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纸质出版日期:2015
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龚琼, 朱盛山, 李碧云, 等. 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[J]. 中国实验方剂学杂志, 2015,21(5):11-15.
GONG Qiong, ZHU Sheng-shan, LI Bi-yun, et al. Effects of Compatibility of Improved Accessory I and Others on Release of Chuanping Extract Sustained-release Tablets[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(5): 11-15.
龚琼, 朱盛山, 李碧云, 等. 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[J]. 中国实验方剂学杂志, 2015,21(5):11-15. DOI: 10.13422/j.cnki.syfjx.2015050011.
GONG Qiong, ZHU Sheng-shan, LI Bi-yun, et al. Effects of Compatibility of Improved Accessory I and Others on Release of Chuanping Extract Sustained-release Tablets[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(5): 11-15. DOI: 10.13422/j.cnki.syfjx.2015050011.
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。
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.
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