改良辅料Ⅰ与其他辅料配伍对喘平提取物缓释片释放度的影响  

Effects of Compatibility of Improved Accessory Ⅰ and Others on Release of Chuanping Extract Sustainedrelease Tablets

作　　者：龚琼[1] 朱盛山[1] 李碧云[1] 钟晓雨[1] 田先地 吴思平[1] 钟娜娜[1] 蔡延渠[1] 

机构地区：[1]广东药学院中药开发研究所,广州510006

出　　处：《中国实验方剂学杂志》2015年第5期11-15,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81373981);广东省中医药局项目(20131252);广东省教育厅高校重点实验室滚动支持项目(2013CXZDA021)

摘　　要：目的:阐明改良辅料Ⅰ与其他辅料配伍后黏度变化对缓释制剂体外释放度的影响。方法:以喘平方提取物为模型药物,糊精为填充剂,与不同用量改良辅料Ⅰ(40%,45%,50%)配伍制备喘平缓释片(处方A,B,C);以最佳比例将改良辅料Ⅰ与不同填充剂[乳糖、糊精-糖粉(1∶1)、淀粉-糖粉(1∶1)、微晶纤维素]配伍制备喘平缓释片(处方D,E,F,G),采用HPLC测定喘平缓释片中盐酸麻黄碱、盐酸伪麻黄碱和东莨菪碱的释放度,利用相似因子法考察各成分间的均衡释放。结果:辅料Ⅰ扭矩<10%。改良辅料Ⅰ黏度218.3×10-3Pa·s。处方A,B,C的黏度分别为105×10-3,265×10-3,540×10-3Pa·s,缓释片基本释放完全时间分别为6,8,10 h;处方C溶完时间符合要求,10 h时盐酸麻黄碱、盐酸伪麻黄碱和东莨菪碱累计释放度分别为97.21%,96.79%,94.21%,成分间释放因子(f2)依次为75.08,71.42,61.88,均衡释放效果较好。处方D,E,F,G黏度分别为400×10-3,435×10-3,475×10-3,808.3×10-3Pa·s,缓释片基本释放完时间分别为8,>10,10,2 h;处方F溶完时间符合要求,10 h时3种成分释放度分别为98.40%,97.92%,97.99%,成分间f2分别为74.78,74.65,74.70,均衡释放效果较好。结论:改良辅料Ⅰ能满足均衡释放的要求,不同辅料的配伍会影响喘平缓释片的体外释放行为。不同用量改良辅料Ⅰ与糊精配伍时,黏度与释放度呈正相关;与不同填充剂配伍时,黏度与释放度未呈正相关关系。Objective： To illuminate effects of viscosity on release of sustained-release preparations after compatibility of homemade slow-release improved accessory I and others. Method： With Chuanping extract as a model drug and dextrin as a filler, different sustained-release tablets （prescription A, B, C） with different dosage of modified accessory I （40%, 45% and 50% ） were prepared; sustained-release tablets （prescription D, E, F, G） with the best proportion of modified accessory I and other accessories [ lactose, dextin-sugar （1： 1）, starch-sugar （1：1）, microcrystalline cellulose] were prepared. HPLC was adopted to measure release rates of ephedrine, pseudoephedrine and scopolamine in Chuanping sustained-release tablets, balanced release of different component were determined by similarity factor method. Result： Torque of accessory I was less than 10% , viscosity of improved accessory I was 218.3×10^-3 Pa·s. Viscosities of prescriptions A, B, C were 105×10^-3, 265×10^-3, 540×10^-3 Pa·s; release finished at 6, 8, 10, respectively. Finished-release time of prescription C met demand, release of ephedrine, pseudoephedrine and scopolamine at 10 h were 97.21%,96.79% , 94. 21% , releasing factor （f2） values were 75.08, 71.42, 61.88, balanced release rates were obtained well. Viscosities of prescription D, E, F, G were 400×10^-3, 455×10^-3, 475×10^-3 , 808.3×10^-3 Pa·s, finished-release times were 8, 〉 10, 10, 2 h, respectively. Prescription F met requirement, release degrees of ephedrine, pseudoephedrine and scopolamine at 10 h were 98.40% , 97.92% , 97.99% , f2 values were 74.78, 74.65, 74.70, balanced release rates were obtained well. Conclusion： Improved accessory I can meet demand of balanced release well. Compatibility of different accessories can affect balanced release of Chuanping sustained-release tablets. When different dosages of improved accessory I combine with dextrin, viscosity and release are positively correlated; when improved accessory I is compatible with

关 键 词：改良辅料Ⅰ 黏度 体外释放度 均衡释放 填充剂 

分 类 号：R283.6[医药卫生—中药学] R942[医药卫生—中医学]