地塞米松磷酸钠温度敏感原位凝胶释药与溶蚀行为的影响因素考察  

The release and dissolution of dexamethasone sodium phosphate from thermosensitive in situ gel in vitro

作　　者：李欣宇[1] 肖磊[2] 朱照静[3] 

机构地区：[1]重庆医科大学附属第一医院药剂科,重庆400016 [2]重庆市妇幼保健院,重庆400020 [3]重庆医药高等专科学校,重庆400030

出　　处：《中国医院药学杂志》2010年第2期142-146,共5页Chinese Journal of Hospital Pharmacy

摘　　要：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PluronicF127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 thermosensitive in situ gel, and investigate drug release behavior of dexam- ethasone sodium phosphate as well as its influencing factors. METHODS Pluronie F127 and F68 were used to prepare thermo- sensitive in situ gel at 4 ℃ and gelation temperature was measured. Membrane-free method and HPLC were used to determine DSP release, and the impact of gel area contacting with release medium, volume and pH value of release medium as well as oscil- lation frequency on drug release were investigated. Gel dissolving behavior and its influence on drug release were studied. RE- SULTS Gelation temperature of the DSP poloxamer gel was heightening with increasing of F127 concentration. Accumulative drug release was influenced by gel area contacting with release medium, the volume of release medium and oscillation 5 requen- cy. But the pH value of the release medium had almost no impact on the drug release. DSP released and gel dissolution followed zero-order kinetics and they were linear correlative. CONCLUSION Sustained release of drug from poloxamer thermosensitive in situ gel is desirable, and drug released was mainly influenced by gel erosion rate as well as contacting area of the gel with re- lease medium.

关 键 词：泊洛沙姆 温度敏感原位凝胶 地塞米松磷酸钠 零级动力学 

分 类 号：R934.4[医药卫生—生药学]