雌二醇阴道用温敏性凝胶的体外释药特性及局部滞留性评价  

Evaluation of in Vitro Release Profile and Local Retention of Estradiol Vaginal Thermosensitive Gel

作　　者：符旭东[1] 王姗姗 陈湖海[1] 

机构地区：[1]中国人民解放军武汉总医院药剂科,武汉430070 [2]湖北省襄阳市第一人民医院药学部,武汉441000

出　　处：《中国药学杂志》2017年第10期852-856,共5页Chinese Pharmaceutical Journal

摘　　要：目的考察雌二醇阴道用温敏性凝胶E2-VTG的体外释药特性及体内滞留性。方法采用冷法工艺制备E2-VTG。采用动态透析法和高效液相色谱-荧光法进行体外释放度研究。以新吲哚菁绿IR820为荧光标记物,ICR小鼠为受试动物,应用CRi Maestro小动物成像系统检测不同时间点温敏凝胶在受试小鼠阴道处的滞留情况。结果雌二醇温敏凝胶具有明显的缓释特征,24 h时药物累计释放率达到87%,释放模型拟合遵循Higuchi方程,推测雌二醇温敏凝胶主要通过扩散机制释药。NIR成像与荧光定量分析显示温敏凝胶在ICR小鼠阴道内滞留时间至少可达8 h。结论雌二醇温敏凝胶可延长药物在阴道内的滞留时间,延缓药物的释放。OBJECTIVE To examine the in vitro release profile and in vivo retention of estradiol vaginal thermosensitive gel （ E2- VTG）. METHODS E2-VTISG was prepared by cold dissolving method. The dynamic membrane dialysis method and HPLC-fluoro- metric method were used to determine the in vitro release characteristic of the estradiol vaginal thermosensitive gel. CRi Maestro was ap- plied to evaluate the retention of E2-VTG in ICR mice with IR820 as the fluorescent marker. RESULTS Estradiol could be released slowly from the thermosensitive gel and the release profile was fitted with Higuchi equation. It was speculated that estradiol was mainly released through diffusion. NIR imaging and fluorescence quantitative analysis showed that thermosensitive gel could reside in vagina for at least 8 h. CONCLUSION Estradiol thermosensitive gel can prolong the drug residence time in vagina and sustain the drug release rate.

关 键 词：雌二醇 泊洛沙姆 温敏凝胶 体外释放度 体内滞留性 

分 类 号：R944[医药卫生—药剂学]