雷公藤红素胶体二氧化硅缓释固体分散体研究

Sustained-release solid dispersion of tripterin carried by colloidal silia dioxide

目的制备雷公藤红素(tripterine)缓释固体分散体,使药物释放度提高,同时缓慢释放药物,以降低其毒副作用。方法以胶体二氧化硅为载体,采用溶剂蒸发法制备雷公藤红素固体分散体,对其体外溶出和物相特征进行研究。结果雷公藤红素和胶体二氧化硅按1∶12制备的固体分散体中,药物缓慢释放,8 h时药物的体外释放度达到90%以上。经差示扫描量热、X衍射和电镜分析,固体分散体中药物以非晶形式存在于载体中。结论雷公藤红素胶体二氧化硅固体分散体制备工艺简单,药物缓慢释放且释放较完全,具有实际应用价值。

Objective To prepare the sustained-release solid dispersion of tripterin （SRSDT） with the intention of improving drug dissolution, meanwhile, the drug release was slowed down so as to make the toxicity diminished. Methods SRSDT was prepared by the solvent method with colloidal silica dioxide （CSD） as carrier. The physical characteristics and in vitro release rate were further evaluated. Results The ideal SRSDT was prepared by mixing tripterin and colloidal silica dioxide with the weight ratio of 1 ： 12; The release rate of drug could keep moderate and controllable. In vitro cumulative release of SRSDT was up to more than 90% after 8 h. The results of differential scanning calorimetry, scanning electron microscopy, and X-ray powder diffraction could prove that the tripterin existed as amorphous form in the carrier. Conclusion The SRSDT carried by CSD could control the release rate of drug and keep moderate and controllable, and the preparation process is simple, which has potential applications.