诺氟沙星阴道用温度敏感原位凝胶的制备及体外释放度研究  

Preparation and in vitro Release of Norfloxacin Thermosensitive in Situ Gel for Vaginal Use

作　　者：张春燕[1] 赵迎春[1] 范义凤[1] 

机构地区：[1]南通大学附属医院药学部,江苏南通226001

出　　处：《中国药师》2017年第11期1983-1986,共4页China Pharmacist

摘　　要：目的:制备诺氟沙星阴道用温度敏感原位凝胶,并考察其体外药物释放行为。方法:以泊洛沙姆为基质,采用冷溶法制备诺氟沙星阴道用温度敏感原位凝胶,考察泊洛沙姆407与泊洛沙姆188的用量对胶凝相变温度的影响,采用星点设计-效应面法优化其处方,并考察其体外药物释放行为。结果:在一定浓度范围内,随着泊洛沙姆407用量的增大胶凝化温度逐渐降低,随着泊洛沙姆188用量的增大胶凝化温度逐渐升高,通过优化得到诺氟沙星阴道用温度敏感原位凝胶的最佳处方为:泊洛沙姆407的浓度为20.6%(w/v),泊洛沙姆188的浓度为5.7%(w/v),在温度为36.5℃以上可发生胶凝。药物在温度敏感原位凝胶中呈持续缓慢释放,6 h药物的累积释放度为87.5%±5.4%。结论:诺氟沙星阴道用温度敏感原位凝胶具有很好的温度敏感性,可以延缓药物释放,有望开发成为一种新型阴道给药制剂。Objective： To prepare norfloxacin thermosensitive in situ gel and investigate its in vitro drug release behavior. Methods： Poloxamer 407 and poloxamer 188 were used as the matrix of norfloxacin thermosensitive in situ gel, and the gel was prepared by a cold dissolving method. The formula was optimized by a central composite design-response surface method. In vitro drug release behavior of norfloxacin thermosensitive in situ gel was studied as well. Results： Within a certain concentration range, the gelation temperature decreased gradually with the amount increase of poloxamer 407, and that increased gradually with the amount increase of poloxamer 188. The optimal formula was as follows： the concentration of poloxamer 407 was 20.6% （w/v） , and that of poloxamer 188 was 5.7% （w/v）, which obtained suitable gelling temperature. The release of norfloxacin from the thermosensitive in situ gel reached up to （87.5% ± 5.4% 7 in 6 h. Conclusion： Norfloxacin thermosensitive in situ gel has excellent temperature sensitivity, and can slow down the drug release, which shows potential use for vaginal drug delivery system.

关 键 词：诺氟沙星 温度敏感原位凝胶 冷溶法 泊洛沙姆 

分 类 号：R944.9[医药卫生—药剂学]