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 Sustained-release Tablets

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^-3 Pa·s。处方A,B,C的黏度分别为105×10^-3,265×10^-3,540×10^-3 Pa·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^-3 Pa·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。

Abstract:

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^-3,435×10^-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 different filler,viscosity and release are negatively correlated.