摘要
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（Ace-Acid TISG） is expected to be used as vaginal topical contraceptive candidate and charactered to be thermosensitive. We aimed to detect the rheological properties at different temperatures, the gel dissolution and in vitro. Methods： Ace-Acid TISG was prepared using the cold method. The phase transition temperature（PTT）, gelling temperature and the different rheological parameters were detected using Kinexus Pro Advanced rotation rheometer during the phase transition.The dissolution behavior was measured by the membraneless dissolution test. In vitro release was tested by the potentiometric titration method. Results： The PTT and the GT of Ace-Acid TISG were 25 ℃ and 30 ℃,respectively. When the temperature was below 25 ℃, Ace-Acid TISG was fluid, it’s viscoelasticity was very low and phase angle（δ） was 80°-90°; as the temperature increasing, it’s viscoelasticity showed exponential growing,δ decreases（30°-40°）. It showed the typical linear relationship between the in vitro release rate and gel dissolution rate of acetic acid, and followed zero-order kinetics. Conclusion： Ace-Acid TISG is the thermosensitive gel.It can meet the requirements for vaginal topical use and is expected to be applied in clinical practice.
出处
《生殖与避孕》
CAS
CSCD
北大核心
2015年第6期373-378,共6页
Reproduction and Contraception
基金
国家科技重大专项(2012ZX10001007-009-003
2013ZX10001006-003-002)
十二五国家科技支撑计划(2012BAI31B04)
国家自然科学基金青年基金项目(81100459)
上海市科委项目(11PJ1408400
11140902900)
上海市人口和计划生育委员会资助项目(2012JG03)
关键词
乙酸
热敏原位凝胶
胶凝温度
相转变
凝胶溶蚀
体外释放
acetic acid
thermosensitive in situ gel
phase transition
gelation temperature
gel dissolution
in vitro release
