超临界CO2抗溶剂法制备微粉化阿西美辛  

Preparation of Micronized Acemetacin by Supercritical CO_2 Anti-solvent Process

作　　者：颜亭辕 林文[1] 宋杏芳 颜庭轩[1] 王志祥[1] 

机构地区：[1]中国药科大学工学院,江苏南京210009 [2]南京正大天晴制药有限公司,江苏南京210023 [3]江苏省药品不良反应监测中心江苏南京210002

出　　处：《中国医药工业杂志》2017年第1期55-59,93,共6页Chinese Journal of Pharmaceuticals

摘　　要：以粒径为主要评价指标,采用单因素试验和正交设计,优化了超临界CO_2抗溶剂法制备微粉化阿西美辛的工艺条件。所得优化参数为:溶剂为丙酮∶二氯甲烷(1∶1),结晶压力16 MPa,结晶温度40℃,阿西美辛浓度9 mg/ml。优化得到的微粉化阿西美辛粒径降至6.02mm;扫描电镜、红外、差示量热扫描等分析结果表明,微粉化阿西美辛的理化性质与原料药相比没有发生明显变化。并且,微粉化阿西美辛在水中10 min的溶出率超过20%,80 min时接近80%,溶出性能相较于原料药得到明显改善。The process parameters of the micronized acemetacin prepared by supercritical CO2 anti-solvent （SAS） technology were optimized with single factor experiment and orthogonal design. The optimal parameters were as follows： the optimal product was prepared with a mixture of acetone and dichloromethane （1∶1） as the solvent under conditions of pressure of 16 MPa, temperature of 40 ℃, and drug concentration of 9 mg/ml. The particle size of the optimal product was reduced to 6.02 μm, and the product was characterized by scanning electron microscopy （SEM）, infrared spectroscopy （IR）, and differential scanning calorimetry （DSC）. The results of these analyses showed no significant changes in physicochemical properties between the micronized acemetacin and the bulk drug. While the dissolution at 10 min of the micronized acemetacin in water was above 20% and at 80 min was about 80%, which indicated that the dissolution performance was significantly improved compared with the bulk drug.

关 键 词：超临界CO2 抗溶剂法 阿西美辛 微粉化 粒径 溶出度 

分 类 号：R944.9[医药卫生—药剂学]