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目的:乙酸阴道热敏原位凝胶剂(Acetic Acid vaginal thermosensitive in situ gel,AceAcid TISG)作为一种候选阴道外用避孕药,具有温度敏感性的特点,本文旨在考察在不同温度下的流变性质、凝胶溶蚀以及体外释放特性。方法:冷法制备Ace-Acid TISG,采用Kinexus Pro高级旋转流变仪测定相转变温度,胶凝温度以及不同温度下相变过程中的流变参数;无膜溶出法检测凝胶的溶蚀行为;电位滴定法测定乙酸的体外释放度。结果:Ace-Acid TISG相转变温度为25℃,胶凝温度为30℃;低温下为流体,粘弹性很低,相角很高;温度升高,粘弹性呈指数增长,相角降低。乙酸体外释放速率与凝胶溶蚀速率呈现良好的线性关系,两者遵循零级动力学方程。结论:本凝胶制剂具有良好的热敏感性和体外释放性,符合阴道即用型凝胶的要求,有望在临床中获得应用。
OBJECTIVE: Acetic Acid vaginal thermosensitive in situ gel (AceAcid TISG), as a candidate vaginal contraceptive, is characterized by its temperature sensitivity. This paper aims to investigate the rheological behavior at different temperatures Nature, gel dissolution and in vitro release characteristics. Methods: Ace-Acid TISG was prepared by cold method. Phase transition temperature, gelling temperature and rheological parameters during phase transition were determined by Kinexus Pro high-performance rotary rheometer. The dissolution behavior of gel was measured by membrane-free dissolution method. Potentiometric titration of acetic acid in vitro release. Results: Ace-Acid TISG has a phase transition temperature of 25 ℃ and a gelation temperature of 30 ℃. It has a low viscoelasticity and a high phase angle at high temperature. Viscoelasticity increases exponentially and phase angle decreases with increasing temperature. The in vitro release rate of acetic acid shows a good linear relationship with the dissolution rate of the gel, both of which follow the zero-order kinetic equation. Conclusion: The gel preparation has good thermal sensitivity and in vitro release, in line with vaginal ready-to-use gel requirements, is expected to be clinically applied.