甲磺酸倍他司汀微孔渗透泵控释片包衣处方的优化  

Optimization of the Coating Prescription of Betahistine Mesilate Controlled Porosity Osmotic Pump Tablets

作　　者：周苏[1] 冯晶[1] 郭斌[2] 

机构地区：[1]辽宁医学院,锦州市121001 [2]辽宁医学院附属第一医院,锦州市121000

出　　处：《中国药房》2011年第21期1970-1972,共3页China Pharmacy

摘　　要：目的:制备甲磺酸倍他司汀微孔渗透泵控释片,并对其包衣处方进行优化。方法:采用相似因子法考察影响释药的主要因素,采用正交试验以致孔剂聚乙二醇的用量、增塑剂邻苯二甲酸二丁酯(DBP)的用量和包衣增重为因素,以释放度的综合指标L值为指标优化包衣处方,并进行验证试验及体外释药模型拟合。结果:相似因子值均小于50,表明聚乙二醇、DBP的用量及包衣增重对制剂的释放均有显著影响;优化的最佳包衣处方中聚乙二醇为30%,DBP为20%,包衣增重为4%;验证试验中3批样品L值分别为13.99、11.15、8.37,12h累积释药百分率大于90%,释药模型特征为零级释药。结论:按最佳处方制得的甲磺酸倍他司汀微孔渗透泵控释片在12h内可稳定释药,且释放完全。OBJECTIVE：To prepare Betahistine mesilate controlled porosity osmotic pump tablets,and to optimize the coating prescription. METHODS：Main influencing factors of drug release of Betahistine mesilate controlled porosity osmotic pump tablets were investigated with single factor experiment. The coating prescription of Betahistine mesilate controlled porosity osmotic pump tablets was optimized by orthogonal test using amount of PEG and DBP as factors and with drug release indicator L as index. RESULTS：Similar factor was less than 50 which indicated that the amount of PEG,DBP and coating level influence the in vitro drug release significantly. The optimized coating prescription was PEG 30%,DBP 20% and the increases of coating material 4%. The drug release indicators of 3 batches of samples in validation test were 13.99,11.15 and 8.37. Accumulative drug release rate was more than 90% within 12 h,and drug release model showed zero-level drug release characteristics. CONCLUSION：Betahistine mesilate controlled porosity osmotic pump tablets with optimized prescription can achieve constant complete release in 12 hours.

关 键 词：甲磺酸倍他司汀 微孔渗透泵控释片 包衣处方 正交设计 优化 

分 类 号：R943[医药卫生—药剂学] R972[医药卫生—药学]