地塞米松磷酸钠温敏凝胶的制备  

Design and preparation of thermosensitive in situ gel of dexamethasone sodium phosphate

作　　者：陈钢[1] 胡平[2] 李晓芳[1] 

机构地区：[1]广东药学院药剂学教研室,广东广州510006 [2]香港浸会大学中医药学院

出　　处：《广东药学院学报》2007年第5期518-521,共4页Academic Journal of Guangdong College of Pharmacy

基　　金：广东省医学科研基金(B2007090);广东药学院博士科研启动基金(43540133)

摘　　要：目的设计和制备地塞米松磷酸钠(dexamethasone sodium phosphate,DSP)温度敏感原位凝胶,为其局部应用奠定基础。方法优选处方,考察各种附加剂对胶凝温度的影响,调节基质浓度以得到适宜的胶凝温度。采用差示扫描量热法(DSC)考察胶凝过程的热效应。结果确定以泊洛沙姆407为基质制备DSP温敏凝胶,得到优化处方:质量分数分别为14.1%的泊洛沙姆407,0.2%的透明质酸,10%的甘油,15%的丙二醇和2%的DSP。DSC测得其胶凝温度为26℃,而且胶凝过程热效应极低,焓变值为0.032 J.g-1.K-1。结论制备的DSP温敏凝胶在室温下为流体,在体温条件下可发生相变成为凝胶,值得进一步开发研究。Objective To design and prepare dexamethasone sodium phosphate （DSP）-loaded thermosensitive in situ gel, and provide scientific information for clinical application. Methods Selection of different materials and their influence on gelation temperature （GT）, were evaluated. Different GT could be obtained by adjusting the concentration of poloxamer 407. Heating curve of gelation process was investigated by employing differential scanning calorimetery （ DSC ）. Results Poloxamer 407 was adopted as gel base to prepare DSP gel. The optimized formulation was composed of 14.1% poloxamer 407,0.2% hyaluronic acid, 10% glycerin, 15% propylene glycol and 2% DSP. GT of the formulation was 26℃ by DSC. And the DSC result displayed that delta Cp ＊ was 0.032 J · g^-1·K^-1 ,which indicated packing of micelles and micelle entanglements may be possible mechanisms of poloxamer solution gelation with increased temperature. Conclusion The optimized formulation is free flowing liquid below room temperature and converted to a gel under the physiological condition, which has potential benefits of therapy.

关 键 词：温度敏感原位凝胶 地塞米松磷酸钠 泊洛沙姆407 

分 类 号：R943[医药卫生—药剂学]