Methodological study on in vitro release of etonogestrel/ethinyl estradiol compound vaginal ring
10.3760/cma.j.cn101441-20220507-00196
- VernacularTitle:依托孕烯/炔雌醇复方阴道环体外释放方法学研究
- Author:
Shasha WANG
1
;
Pan CHEN
;
Jia ZENG
;
Man XUE
;
Fang LI
;
Feng PAN
;
Yanhong ZHAO
;
Shiyu MA
;
Fuzheng REN
;
Yanxiong KE
;
Linglin FENG
Author Information
1. 华东理工大学制药工程与过程化学教育部工程研究中心，上海 200237
- Publication Type:Journal Article
- Keywords:
Etonogestrel;
Ethinyl estradiol;
Waginal ring;
Real-time release;
Accelerated release;
Correlation
- From:
Chinese Journal of Reproduction and Contraception
2023;43(8):813-819
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To develop an etonogestrel (ENG)/ethinyl estradiol (EE) compound vaginal ring with good sustained-release properties, studying its in vitro release assay methodology, and establishing an accelerated release method with good correlation with real-time release methods. Methods:Ethylene-vinyl acetate copolymer (EVA) was used as the matrix to prepare ENG/EE compound vaginal ring by hot melt extrusion method, and an in vitro real-time release assay method and an accelerated release assay method based on shake flask method were established. The in vitro release behavior and release mechanism of ENG/EE compound vaginal ring were investigated, and the correlation between real-time release and accelerated release over time was analyzed. Results:The obtained vaginal ring had a round appearance and a smooth surface, and the drug was slowly released under the optimal real-time release conditions in vitro (release medium: 200 mL of pure water, shaking at 60 r/min in a constant temperature water bath shaker at 37 ℃), and the cumulative release of ENG and EE on the 21st day were 54.39% and 46.80%, respectively. The correlation coefficients of drug release and its mechanism under the optimized in vitro accelerated conditions (release medium: 200 mL of 0.6% sodium dodecyl sulfate aqueous solution, shaking at 60 r/min at 55 ℃) with the results under real-time release conditions were all greater than 0.99. Conclusion:The ENG/EE compound vaginal ring obtained in this study has a significant in vitro sustained-release effect, and the established accelerated release conditions have a good correlation with real-time release conditions, which can provide a useful reference for the quality evaluation research of such vaginal ring products and the formulation of guidelines for in vitro release research methods.
