对乙酰氨基酚配伍腺苷蛋氨酸复方片剂的制备及质量评价

Preparation and Quality Evaluation of Acetaminophen Combined with S-Adenosy-L-Methionine Tablets

目的:确定对乙酰氨基酚(APAP)配伍腺苷蛋氨酸(SAMe)复方制剂的制备工艺并进行质量标准研究。方法:通过正交实验优选辅料及其用量,以溶出度、外观性状、硬度及脆碎度等指标,进行质量评价,筛选得到复方制剂的最佳处方。结果:最佳处方选定粘合剂聚乙烯吡咯烷酮的用量为7%,填充剂微晶纤维素与乳糖总用量为11%,质量比例为2.5∶1,崩解剂交联聚乙烯吡咯烷酮(PVP-K30)用量为5%。原料药与辅料过100目筛(筛孔径0.15 mm)备用,按照用量要求将主药与辅料均匀混合,加入5%PVP-K30乙醇溶液制软材(握之成团,触之即散),20目筛(筛孔径0.85 mm)制粒,50℃鼓风干燥30 min后,20目筛(筛孔径0.85 mm)整粒,等量递加润滑剂混匀,压片。制备的片剂外观性状,片重差异,硬度及脆碎度等指标符合《中国药典》的相关规定。结论:对乙酰氨基酚复方片剂制备工艺稳定可行,质量稳定可控,按照最优处方和工艺制备片剂进行质量评价,各项考察指标均符合拟定的质量标准。

Objective:To determine the preparation process of acetaminophen(APAP)combined with S-adenosy-L-methionine(SAMe)compound formulation and conduct quality standard research.Method:By optimizing the excipients and their dosage through orthogonal experiments,quality evaluation was conducted based on indicators such as dissolution,appearance,hardness,and fragility,and the optimal formula for the compound formulation was selected.Result:The optimal prescription was selected with a dosage of 7%for the adhesive polyvinylpyrrolidone,11%for the total dosage of microcrystalline cellulose and lactose as the filler,and a ratio of 2.5∶1.The dosage of the disintegrating agent cross-linked polyvinylpyrrolidone(PVP-K30)was 5%.The raw material and excipients are sieved through a 100 mesh sieve for later use.The main drug and excipients are evenly mixed according to the dosage requirements,and a 5%PVP-K30 ethanol solution is added to prepare a soft material(hold it into a ball and disperse when touched).The 20 mesh sieve is used for granulation,and after drying at 50℃ for 30 min,the 20 mesh sieve is used for granulation.An equal amount of lubricant is added to mix well,and the tablet is pressed.The appearance,weight difference,hardness,and fragility of the prepared tablets comply with the relevant provisions of the Chinese Pharmacopoeia.Conclusion:The preparation process of acetaminophen compound tablets is stable and feasible,and the quality is stable and controllable.The tablets were prepared according to the optimal prescription and process for quality evaluation,and all inspection indicators meet the proposed quality standards.