was significantly increased upon complexation with HP-β-CD, with the solubility isotherm being an A(N) type due to the presence of aggregates and the stability constant calculated for a 1:1 complex being 302 ± 3 M⁻¹. Fourier-transform infrared (FT-IR) spectroscopy and scanning electron microscopy (SEM) experiments were used to compare the freeze-dried system with a physical mixture, and demonstrated the complex formation in the solid state. The differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) showed that the thermal stability of SMX was enhanced in the presence of HP-β-CD.

摘要

为了研究磺胺甲噁唑(SMX)和羟丙基-β-环糊精(HP-β-CD)在水溶液和固态中的相互作用,开发并表征了它们的复合物。与 HP-β-CD 复合后,SMX 的溶解度显著增加,由于存在聚集体,因此溶解度等温线呈 A(N)型,计算得到的稳定常数为 1:1 复合物为 302±3 M⁻¹。傅里叶变换红外(FT-IR)光谱和扫描电子显微镜(SEM)实验用于比较冻干系统与物理混合物,并证明了固态中的复合物形成。差示扫描量热法(DSC)和热重分析(TGA)表明,在 HP-β-CD 的存在下,SMX 的热稳定性得到增强。

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