氨酚氯雷伪麻缓释片的制备及其体外释放度的研究

目的研制亲水凝胶骨架型氨酚氯雷伪麻缓释片,并考察其体外释放度。方法采用湿法制粒工艺,以羟丙基甲基纤维素(HPMC)为缓释骨架材料,制备了氨酚氯雷伪麻缓释片。以对乙酰氨基酚的体外释放度为考察指标,通过正交试验筛选出最佳处方,并考察了原料药粒径、HPMC和碳酸氢钙的用量、颗粒水分和制片压力对缓释片中对乙酰氨基酚体外释放速率的影响。结果原料药粒径、HPMC用量、颗粒水分和制片压力对氨酚氯雷伪麻缓释片体外释放速率有明显的影响;碳酸钙用量对释放速率基本无影响。结论按优化处方制备的氨酚氯雷伪麻缓释片缓释效果明显,符合相关规定,可应用于工业化大生产。

Study on Preparation and in Vitro Release Behavior of Paracetamol, Loratadine and Pseudoephedrine Sulfate Sustained Release Tablets

Objective To investigate the preparation and to determine the dissolution behavior of the paracetamol,loratadine and pseudoephedrine sulfate sustained release tablets.Methods By using HPMC as sustained-release matrix material,paracetamol,loratadine and pseudoephedrine sulfate sustained release tablets were prepared by wet granulation.The optimum formulation was selected by studying on the release degree of paracetamol in vitro via orthogonal test.The factors affecting the release rate of paracetamol in vitro from matrix,including particle size of paracetamol,quantity of HPMC and Ca（HCO3）2,moisture in granules and tablets pressure were evaluated.Results The particle size of paracetamol,the quantity of HPMC,the moisture in granules and the tablets pressure were found to be the sole factors that affected the release rate of paracetamol.The quantity of Ca（HCO3）2 showed no significant effects on the release rate.Conclusion The paracetamol,loratadine and pseudoephedrine sulfate sustained release tablets prepared according to the optimized formulation show significant sustained release behavior,and comply with relevant requirement,can be applied to industrial production.