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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 clarify the influence of the viscosity change of modified adjuvant (Ⅰ) and other excipients on the in vitro release of sustained release preparation. Methods: Chuan square extract was used as model drug and dextrin was used as filler to prepare astragalus sustained release tablets (prescriptions A, B and C) with different dosage of modified excipients Ⅰ (40%, 45%, 50%). The optimal ratio of modified excipients Ⅰ with different filler [lactose, dextrin - sugar powder (1: 1), starch - sugar powder (1: 1) , E, F, G). The release of ephedrine hydrochloride, pseudoephedrine hydrochloride and scopolamine hydrochloride were determined by HPLC. The equilibrium release of each component was investigated by the similarity factor method. Results: Accessories Ⅰ torque <10%. Improved accessories Ⅰ viscosity 218.3 × 10-3Pa · s. The viscosity of prescription A, B and C were 105 × 10-3, 265 × 10-3 and 540 × 10-3Pa · s, respectively, and the release time of sustained release tablets was 6, 8 and 10 h respectively. The dissolution time of prescription C was satisfactory, The cumulative release rates of ephedrine hydrochloride, pseudoephedrine hydrochloride and scopolamine hydrochloride for 10 h were 97.21%, 96.79% and 94.21%, respectively, and the release factors (f2) were 75.08, 71.42 and 61.88 among the components, respectively. The viscosities of prescription D, E, F and G were 400 × 10-3, 435 × 10-3, 475 × 10-3 and 808.3 × 10-3Pa · s, respectively. The release time of sustained release tablets were 8, 10, 10, The dissolution time of prescription F meets the requirements. The release rates of the three components at 10 h were 98.40%, 97.92% and 97.99% respectively. The f2 contents of the components were 74.78, 74.65 and 74.70 respectively, and the balanced release was better. Conclusion: The modified excipient Ⅰ can meet the requirements of balanced release. The compatibility of different excipients will affect the release behavior of sustained release tablets in vitro. The results showed that there was a positive correlation between the viscosity and the release rate when the different dosage of modified excipients (Ⅰ) and dextrin were compatibilized. There was no positive correlation between the viscosity and the release degree when they were mixed with different fillers.