影响κ-卡拉胶/黄原胶骨架片体外释药因素的研究

Study on Influencing Factors of in Vitro Release of Aspirin κ-Carrageenan/Xanthan Gum Matrix Tablet

目的研究κ-卡拉胶/黄原胶骨架片的体外释药因素,探讨其释药特性。方法以κ-卡拉胶和黄原胶复配为骨架材料,阿司匹林为模型药物,湿法制粒压片制备骨架片,测定骨架片在不同pH值、离子强度的释放介质和不同搅拌方式、转速下的体外释放度及溶蚀度,分别采用Peppas方程和零级方程对骨架片释放度和溶蚀度数据进行拟合。结果骨架片在pH6.8磷酸盐缓冲液中药物释放最快,纯化水中次之,0.1mol·L-1盐酸液中最慢;药物释放随介质离子强度增加而减慢;药物释放随搅拌转速增加而加快;骨架片药物释放机制为扩散和溶蚀释放协同的作用。结论κ-卡拉胶与黄原胶复配作为骨架材料可延缓骨架片中药物的释放。

Objective To study the in vitro release of aspirin κ-carrageenan/xanthan gum matrix tablet and approach the release features. Methods The hydrophilic matrix tablets containing aspirin as a model drug were prepared by the wet granulation technique with κ-carrageenan and xanthan gum as the matrix materials. The effects of pH value, ionic strength of dissolution media, mixing style and rotation speed on drug release and tablet erosion were studied by in vitro dissolution test. The date of tablet erosion and drug release were confirmed by the zero order equation and Peppas equation, respectively. Results Among the rate of drug release in different dissolution media, pH6.8 PBS was the fastest, distilled water was the second, 0.1 mol·L^-1HCl was the slowest. The drug release increased with increasing the ionic strength of dissolution media or with increasing the rotation speeds. The mechanism of drug release was a synergistic effect of diffusion and erosion. Conclusion The drug can be released slowly from the matrix tablet containing κ-carrageenan and xanthan gum as the matrix materials.