生物黏附性神衰果素缓释片体外释放度及组织黏附力研究

Studies on Release of Helicid Bioadhesive Sustain-Release Tablet and Determination of Adhesive Force in Vitro

目的研究生物黏附性神衰果素缓释片的体外释放度及释药规律,并测定其体外黏附力。方法采用转篮法,以900mL水为释放介质,转速100 r.min-1测定其累积释放度,用多种数学模型对释放曲线进行拟合,根据各模型拟合的AIC值、计算值与真实值的绝对误差以及相对误差确定最优模型。以自制黏附力测定装置测定了生物黏附性缓释片的大鼠离体胃、小肠组织的黏附力。结果缓释片以Higuchi,Ritger-Peppas模型拟合皆佳,在大鼠离体胃、小肠组织的黏附力分别为6.1,13.2 kPa。结论生物黏附性神衰果素缓释片的释药参数n=0.619 9,药物的释放是通过扩散和凝胶骨架溶蚀两种机制协同作用的结果;在大鼠离体胃、小肠组织均具有黏附作用,且在小肠组织的黏附作用强于胃。

OBJECTIVE To study the drug release mechanism of helicid（HD） bioadhesive sustained-release tablet and to determine the adhesive force in vitro. METHODS Using rotating basket method, the accumulative drug release was determined with water as releasing mediums at the speed of 100 r· min^- 1 ; several mathematic models were used to simulate the release curve. The biggest absolute error, the biggest relative error and AIC were used as comprehensive indices to select the best optimum model. A building apparatus was used to determine the adhesive force at rat stomach and small intestine in vitro. RESULTS The Higuchi and Ritger-Peppas models were chosen as the optimum model for HD bioadhesive sustained-release tablet. The adhesive forces were 6.1 and 13.2 kPa in rat stomach and small intestine respectively. CONCLUSION The releasing parameter of n is 0.619 9. The releasing action is the result of both diffusion and erosion mechanism. The HD bioadhesive sustained-release tablet is adhesive in stomach and small intestine and the adhesive force is stronger at small intestine than that in stomach.