温度敏感性壬苯醇醚阴道用缓释凝胶的制备与评价  

preparation of temperature-sensitive nonoxynol-9 sustained-release gel for vagina

作　　者：王成伟[1] 唐星[1] 王晓梅[1] 田晓琳[1] 李真[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2006年第4期280-284,共5页Chinese Journal of New Drugs

摘　　要：目的:制备以聚丙烯酸类为基本材料的温度敏感性壬苯醇醚阴道用缓释凝胶,建立温度敏感性阴道用缓释凝胶剂的体内外评价方法。方法:采用均匀试验设计,考察了泊洛沙姆F127和F68对凝胶化温度及25℃时和37℃时的黏度变化的影响,筛选出优化组合;加入聚丙烯酸类材料制备凝胶,进行显微观察、释放度、灌流冲洗量、黏度与黏附力评价;大鼠阴道内给予优化处方与国外产品,测定阴道冲洗液中药物的质量浓度。结果:温度敏感性材料优化组合为:泊洛沙姆F127的质量分数为18．2%,泊洛沙姆F68的质量分数为8．8%,制备的凝胶在大鼠阴道滞留时间可达12 h以上,室温下有较好的流动性。结论:温度敏感性壬苯醇醚阴道用缓释凝胶具有良好的体外释放性能、温度敏感黏附性能及阴道内滞留性能。Objective： To prepare and characterize the temperature-sensitive nonoxynol-9 sustained-release vaginal gel. Methods： The optimal vehicles were identified by measuring the effects of poloxamer F127 and F68 on the gelling temperature and the gel viscosity at 25 ℃ and 37 ℃. Polyacrylic acid was used as a bioadhesive agent. The optimal formulation was assessed based on several factors such as the release behavior, viscosity and adhesive force. The dispensation of the active ingredients from the optimal gel made locally throughout the rat vagina was compared with the gel imported. Results： The optimal mass percentage of temperature-sensitive vehicles in the gel were as follows： 18.2 % of poloxamer F127 and 8.8 % of poloxamer F68. The active nonoxynol-9 was sustained into the rat＇s vagina up to 12 hours. Conclusion： The temperature-sensitive nonoxynol-9 sustained-release vaginal gel showed better behaviors of sustained release in vitro, temperature-sensitive adhesion and vaginal retention.

关 键 词：壬苯醇醚 温度敏感性凝胶 生物黏附 缓释 阴道滞留 

分 类 号：R944.9[医药卫生—药剂学] R979.12[医药卫生—药学]