星点设计-效应面法优化复方葛黄微孔渗透泵片的处方组成

Optimization of Prescription of Compound Gehuang Microporous Osmotic Pump Tablets by Central Composite Design-response Surface Methodology

目的:优化复方葛黄微孔渗透泵片的处方组成,为中药有效组分的口服渗透泵控释制剂提供研究模式,促进新技术、新工艺在中药领域中的应用。方法:采用紫外分光光度法在346 nm处测定吸光度,计算黄连总生物碱含量,以黄连总生物碱的累积释药率为指标,在单因素试验考察基础上,采用星点设计-效应面法对聚氧乙烯用量、致孔剂聚乙二醇400用量和包衣增重进行考察。结果:最佳处方组成为黄连提取物75 mg,葛根提取物75 mg,氯化钠72 mg,聚氧乙烯78 mg,微晶纤维素15 mg,十二烷基硫酸钠9 mg;包衣液中乙酸纤维素、聚乙二醇400及邻苯二甲酸二丁酯的质量浓度分别为30,82,9 g·L^(-1),包衣增重8.2%;12 h内累计释放率达81.9%。结论:制备的微孔渗透泵片释放曲线符合要求,零级方程拟合度达0.990 9,优选的处方工艺稳定可行,可推广于复方葛黄微孔渗透泵片的工业化生产。

Objective： To optimize composition of compound Gehuang microporous osmotic pump tablets for providing a research model of microporous osmotic pump tablets of Chinese medicine effective components.Method： The content of total alkaloids in Coptidis Rhizoma was determined by ultraviolet spectrophotometry at346 nm. Taking accumulative release rate of total alkaloids in Coptidis Rhizoma as index,based on single factor tests, central composite design-response surface methodology was adopted to optimize prescription with polyoxyethylene content and polyethylene glycol 400 content and coating weight as factors. Result： The best prescription were： Coptidis Rhizoma extract of 75 mg,Puerariae Lobatae Radix extract of 75 mg,Na Cl of 72 mg,polyoxyethylene of 78 mg, microcrystalline cellulose of 15 mg, sodium dodecyl sulfate of 9 mg. In coating solution,concentrations of cellulose acetate,polyethylene glycol and dibutyl phthalate were 30,82,9 g·L^-1,coating weight was 8. 2%. Accumulative release rate in 12 h of total alkaloids was 81. 9%. Conclusion： Release profile of compound Gehuang microporous osmotic pump tablets meets requirements,its zero order equation fitting degree reaches 0. 990 9. This optimized preparation processes is stable and reasonable.