卡托普利缓释微丸的制备及处方因素考察

Preparation of Captopril Sustained-release Pellets and Study of the Formulation

目的:制备卡托普利缓释微丸,并对其处方工艺因素进行考察。方法:选用尤特奇RS 30 D与尤特奇RL 30 D的混合物作为包农缓释材料,采用溶液层积法、流化床底喷方式,进行空白丸芯的上药和缓释包衣;并考察缓释聚合物尤特奇RS 30D与尤特奇RL 30D的不同比例、包衣增重,以及增塑剂用量对药物释放的影响。结果:当尤特奇RS 30D与尤特奇RL 30D的比例为4:1,包衣增重为10%,增塑剂用量为20%时,所制得的缓释微丸具有较好的缓释效果,在1、4和8 h的累积释放率分别为标示量的20%～35%,40%～65%和75%以上。结论:通过调整尤特奇RS 30D与尤特奇RL 30D之间的比例,或提高聚合物包衣增重等手段,能使卡托普利栽药微丸具备较理想的缓释效果。

Objective： To prepare captopril sustained release pellets, and study the relevant process and formulation. Method： Mixed Eudragit RS 30D and Eudragit RL 30D was chosen as the sustained release coating material. Solution - layered method was employed to prepare both the drug loaded pellets and the sustained coating with fluid bed bottom spray （wutster insert） ; meanwhile, studied various influencing factors in coating formulation, including ratios of Eudragit RS 30D and Eudragit RL 30D, polymer weight gain and levels of plasticizer, etc, on the drug sustained - release behavior. Result： When ratio of Eudragit RS 30D and Eudragit RL 30D, polymer weight gain and level of plasticizer were 4： 1, 10% and 20%, respectively, a ideal in vitro release behavior was reached, with the accumulated release percentage at 1,4 and 8h time intervals being 20% - 35% ,40% -65% and above 75% respectively. Conclusion ： A ideal release behavior could be obtained by adjustment of the ratio between Eudragit RS 30D and Eudragit RL 30D, as well as altering polymer weight gain, etc.