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超临界流体辅助将吲哚美辛浸渍到壳聚糖热固性材料中用于控释应用。

Supercritical fluid assisted impregnation of indomethacin into chitosan thermosets for controlled release applications.

作者信息

Gong K, Darr J A, Rehman I U

机构信息

Clean Materials Technology Group, Department of Materials, Queen Mary University of London, Mile End Road, London E1 4NS, UK.

出版信息

Int J Pharm. 2006 Jun 6;315(1-2):93-8. doi: 10.1016/j.ijpharm.2006.02.030. Epub 2006 Mar 6.

DOI:10.1016/j.ijpharm.2006.02.030
PMID:16569485
Abstract

Supercritical carbon dioxide (sc-CO(2)) was used to impregnate indomethacin (a non-steroidal anti-inflammatory drug) into chitosan thermosets for the preparation of controlled release formulations. The products were analyzed by a range of methods including powder X-ray diffraction (XRD) and scanning electron microscopy (SEM). The effects of the experimental temperature and pressure of the sc-CO(2) on the thermal behavior of chitosan-indomethacin drug composites (DCs) was investigated via differential scanning calorimeter (DSC). The interaction of chitosan and indomethacin after impregnation was then studied by Fourier transform infrared (FTIR) and Raman spectroscopy, respectively. Our results suggest that the supercritical fluid impregnation process results in indomethacin being amorphously dispersed within the chitosan matrix. FTIR data suggest that the aliphatic carbonyl group of indomethacin interacts with the NH(2) group of the chitosan backbone. In vitro dissolution studies (via UV-vis spectroscopy) reveal that the dissolution rate of indomethacin substantially increases after processing in sc-CO(2), particularly, under the experimental conditions 20.7 MPa and 70 degrees C.

摘要

采用超临界二氧化碳(sc-CO₂)将吲哚美辛(一种非甾体抗炎药)浸渍到壳聚糖热固性材料中,以制备控释制剂。通过包括粉末X射线衍射(XRD)和扫描电子显微镜(SEM)在内的一系列方法对产物进行分析。通过差示扫描量热仪(DSC)研究sc-CO₂的实验温度和压力对壳聚糖-吲哚美辛药物复合物(DCs)热行为的影响。然后分别通过傅里叶变换红外(FTIR)和拉曼光谱研究浸渍后壳聚糖与吲哚美辛的相互作用。我们的结果表明,超临界流体浸渍过程导致吲哚美辛无定形地分散在壳聚糖基质中。FTIR数据表明,吲哚美辛的脂肪族羰基与壳聚糖主链的NH₂基团相互作用。体外溶出研究(通过紫外可见光谱法)表明,在sc-CO₂中处理后,吲哚美辛的溶出速率显著增加,特别是在20.7 MPa和70℃的实验条件下。

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