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目的:以羟丙基甲基纤维素(HPMC)-硬脂酸为载体制备雷公藤红素缓释固体分散体,提高药物释放度,控制药物缓慢稳定释放,降低其毒副作用。方法:将不同比列的HPMC-硬脂酸和雷公藤红素溶于95%乙醇中,溶剂蒸发法制备雷公藤红素固体分散体,进行体外溶出试验,差示扫描量热法、扫描电镜法、X-射线衍射法鉴别固体分散体的形成。结果:雷公藤红素和HPMC-硬脂酸按1∶10制备的固体分散体,药物缓慢释放,8 h时药物的体外累积释放达到90%以上;雷公藤红素以非晶形态分散在固体分散体中。结论:以HPMC-硬脂酸为载体制备的雷公藤红素缓释固体分散体,药物释放较完全且缓慢释放,制备工艺简单,具有潜在应用价值。
OBJECTIVE: To prepare tripterine sustained-release solid dispersion with hydroxypropyl methylcellulose (HPMC) -stearic acid as carrier, to improve the drug release, to control the slow and steady drug release, and to reduce its side effects. Methods: Different ratios of HPMC-stearic acid and tripterine were dissolved in 95% ethanol. Tripterygium solanum solid dispersion was prepared by solvent evaporation method. The dissolution rate was measured by differential scanning calorimetry and scanning electron microscopy Method, X-ray diffraction to identify the formation of solid dispersions. Results: Tripterygium wilfordii and HPMC-stearic acid prepared solid dispersion 1:10, the drug release slowly, 8 h cumulative drug release in vitro reached more than 90%; tripterine in amorphous form dispersed in solid Dispersion. Conclusion: Celastrol prepared with HPMC-stearic acid as carrier can release drug more completely and slowly, and its preparation process is simple and has potential application value.