氯霉素温敏型眼用原位凝胶的研制  

Preparation of a poloxamers based in situ thermosensitive gel containing chloramphenicol for ophthalmic use

作　　者：孔志峰[1,2] 郝吉福[2] 郭丰广[2] 孝建华[2] 王建筑[2] 张雯[2] 

机构地区：[1]山东大学药学院,山东济南250012 [2]泰山医学院药学院,山东泰安271000

出　　处：《中国生化药物杂志》2010年第3期185-189,共5页Chinese Journal of Biochemical Pharmaceutics

摘　　要：目的制备氯霉素泊洛沙姆眼用原位温敏型凝胶并建立其质量控制方法。方法以泊洛沙姆P407和P188为温敏材料,通过测定溶液-凝胶相转变温度优化处方;采用紫外分光光度法测定氯霉素含量。结果氯霉素温敏型原位凝胶的胶凝温度随P407浓度增大而降低,随P188浓度增加先升高后降低,模拟泪液的稀释可使胶凝温度升高,建立了泪液稀释后相变温度与泊洛沙姆浓度的拟合方程,经Design-Expert软件优化出的氯霉素温敏型原位凝胶最佳处方为25%P407和4.19%P188;优化处方在29.5℃时为自由流动的液体,泪液稀释后在34.6℃能够发生相变形成凝胶。结论该眼用温敏凝胶符合眼部应用要求,体现出良好的应用前景。Purpose To prepare a poloxamers based in situ thermosensitive gel containing chloram- phenicol for ophthalmic use and to establish its quality control method. Methods The in situ thermosensitire gel of chloramphenicol was prepared with poloxamer 407 （P407） and poloxamer 188 （P188） as ther-mosensitive material,and the formulation was optimized by determining solution-gelation conversion temperature. The content of ehloramphenieol was determined by ultraviolet spectrophotometry. Results The gelation temperature of in situ thermosensitive gel of chloramphenicol formulations was lowered as the P407 concentration increased. As the P188 concentration increased gradually the gelation temperature initially increased to maximum, and then decreased. The gelation temperature all increased after simulated tear fluid （STF） dilution. The fitted equation was established for the gelation temperature with the concentration of poloxamer solutions after being diluted by STF. An optimized formulation by Design-Expert soft was freely flowing liquid at 29.5 ℃ and it converts to a firm gel at 34.6 ℃ after STF diluted. Con- clusion In situ thermosensitive gel satisfied the requirement for ophthalmic application and showed a great potential in ophthalmic application.

关 键 词：氯霉素 泊洛沙姆 原位温敏凝胶 制备 

分 类 号：R944.9[医药卫生—药剂学]