超临界抗溶剂法研制卡马西平微粒  

Preparation of Carbamazepine Particles by Supercritical Anti-solvent Process

作　　者：潘丁丁[1] 颜庭轩[1] 王志祥[1] 黄德春[1] 党蓓蕾[1] 

机构地区：[1]中国药科大学药学院,江苏南京210009

出　　处：《中国医药工业杂志》2014年第4期349-353,共5页Chinese Journal of Pharmaceuticals

基　　金：江苏省自然科学基金资助项目(BK2012763);中央高校基本科研业务费专项资金资助项目(JKY2011026)

摘　　要：以丙酮为溶剂,采用超临界抗溶剂法制备卡马西平微粒,以增加药物的溶出速度。以产品粒径为指标,采用单因素和正交设计优化制备工艺。所得最优工艺组合为料液体积流量1 ml/min、压力8 MPa、温度50℃和料液质量浓度16 mg/ml。采用扫描电镜、红外、差示扫描量热和X射线衍射分析表征所得优化微粒,并测定了体外溶出度。结果表明,优化产品平均粒径约5.9um,粒度分布较均一,晶型为I型。与原药相比,所得优化微粒初始阶段溶出速率低于原药,但后期溶出率明显高于原药,240 min时溶出率达70.8%,而原药仅43.7%。To improve the dissolution of carbamazepine （1）, the particles were prepared by supercritical anti- solvent process with acetone as solvent. With particle size as the evaluation index, the preparation process was optimized by single factor experiment and orthogonal design. The optimal particles were prepared under the process conditions of solution volumetric flow rate of 1.0 ml/min, pressure of 8 MPa, temperature of 50 ℃ and 1 mass concentration of 16 mg/ml. The prepared particles were characterized by SEM, IR, DSC and XRD, the in vitro dissolution test was also conducted. The results showed that the average particle size of the optimal product was 5.9 um with I crystal form and narrow particle size distribution. Although the dissolution rate of the particles was lower than the bulk drug in the initial phase, but it was notably accelerated and finally the dissolution was about 70.8 % at 240 min, which was significantly higher than the bulk drug of 43.7%.

关 键 词：超临界抗溶剂法 卡马西平 微粒 晶型 溶出度 

分 类 号：R944.9[医药卫生—药剂学]