黄体酮缓释栓剂的制备与优化

以热熔法制备黄体酮缓释栓剂,转篮法考察栓剂的体外溶出效果,并采用高效液相色谱法测定黄体酮的含量,筛选栓剂基质以及优化释放速度调节剂浓度.实验结果表明:以混合脂肪酸甘油酯作为栓剂基质制备的黄体酮缓释栓剂能保留50 h的完整形态;羟丙基甲基纤维素、羧甲基纤维素钠和硬脂酸3种释放速度调节剂的最佳浓度分别为1.5%、0.5%、1%,其中,以1%的硬脂酸为释放速度调节剂制备的黄体酮缓释栓剂在48h时的药物溶出度为73.90%,其释药时间超过50 h,缓释效果优于羟丙基甲基纤维素、羧甲基纤维素钠.

Preparation and Optimization of Progesterone Sustained-Release Suppositories

Sustained-release suppositories have the advantages of prolonged drug action time and good drug compliance. Effectively extending drug release time is essential for pharmaceutical process research. In this paper,progesterone sustained-release suppositories are prepared by hot-melt method,and the dissolution effect of suppositories in vitro is investigated by the basket method. HPLC method is used to quantitatively determine the content of progesterone,to screen the suppository matrix and to optimize the concentration of sustained-release agents. The experimental results show that the progesterone sustained-release suppository prepared with mixed fatty acid glyceride as a suppository base can retain the complete form for 50 hours. The optimal concentration of three slow-release agents( HPMC,CMC-Na and stearic acid) is 1. 5%,0. 5%,1% respectively,among which,progesterone sustainedrelease suppositories prepared with 1% stearic acid as a sustained-release suppository have a drug dissolution rate of only 73. 90% after 48 h,and its release time exceeds 50 h. Theerefore,the sustainedrelease effect of stearic acid is better than that of HPMC and CMC-Na.