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, 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
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Key words
indomethacin /
amorphous /
Co-PVP /
crystallization inhibition /
dissolution
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中图分类号：
R944
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参考文献
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脚注
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基金
国家重大新药创制项目(2014ZX09507005-002)
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