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目的:制备泊洛沙姆温度敏感原位凝胶,考察地塞米松磷酸钠(DSP)在其中的释放行为以及影响释放的因素。方法:以PluronicF127和F68为材料,DSP为模型药物制备温度敏感原位凝胶并测定胶凝温度。采用无膜溶出法和HPLC法测定DSP的释放行为;考察释放介质的接触面积、体积、pH值及振荡频率对DSP释放的影响。测定凝胶的溶蚀行为及其对药物释放的影响。结果:胶凝温度随F127浓度增大而升高,释放介质的接触面积、体积、振荡频率对药物的释放速率有显著影响,释放介质的pH对药物释放速率无显著影响。DSP的释放和凝胶的溶蚀遵循零级动力学方程,释放量随溶蚀量增加而增加,二者间存在线性关系。结论:DSP温度敏感原位凝胶的缓释效果良好,凝胶溶蚀速率、凝胶与释放介质的接触面积是控制药物释放的主要因素。
OBJECTIVE: To prepare poloxamer temperature-sensitive in situ gels and investigate the release behavior of dexamethasone sodium phosphate (DSP) and the factors affecting the release. Methods: Pluronic F127 and F68 were used as materials. DSP was used as model drug to prepare temperature-sensitive in-situ gels and gelation temperature was measured. The release behavior of DSP was determined by membrane-free dissolution method and HPLC method. The effects of contact area, volume, pH and oscillation frequency on release of DSP were investigated. The dissolution behavior of the gel and its effect on drug release were determined. Results: The gelation temperature increased with the increase of F127 concentration. The contact area, volume and oscillation frequency of release medium had a significant effect on the drug release rate. The release of the medium had no significant effect on the drug release rate. The release of DSP and the dissolution of the gel follow the zero-order kinetic equation, and the amount of release increases with the increase of the amount of dissolution. There is a linear relationship between the two. Conclusion: The sustained-release effect of DSP temperature-sensitive in situ gels is good. The dissolution rate of gels and the contact area between gels and release media are the main factors that control drug release.