左羟丙哌嗪-β-环糊精包合物分散片的制备与评价

Preparation and evaluation of dispersible tablets containing levodropropizine-β-cyclodextrin inclusion complexes

目的:优选左羟丙哌嗪-β-环糊精包合物分散片的处方组成与制备工艺。方法:制备左羟丙哌嗪-β-环糊精包合物,并以此为中间体添加适宜的辅料制备分散片。以崩解时限、片剂外观等为评价指标,进行处方及制备工艺的全面考察优化。结果:分散片最优处方为:左羟丙哌嗪-β-环糊精包合物80.0%,L-HPC10.0%,MCC9.6%,硬脂酸镁0.4%。其崩解时间不超过60 s,5 min溶出可达85%以上。结论:该分散片处方设计简单合理,工艺稳定可行,符合《中国药典》2015年版的规定。

OBJECTIVE To screen the optimal formula and preparation process for dispersible tablets containing levodropropizine-β-cyclodextrin inclusion complexes.METHODS Levodropropizine-β-cyclodextrin inclusion complexes were prepared firstly and used as the intermediates, then dispersible tablets were developed with inclusion complexes mixed with some appropriate excipients. The prescription composition and preparation process were optimized and evaluated by using disintegration time and tablet appearance as indicators.RESULTS The optimal formulation was as follows：80.0% β-cyclodextrin inclusion complexes, 10.0% L-HPC, 9.6% MCC and 0.4% magnesium stearate. The disintegration time of dispersible tablets was no more than 60 s.Dissolution of levodropropizine from dispersible tablets at 5 min was ≥ 85%.CONCLUSION The dispersible tablets have simple, reasonable prescription and stable, feasible preparation process. It meets the requirements of the Chinese Pharmacopoeia （2015）.