Three solvent based methods: spray drying (SD), electrospinning (ES) and air-assisted electrospinning (electroblowing; EB) were used to prepare solid dispersions of itraconazole and Eudragit E. Samples with the same API/polymer ratios were prepared in order to make the three technologies comparable. The structure and morphology of solid dispersions were identified by scanning electron microscopy and solid phase analytical methods such as, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Raman chemical mapping. Moreover, the residual organic solvents of the solid products were determined by static headspace-gas chromatography/mass spectroscopy measurements and the wettability of samples was characterized by contact angle measurement. The pharmaceutical performance of the three dispersion type, evaluated by dissolution tests, proved to be very similar. According to XRPD and DSC analyses, made after the production, all the solid dispersions were free of any API crystal clusters but about 10 wt% drug crystallinity was observed after three months of storage in the case of the SD samples in contrast to the samples produced by ES and EB in which the polymer matrix preserved the API in amorphous state.

译文

:三种基于溶剂的方法:喷雾干燥(SD),电纺(ES)和空气辅助电纺(电吹; EB)用于制备伊曲康唑和Eudragit E的固体分散体。按顺序制备具有相同API /聚合物比的样品使这三种技术具有可比性。通过扫描电子显微镜和固相分析方法,如X射线粉末衍射(XRPD),差示扫描量热法(DSC)和拉曼化学作图,鉴定了固体分散体的结构和形态。此外,通过静态顶空-气相色谱/质谱法测定来测定固体产物的残留有机溶剂,并通过接触角测定来表征样品的润湿性。通过溶出度测试评估的三种分散体类型的药物性能非常相似。根据生产后进行的XRPD和DSC分析,所有固体分散体均不含任何API晶体簇,但与生产的样品相比,SD样品在储存三个月后观察到约10 wt%的药物结晶度通过ES和EB,其中聚合物基质将API保持在非晶态。

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