长春西汀海藻酸钠骨架片体外释药影响因素研究

Studies on the influencing factors in the vinpocetine release in vitro from sodium alginate matrices

目的以海藻酸钠为骨架材料 ,制备长春西汀控释骨架片 ,对影响其体外释放的多种因素进行了考察。方法以海藻酸钠为亲水骨架材料 ,粉末直接压片制备长春西汀控释片 ,采用《中华人民共和国药典》2 0 0 0年版二部收载的溶出度测定方法Ⅱ法 (桨法 ) ,测定药物在不同条件下的体外释放度 ,考察海藻酸钠用量及黏度 ,枸橼酸用量 ,释放介质离子强度和pH值对药物体外释放行为的影响。结果与结论海藻酸钠用量及黏度 ,枸橼酸用量 ,释放介质离子强度和pH值均对药物体外释放行为有显著影响。值得注意的是 ,通过调节处方中枸橼酸用量可以使释药行为达零级 ,这为制备长春西汀控释片提供指导 ,有进一步开发的价值。

Objective To prepere vinpocetine sustained release matrix tablets by sodium alginate as the hydrophilic polymer and investigate of the influencing factors in drug release from matrices.Methods With sodium alginate as the matrix,the tablets were prepared by the direct compression method.The dissolution of vinpocetine from prepared tablet formulations was performed according to the Chinese Pharmacopoeia(2000) Dissolution Apparatus Ⅱ(the paddle method).The investigation of the influencing factors,such as the content and viscosity of sodium alginate,the amount of citric acid,ionic strength and pH value of dissolution media,on the drug release behavior was performed by measuring the drug cumulative released percent.Results and Conclusions The results showed that the content and viscosity of sodium alginate ,the amount of citric acid,ionic strength and pH value of dissolution media all have significant effect on the drug release behavior.Interestingly,the zero-order release of the drug can be produced by regulating the amount of citric acid added to the sodium alginate,which can provide valuable information and be useful for further research on the controlled-release vinpocetine matrices.