盐酸安非他酮缓释片处方筛选及体外释放评价

Formulation and in-vitro release evaluation of bupropion hydrochloride extended-release tablet

目的筛选盐酸安非他酮缓释片的处方及缓释层包衣增重。方法分别以盐酸安非他酮缓释片片芯的物理参数及缓释片的释放曲线为考察指标,通过调整片芯处方中填充剂、润滑剂、助流剂及缓释层包衣增重,确定了盐酸安非他酮缓释片的处方。结果当片芯处方中采用微晶纤维素KG802、山嵛酸甘油酯和胶体二氧化硅时可获得片面较好的片芯,当处方中缓释层增重为4.0%时制得的缓释片分别在0.1 mol·L-1盐酸溶液、p H 4.5醋酸盐和p H 6.8磷酸盐溶出介质中的释放曲线与原研制剂释放行为相似。结论筛选的盐酸安非他酮缓释片处方合理。

Objective To formulate the core tablets and evaluate the weight gain of sustained release layer for bupropion hydrochloride extended-release tablets.Methods Through adjusting the fillers,lubricants,glidants of core tablet formulation and weight gain of sus-tained release coating,the formula of bupropion hydrochloride extended-release tablet was established according to the physical parame-ters of core tablets and the release profile respectively.Results Formulation with microcrystalline cellulose KG802,glyceryl behenate and colloidal silicon dioxide indicated an ideal appearance of core tablet.Formulation with a 4.0% weight gain of sustained release lay-er obtained similar release profile in 0.1 mol·L -1 HCl,pH 4.5 acetate and pH 6.8 phosphate medium compared to innovator drug re-spectively.Conclusions The selected formula of bupropion hydrochloride extended-release tablet was suitable.