5-氟尿嘧啶液体栓的制备及体外释放研究  

Research of Preparation and in vitro Release of 5-fluorojuracil Liquid Suppositories

作　　者：陈凯 郭文健[2] 张岭[2] 胡霞[3] 孙璐 陈有权 林宁 张莉[2] CHEN Kai;GUO Wenjian;ZHANG Ling;HU Xia;SUN Lu;CHEN Youquan;LIN Ning;ZHANG Li(College of Pharmacy, Hubei University of Chinese Medicine, Wuhan 430065;Department of Pharmacy, Logistics University of Chinese People＇ s Armed Police Force, Tianjin 300162;Department of Pharmacy, Hubei Municipal Corps Hospital of Chinese People＇ s Armed Police Force, Wuhan 430060;75222 Force of The Chinese People＇ s Liberation Army, Shantou 515000)

机构地区：[1]湖北中医药大学药学院 [2]武警后勤学院药剂学教研室 [3]武警湖北总队医院药剂科 [4]中国人民解放军75222部队88分队

出　　处：《湖北中医药大学学报》2018年第1期49-52,共4页Journal of Hubei University of Chinese Medicine

基　　金：湖北省教育厅科学技术研究项目(项目编号:D20101801);湖北省自然科学基金项目(项目编号:2012FFB03705)

摘　　要：目的筛选5-氟尿嘧啶液体栓处方并进行体外释放研究。方法以泊洛沙姆407为凝胶材料,海藻酸钠和PEG4000为黏度调节剂,制备5-氟尿嘧啶液体栓,考察5-氟尿嘧啶用量、凝胶材料比例以及黏度调节剂对胶凝温度的影响,采用紫外法考察其体外释放规律。结果所制2%5-氟尿嘧啶液体栓的胶凝点在(36.2±0.33)℃,体外释放结果显示5-氟尿嘧啶液体栓在240min累积释放率为94.50%。结论将5-氟尿嘧啶制成液体栓能加快药物的溶出速度,延长药效时间,通过调整液体栓材料比例以及黏度调节剂可制得性状优良的液体栓剂。Objective To prepare the liquid suppository of S-fluorojuracil and investigate the in vitro drug release behavior of 5-fluorojuracil and choose the optimal formulation. Methods The thermosensitive gel was prepared with Poloxamer 407 as the gel material, sodium alginate as thickening agent. The effects of 5-fluorojuracil dosages, gel matrix ratios and viscosity regulator on gelatinization temperature were investigated and the in vitro drug release was determined by UV Spectrophotometry. Results The gelatination temperature for liquid suppository of 5-fluorojuracil was 36.2 ± 0.33 ℃.The in vitro accumulate release ratio of 5-fluorojuracil in the liquid suppository was 94.50% after 240 min. Conclusion The preparation of S-fluorojuracil into liquid suppository could accelerate drug dissolution rate and prolong the efficacy time. Liquid suppository with qualified char- acteristics could be prepared through adjusting the proportion of gel matrix and viscosity regulator.

关 键 词：5-氟尿嘧啶 液体栓 胶凝温度 紫外分光光度法 体外释放百分率 

分 类 号：R318.08[医药卫生—生物医学工程]