吲哚美辛共聚维酮非晶态制剂的性质及体外溶出度考察

发布时间：2018-07-03 16:56

本文选题：吲哚美辛 + 非晶态　；参考：《中国药学杂志》2017年01期

【摘要】：目的以共聚维酮(Co-PVP)为载体制备吲哚美辛非晶态制剂,对其加以表征以探讨药物分子与Co-PVP间的相互作用形式,并比较吲哚美辛晶态与非晶态的体外溶出差异。方法考察了Co-PVP对吲哚美辛超饱和溶液的结晶抑制作用。采用溶剂蒸发法制备吲哚美辛非晶态制剂,通过差示扫描量热(DSC)、粉末X射线衍射(PXRD)和傅立叶红外光谱(FTIR)技术对其表征,并进行了体外溶出实验。结果 Co-PVP对吲哚美辛超饱和溶液有较强的抑晶作用。吲哚美辛与Co-PVP分子之间形成氢键,主药以非晶态分散于载体中,该非晶态制剂的体外溶出速率和程度均显著增加。结论以Co-PVP为载体制备的非晶态制剂能显著提高吲哚美辛体外溶出,可为获得稳定的药物非晶态制剂提供参考。
[Abstract]:Objective to prepare indomethacin amorphous preparation with co-PVP as carrier, to investigate the interaction between drug molecules and Co-PVP, and to compare the dissolution of indomethacin in vitro. Methods the inhibition of Co-PVP on the crystallization of indomethacin supersaturated solution was investigated. Indomethacin amorphous preparation was prepared by solvent evaporation method. It was characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR). Results Co-PVP had strong inhibitory effect on indomethacin supersaturated solution. The hydrogen bond between indomethacin and Co-PVP was formed, and the main drug was dispersed in the carrier in amorphous state. The dissolution rate and degree of the amorphous preparation in vitro increased significantly. Conclusion Co-PVP as carrier can significantly improve the dissolution of indomethacin in vitro and provide a reference for obtaining stable amorphous preparations.
【作者单位】：河南大学;天津药物研究院有限公司释药技术与药代动力学国家重点实验室;天津中医药大学;
【基金】：国家重大新药创制项目(2014ZX09507005-002)
【分类号】：R943

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