溴吡斯的明口腔崩解片的研制及质量控制

Preparation and Quality Control of Pyridostigmine Bromide Orally Disintegrating Tablet

目的制备口感良好的溴吡斯的明口腔崩解片,并优化处方。方法采用溶剂蒸发-沉积法制备固体分散体掩盖药物苦味,以崩解时间为指标,采用星点设计-效应面法优化处方。结果制备的口腔崩解片表面完整光洁,口感良好,能在30s内崩解完全。在水中0.5min内的药物溶出率约为8.5%,释药量约为2.5mg,低于苦味阈值(约3mg);在0.1mol/L盐酸介质中,2min累积溶出率大于95%。结论制备的口腔崩解片处方合理,工艺可行,方便患者服用。

Objective To prepare orally disintegrating tablets containing pyridostigmine bromide and optimize formulations.Methods Solid dispersion was prepared using solvent evaporation-deposition method.The formulation was optimized by central composite design-response surface methodology（RSM plus CCD） with disintegration time as a reference parameter.Results The orally disintegrating tablets showed integrity and were smooth with desirable taste and feel in mouth.The disintegration time was less than 30 s.The cumulative drug dissolution was around 8.5%（around 2.5 mg which was less than bitterness threshold of pyridostigmine bromide of 3 mg） within 5 min in water while the cumulative drug dissolution was higher than 95% within 2 min in 0.1 N HCl.Conclusion The orally disintegrating tablets are reasonable in formulation,feasible in technology and patient-friendly.