吲哚美辛Soluplus非晶态制剂的性质及体外溶出考察

Properties and dissolution in vitro of indomethacin Soluplus amorphous preparation

目的:以Soluplus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Soluplus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Soluplus对药物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与Soluplus非晶态制剂。通过粉末X射线衍射(PXRD)、差示扫描量热(DSC)及傅立叶红外光谱(FTIR)加以表征,并进行体外溶出实验。结果:Soluplus可明显抑制吲哚美辛超饱和溶液的结晶。吲哚美辛与Soluplus以氢键形式缔合,药物以非晶态分散于载体中。该非晶态制剂显著提高了药物的溶出速度和程度。结论:以Soluplus为载体制备的吲哚美辛非晶态制剂使药物的溶出速度和程度显著提高,为获得稳定的非晶态制剂提供参考。

Objective：To prepare and characterize indomethacin amorphous preparation with Soluplus as carrier, investigate the interaction between drug molecules and Soluplus, and compare the dissolution in vitro of crystalline and amorphous indomethacin preparations. Methods： The crystallization inhibition effect of Soluplus on the supersaturated solution of indomethacin was investigated. Indomethacin amorphous preparation was prepared by solvent evaporation method. Differential scanning calorimetry （DSC）, powder X-ray diffraction （PXRD）, and Fourier transform infrared spectroscopy （FTIR） were used to study the existing status of indomethacin in amorphous preparation and bond between indomethacin and carriers. Its dissolution in vitro was also determined. Results： Soluplus＇s crystallization inhibition effect on indomethacin was obvious. The indomethacin was binded with Soluplus via hydrogen bonds and dispersed in the carrier in amorphous form. The rate and extent of dissolution of indometha- cin amorphous preparation in vitro were significantly increased. Conclusion：Using Soluplus as carrier for indom- ethacin amorphous preparation can improve the dissolution rate and extent in vitro remarkably, which provides refer- ence for obtaining a stable amorphous preparation.