蛇床子酸缓冲温敏型凝胶的制备与体外评价

Preparation and in vitro evaluation of Cnidium acid buffered temperature-sensitive gel for senile vaginitis

关键词:  老年性阴道炎  蛇床子  温敏凝胶剂  酸缓冲体系  D-最优混料设计法  胶凝温度

Key words:  senile vaginitis  cnidium  temperature-sensitive gel  lactic acid buffer  D-optimal mixture design  senile vaginitis  gelation temperature

摘要:

[目的] 制备蛇床子酸缓冲温敏型凝胶并对其进行体外评价。[方法] 以缓冲能力为指标，筛选酸缓冲体系，以蛇床子为模型药物，泊洛沙姆407和泊洛沙姆188为凝胶材料，采用冷溶法制备温敏凝胶，采用D-最优混料设计，以胶凝温度为指标优化处方，并对优化后处方进行体外评价。[结果] 最优处方为5.0%蛇床子提取物、0.2%尼泊金乙酯、10.0% PEG400、16.4%泊洛沙姆407、5.2%泊洛沙姆188、5.6%乳酸-乳酸钠缓冲体系、57.6%纯化水；优化后温敏凝胶的胶凝温度为（35.1±0.1）℃，pH值为（4.21±0.03），胶凝时间为（2.4±0.4） s，铺展性良好，黏度适宜，具有缓释作用。[结论] 制得的中药蛇床子凝胶具有温敏、缓释及酸缓冲特性，符合老年性阴道炎局部用药的生理结构特点及用药需求，为老年性阴道炎外用制剂的设计与开发提供参考。

Abstract:

[Objective] Prepare and evaluate cnidium acid buffered temperature-sensitive gel for senile vaginitis in vitro. [Methods] Taking buffer capacity as an indicator, to screen acid buffer system, and taking cnidium as a model drug, poloxamer 407 and poloxamer 188 were gel materials, to prepare temperature-sensitive gel by cold solution method, using gelation temperature as an indicator, the D-optimized mixture design was used to optimize the prescription, and in vitro evaluation of the optimized prescription was determined. [Results] The optimal prescription was:5.0% cnidium extract, 0.2% ethylparaben, 10% PEG400, 16.4% poloxamer 407, 5.2% poloxamer 188, 5.6% lactic acid-sodium lactate buffer system, 57.6% purified water;The optimized temperature-sensitive gel had an gelation temperature of (35.1±0.1)℃, pH value was 4.21±0.03, gel time was (2.4±0.4) s, spread ability was excellent, viscosity was proper, and it also had a sustained release effect. [Conclusion] The prepared Chinese medicine cnidium gel has temperature sensitivity, sustained release and acid buffering properties, and it is in line with the physiological structural characteristics of local vaginal vaginitis and the need for medication, which can provide reference for the design and development of external preparations for senile vaginitis.