胃幽康胃漂浮片的制备及其体外释药特性研究

发布时间：2019-01-02 13:54

【摘要】：目的:制备胃幽康胃漂浮片并考察其体外释药特性。方法:以羟丙基甲基纤维素K15M(HPMC-K15M,骨架材料)、十八醇(低密度助漂剂)、碳酸氢钠(发泡剂)、聚乙烯基吡咯烷酮K30(PVP-K30,释放调节剂)、硬脂酸镁(润滑剂)为辅料,采用全粉末压片法制备胃幽康胃漂浮片。以小檗碱2、4、8 h的累积释放度(Y2 h、Y4 h、Y8 h)为指标,起飘时间(T1)和持续漂浮时间(T2)为辅助指标,采用正交试验对HPMC-K15M、十八醇、PVP-K30用量进行优选,并进行验证。以释放模型拟合法、Peppas方程拟合法考察所制制剂中主要臣药黄连、延胡索、黄芩和甘草中有效成分小檗碱、延胡索乙素、黄芩苷和甘草酸的释药规律;并以相似因子(f2)法考察4种有效成分的释药相似性。结果:最优处方为HPMC-K15M 40 g、十八醇14 g、PVP-K30 2 g(200片量)。所制制剂中小檗碱Y2 h、Y4 h、Y8 h分别为31.94%、55.88%、93.34%(RSD为1.2%、1.5%、1.5%,n=3),T1、T2分别在1 min和13 h左右;4种成分释药特性均符合Higuchi模型;均为扩散协同骨架溶蚀作用;f2均大于80,各成分均衡释放。结论:成功制得起飘时间快、持飘时间长,且具有缓释和多成分均衡释药特性的胃幽康胃漂浮片。
[Abstract]:Objective: to prepare Weiyou Kang Wei floating tablet and to investigate its release characteristics in vitro. Methods: hydroxypropyl methyl cellulose K15M (HPMC-K15M, skeleton material), octadecanol (low density bleaching aid), sodium bicarbonate (foaming agent) and polyvinylpyrrolidone K30 (PVP-K30, release regulator) were used. Magnesium stearate (lubricant) was used to prepare Weiyou Kang gastric floating tablets by the method of full powder pressing. The cumulative release rate of berberine (Y2HX, Y4hT8 h), the rising and floating time (T1) and the persistent floating time (T2) of berberine for 8 h were used to optimize the dosage of HPMC-K15M, octadecanol and PVP-K30 by orthogonal test. And verify it. The release patterns of berberine, tetrahydropalmatine, baicalin and glycyrrhizic acid in Coptis chinensis, Rhizoma Corydalis, Radix Scutellariae and Glycyrrhiza uralensis were investigated by the method of release model and Peppas equation. Similarity factor (f 2) method was used to study the drug release similarity of four active components. Results: the optimal prescription was HPMC-K15M 40 g and octadecanol 14 g PVP-K 302 g (200 tablets). The content of berberine Y _ 2H _ 4H _ 4H _ (8 h) was 31.94% and 93.34% (RSD = 1.2 ~ 1.5), T _ (1) T _ 2 was about 1 min and 13 h, respectively. The drug release characteristics of the four components were all in accordance with Higuchi model, all of them were diffusion synergistic cytoskeleton dissolution, f2 was more than 80, and each component was released equably. Conclusion: Weiyoukang Weiyukang floating tablets with the characteristics of slow release and multi-component equilibrium release can be successfully prepared with fast floating time and long floating time.
【作者单位】：溧阳市中医院药剂科;南京中医药大学药学院;
【基金】：常州市卫生局科技项目(No.WZ201228)
【分类号】：R943

【参考文献】