香连胃漂浮片的制备及体外释放研究

目的制备香连胃漂浮片并考察其体外释放性能。方法以羟丙基甲基纤维素K4M(hydroxypropyl methylcellulose K4M,HPMC-K4M)、十六醇、碳酸氢钠(NaHCO3)、乳糖、聚维酮K30(povidone K30,PVP-K30)、硬脂酸镁为辅料,采用粉末压片法制备香连胃漂浮片;以盐酸小檗碱的累积释放度为指标考察制剂的体外释药性能;采用正交试验对HPMC-K4M、十六醇、NaHCO3用量进行优选。通过数据拟合方程探讨制剂中盐酸小檗碱、木香烃内酯的释药机制。结果最优处方为香连复方提取物60.0 g、HPMC-K4M30.0 g、十六醇8.0 g、NaHCO38.0 g、乳糖8.0 g、PVP-K304.8 g、硬脂酸镁1.2 g(200片量)。指标成分盐酸小檗碱和木香烃内酯的体外释药特性均符合Riger Peppas模型,为扩散与骨架溶蚀协同作用。结论成功制得香连胃漂浮片,漂浮滞后时间短,持续漂浮时间长,且具有缓释特性。

Study on Preparation and in Vitro Release Behaviors of Xianglian Gastric Floating Tablets

Objective To prepare Xianglian gastric floating tablets and investigate the release behaviors in vitro.Methods Xianglian gastric floating tablets were prepared by full powder compression method using hydroxypropyl methylcellulose K4 M(HPMC-K4 M),hexadecanol,sodium bicarbonate(NaHCO3),lactose,povidone K30(PVP-K30),magnesium stearate as excipients;the accumulative release rate of berberine hydrochloride was used as evaluation index.The orthogonal test was used to optimize the dosage of HPMC-K4 M,hexadecanol and NaHCO3;Through the data fitting equation,the release mechanism of berberine hydrochloride and woody hydrocarbon lactone in the preparation was discussed.Results The optimized formulation was as follows:Xianglian compound extracts 60.0 g,HPMC-K4 M 30.0 g,hexadecanol 8.0 g,NaHCO38.0 g,lactose 8.0 g,PVP-K304.8 g,magnesium stearate 1.2 g(dosage of 200 tablets).The drug release of berberine hydrochloride and costunolide fitted Riger Peppas models,and were synergistic action of diffusion and matrix erode.Conclusion Xianglian gastric floating tablets are prepared successfully,showing fast onset,long floating and sustained-release.