吲哚美辛共聚维酮非晶态制剂的性质及体外溶出度考察  

Properties and in Vitro Dissolution of Indomethacin Co-PVP Amorphous Preparation

作　　者：潘凤[1,2] 王转[2,3] 姚静[1,2] 尹东东[2] 时念秋[2] 王杏林[2] 

机构地区：[1]河南大学,河南开封475001 [2]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300193 [3]天津中医药大学,天津300193

出　　处：《中国药学杂志》2017年第1期47-52,共6页Chinese Pharmaceutical Journal

基　　金：国家重大新药创制项目(2014ZX09507005-002)

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。OBJECTIVE To prepare indomethacin amorphous preparation with Co-PVP as carrier, characterize it for exploring the interaction between indomethacin and Co-PVP, and investigate the difference of dissolution between indomethacin crystalline and amorphous preparations. METHODS The inhibitory effect of Co-PVP on the crystallization of indomethacin supersaturated solution was studied. The indomethacin amorphous preparation was prepared by solvent evaporation method and characterized by differential scanning calorimetry （DSC）, powder X-ray diffraction （PXRD）, and Fourier transform infrared spectroscopy （FT-IR）. In addition, the dissolution behavior in vitro was investigated. RESULTS Co-PVP had an inhibitory effect on the crystallization of indomethacin supersaturated solution evidently. Indomethacin existed in amorphous state in Co-PVP as hydrogen bonds formed between them. The amorphous preparation of indomethacin-Co-PVP improved the dissolution rate and extent obviously. CONCLUSION The indomethacin amorphous preparation with Co-PVP as carrier can improve the dissolution in vitro significantly, which providing a reference for obtaining stable amorphous preparation.

关 键 词：吲哚美辛 非晶态 共聚维酮 结晶抑制 溶出度 

分 类 号：R944[医药卫生—药剂学]