磷酸川芎嗪微孔渗透泵片的研制及释药机制研究  

Preparation and Drug Release Mechanism of Tetramethylpyrazine Phosphate Porosity Osmotic Tablet

作　　者：宋金春[1] 以盛[2] 吕桦[2] 邓瑞园[2] 

机构地区：[1]武汉大学人民医院药学部,武汉市430060 [2]武汉大学药学院,武汉市430072

出　　处：《中国药房》2008年第6期420-424,共5页China Pharmacy

摘　　要：目的:制备磷酸川芎嗪微孔渗透泵片,并进行处方优化和释药机制考察。方法:利用单因素考察和正交试验设计,优化筛选出最佳处方;测定不同处方制剂累积释药百分率;并对其释药机制进行探讨。结果:包衣膜中致孔剂聚乙二醇400用量、片芯羟丙甲基纤维素含量、增塑剂邻苯二甲酸二丁酯用量、包衣增重为影响药物释放的4个重要因素。最优处方为聚乙二醇400用量10%,羟丙甲基纤维素用量5%,增塑剂10%,包衣增重12mg,制得微孔渗透泵片在12h内呈现零级控释释放特征(r=0.99981),累积释放率为94.2%,批间重现性良好,不受胃肠道环境影响;释药机制包括渗透泵机制和扩散机制,以渗透泵机制为主。结论:该微孔渗透泵片处方及制备工艺简单有效,12h零级释放特征显著,重现性好,可为工业生产提供理论依据。OBJECTIVE： To prepare Tetramethylpyrazine phosphate porosity osmotic tablet （TMPP） and to optimize its formulation and investigate its mechanism of drug release. METHODS： The formulation was optimized by the orthogonal experiment design through investigation of one factor; the accumulative drug release rates of preparations of different formulation were measured, and the mechanism of drug release of the tablets was discussed. RESULTS： The dosage of PEG 400 in coating solution, the content of hydroxy -propyl methyl cellulose （HPMC） in tablet core, the dosage of dibutylphthalate as plasticizer, and the weight gain of coating membrane were four important factors influencing drug release. The optimal formulation was to use 10% of PEG400, 5% of HPMC, 10% of dibutylphthalate and 12 mg coating membrane. The release behavior in vitro of the porosity osmotic tablets prepared in the above condition within 10 h complied with zero order release rule（ r = 0.999 81）, with accumulative release rate of 94.2%. The tablets had good reproducibility in interassay and which was independent of the influence of gastrointestinal condition. The mechanism of drug release included osmotic pump mechanism and diffusion mecha- nism, but osmotic pump one was the main type. CONCLUSION： The formulation and preparation technology of the porosity osmotic tablets were simple but effective, showing an obvious zero order release within 12 h and good reproducibility, thus suitable for the industrial production of porosity osmotic tablets.

关 键 词：磷酸川芎嗪 微孔渗透泵 零级释放 

分 类 号：R972[医药卫生—药品] R944.4[医药卫生—药学]