采用亚临界水反溶剂法进行了醋酸甲地孕酮微粉化实验研究。通过考察与普通去离子水之间的温差、体积比、搅拌时间、表面活性剂等因素的影响，得到形貌均匀的醋酸甲地孕酮颗粒。实验结果表明，在普通去离子水、亚临界水的温度分别为0℃和170℃，体积比为13:6，搅拌速度1000r/min和搅拌时间1h，表面活性剂聚乙烯吡咯烷酮质量分数为0.1%的条件下，所制备的颗粒粒径在100～500nm之间。原料药和样品的红外光谱图对比结果显示，颗粒的化学结构没有发生变化。溶出结果表明，微粉化后的醋酸甲地孕酮颗粒溶出有了明显的提高，30min内溶出可达86.7%。
Abstract
The micronization of megestrol acetate (MA) was obtained by using the technology of subcritical water (SBCW) in this study. The influences of the experimental parameters, such as temperature difference, volume ratio of subcritical water and deionized water, stirring condition, surfactant concentration were studied. The optimized technological conditions were as follow: the temperature of subcritical water and deionized water was 0℃, 170℃ respectively, the volume ratio of 13:6, the proper stirring speed and time of the receiver (deionized water) were 1000r/min and 1h, the surfactant mass fraction of polyvinylpyrrolidone (PVP) was 01%. The diameter of the particles prepared in the optimal conditions was in a range of 100 to 500nm. Infrared spectra of raw materials and prepared samples showed that chemical construction did not occur in the experiment. Results of dissolution rate tests showed that the dissolution rate of MA particles was enhanced significantly, and 86.7% drug dissolution was achieved within 30min.
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