用乙基纤维素制备酮洛芬缓释固体分散体的研究

Sustained Release Solid Dispersions of Ketoprofen with Ethylcellulose

为评价以水不溶性聚合物EC 为载体,用固体分散技术( 溶剂法) 制备难溶性药物酮洛芬缓释固体分散体,并进行DSC 和体外释放度研究。DSC 结果表明:药物与EC 比例为1∶2 和1∶3 时药物以非晶态存在于载体中。体外释放度试验结果表明,药物体外释药行为均符合Higuchi 方程;缓释效果与EC 量和固体分散体的粒径有主要关系,药物释放速率随EC 用量和粘度增加而减小;固体分散体粒径越小药物体外释放速率越快;在pH 6 .8 介质中的体外释放速率高于在pH1 .2 介质。

Sustained release solid dispersions have been investigated using different amount and viscosity of EC as carriers and sparingly water soluble Ketoprofen(KPF) as a model drug. The solid dispersions were prepared by the solvent method. KPF can be dispersed amorphously with the KPF/EC ratio 1∶2 and 1∶3. The release profiles of the drug can be fitted the Higuchi model. By increasing the amount and viscosity of EC, and increasing the particle size of the solid dispersions from 200 600 μm, the release rate can be reduced. But prolongation of drug release was primarily associated with an increase in amount of ethylcellulose and particle size rather than the viscosity grade of ethylcellulose. KPF release rate was higher in the release media of pH 6.8 than that in the release media of pH \{1.2\}.