熔融法制备卡马西平-烟酰胺共结晶固体分散体  

Development and Evaluation of Carbamazepine-Nicotinamide Cocrystal Solid Dispersion Prepared by Melt Method

作　　者：刘旭[1] 彭新生[1] 苏健芬[1] 陆明[1] 吴传斌 

机构地区：[1]中山大学药学院,广东广州510006 [2]广东省高校创新药物制剂工程技术研究中心,广东广州510006

出　　处：《今日药学》2011年第1期10-13,32,共5页Pharmacy Today

基　　金：广东省高校创新药物制剂工程技术研究中心资助项目(编号:GCZX-A0801)

摘　　要：目的联用共结晶和固体分散技术,提高卡马西平的体外溶出度。方法以PVP VA64为载体,采用熔融法制备卡马西平-烟酰胺共结晶固体分散体。进行体外溶出实验,并采用粉末X射线衍射和差示扫描量热法鉴别卡马西平和烟酰胺在载体中的分散状态。结果卡马西平和烟酰胺结合形成共结晶后以无定形态或分子态分散在载体中,而在卡马西平固体分散体中,药物和载体形成低共融物,以微晶状态分散。卡马西平-烟酰胺共结晶固体分散体的体外溶出结果优于卡马西平固体分散体。结论共结晶固体分散体显著提高了药物的体外溶出度。Objective To improve the dissolution properties of carbamazepine with the combination of cocrystal and solid dispersion technologies.Methods The carbamazepine-nicotinamide cocrystal solid dispersion was prepared by melt method with PVP VA 64 as carriers.The release rate of carbamazepine was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by X-ray power diffraction（XRPD） and differential scanning calorimetry（DSC）.Results The results of XRPD,DSC proved the formation of cocrystal in carbamazepine-nicotinamide cocrystal solid dispersion,which existed as amorphous or molecules state.In carbamzepine solid dispersion,the drug was fine crystalline form.The dissolution performance in vitro of carbamazepine-nicotinamide cocrystal solid dispersion was better than carbamazepine solid dispersion.Conclusion The dissolution of carbamazepine is significantly improved by cocrystal-solid dispersion technique.

关 键 词：卡马西平 共结晶 固体分散体 溶出速率 

分 类 号：R943[医药卫生—药剂学]