对乙酰氨基酚缓释微丸的制备及释放度研究

Preparation and Release Behavior of Paracetamol Sustained-Selease Pellets

目的制备对乙酰氨基酚缓释微丸,考察包衣处方等因素对微丸释放度的影响。方法采用离心-造粒法制备微晶纤维素空白丸核和对乙酰氨基酚微丸,并在此基础上采用甲基丙烯酸树脂(Eudragit RS30D/RL30D)包衣,制备对乙酰氨基酚缓释微丸。采用HPLC法测定对乙酰氨基酚缓释微丸释放度,单因素筛选包衣处方的优化参数。结果以Eudragit RS30D/RL30D比例为15:1(w/w),包衣增重为10%,柠檬酸三乙酯占包衣材料量的25%,滑石粉占包衣材料量的40%为包衣液,制备的对乙酰氨基酚释微丸释药曲线具有较好的缓释特性。结论制备的对乙酰氨基酚缓释微丸具有缓释特性且操作简便、工艺稳定。

Objective In this paper we wanted to prepare paracetamol sustaied-release pellets and to study their release behavior. Methods Cenrifugal granulation method was used to prepare MCC pellets and paracetamol pellets respectively. On that basis Eudragit RS30D/RL30D as a coating material was adopted to coat the paracetamol pellets with a fluid bed spray processor. HPLC method was utilized to determine the release behavior of paracetamol sustained-release pellets. The coating prescription parameters were investigated and optimized with single factor experiments. Results The paracetamol sustained-release pellets coated with 10%coating material sustained released best, and the coating material consisted of Eudragit R.S30D/RL30D（15：1,w/w）, TEC（25%,w/w） and talc（40%,w/w）. Conclusion These showed that paracetamol sustained-release pellets contained a characteristic of sustained-release and the established process and formula were simple and stable.