Compritol■ 888 ATO 对双氯芬酸钠的缓释作用

The sustained release of diclofenac sodium by Compritol■ 888 ATO

以Compritol■ 888 ATO(山嵛酸甘油酯)为骨架材料制备双氯芬酸钠缓释片并对其体外释放进行评价,得到与市售产品Voltaren-SR体外释放一致的自制片。通过差示扫描量热(DSC)、傅里叶红外变换光谱(FT-IR)和粉末X线衍射(PXRD)等手段探究Compritol■ 888 ATO与双氯芬酸钠的二元体系,采用热熔挤出联合粉末直压的工艺制备双氯芬酸钠缓释片并测定体外释放。结果发现:Compritol■ 888 ATO与双氯芬酸钠二元体系表现为偏晶行为,且偏晶体系的形成对药物释放影响不大,Compritol■ 888 ATO用量越多,药物释放越慢。结论:Compritol■ 888 ATO的疏水性对药物释放起着更为显著的作用,骨架材料的用量与药物释放速率呈负相关性。

The sustained release tablets of diclofenac sodium was prepared with Compritol■888 ATO as a lipid matrix and the in-vitro dissolution characteristics were studied.The binary systems of Compritol■888 ATO and diclofenac sodium was investigated by differential scanning calorimetry(DSC),Fourier transform infrared spectroscopy(FT-IR)and powder X-ray diffraction(PXRD).The sustained release tablet of diclofenac sodium was prepared by hot melt extrusion and then powder direction.The results showed that the binary systems of Compritol■888 ATO and diclofenac sodium behave monotectic,and the monotectics has little effect on drug release.The more the Compritol■888 ATO is used,the slower the drug release.In conclusion,the hydrophobicity of Compritol■888 ATO plays a more significant role in drug release,and the amount of matrix is negatively correlated with drug release rate.