星点设计-效应面法对左氧氟沙星泊洛沙姆407/188眼用凝胶的制备工艺优化  

Optimization of preparation process of levofloxacin poloxamer 407/188 ophthalmic gel by central composite design-response surface methodology

作　　者：黄骞[1] 张培雯 代晶[2] 樊莲莲[1] 苏文成[1] 李林峻 曹飞 HUANG Qian;ZHANG Peiwen;DAI Jing;FAN Lianian;SU Wencheng;LI Linjun;CAO Fei(PhaseⅠClinical Trial Center,People’s Hospital of Deyang City,Sichuan,Deyang 618000,China;ChengduMedical College,Sichuan,Chengdu 610500,China)

机构地区：[1]四川省德阳市人民医院Ⅰ期临床研究中心,四川德阳618000 [2]成都医学院,四川成都610500

出　　处：《中国医药科学》2023年第5期94-98,共5页China Medicine And Pharmacy

基　　金：四川省德阳重点科学技术研究项目(2016SZ034)。

摘　　要：目的 应用星点设计-效应面法研制左氧氟沙星温度敏感型眼用凝胶,优化处方工艺,以期获得可用于白内障术后感染的眼用制剂。方法 选择泊洛沙姆407(P407)和泊洛沙姆188(P188)作为凝胶温敏材料,以凝胶温度为响应值,通过星点设计-效应面法进行模型拟合;采用无膜溶出模型考察药物的体外溶蚀行为与释放度。结果 模型拟合获得优化处方:P407浓度25.23%、P188浓度1.89%,胶凝温度的实测值与预测值相对偏差<5%。泪液溶蚀是影响药物释放的主要因素。结论 星点设计-效应面法得到的左氧氟沙星眼用温敏型凝胶处方精密度较高,可作进一步推广应用研究。Objective To prepare levofloxacin thermosensitive ophthalmic gel by central composite design-response surface methodology(CCD-RSM),and optimize the prescription and process,so as to obtain ophthalmic preparation that can be used for cataract postoperative infection.Methods Poloxamer 407(P407)and poloxamer 188(P188)were selected as the thermosensitive materials of gel,and the gel temperature was taken as the response value for model fitting using CCD-RSM.The in vitro dissolution behavior and release rate of drug were investigated using a membrane-free dissolution model.Results The optimal prescription was obtained by model fitting:the concentrations of P407 and P188 were 25.23%and 1.89%,respectively.The relative deviation of the measured value and predicted value of gel temperature was less than 5%.Tear dissolution is the main factor affecting drug release.Conclusion The precision of levofloxacin thermosensitive ophthalmic gel prescription obtained by CCD-RSM is high,so this prescription can be further popularized and applied.

关 键 词：左氧氟沙星 泊洛沙姆 原位凝胶 星点设计 

分 类 号：R944[医药卫生—药剂学]