Characterization of Poloxamer188 Solid Dispersion with Etonogestrel and Ethinylestradiol Loaded

LV Yunqi; GAO Feng; WANG Yingying; WANG Hao

doi:10.3969/j.issn.2096-305X.2025.01.001

Abstract：Objective To prepare solid dispersion of etonogestrel and ethinylestradiol of the clinical prescription amount,and to investigate the drug loading and release behavior.Methods After different amounts of etonogestrel or ethinylestradiol and Poloxamer188 were dissolved in methylene chloride,the solvent was cast on the glass plate and dried.High performance liquid chromatography-ultraviolet spectrophotometry was used to measure the amount of drug released from the solid dispersion in the release medium and plot the time release curve.Differential thermal analysis,thermogravimetric analysis and X-ray diffraction were used to evaluate the coating behavior of the two drugs in solid dispersions.Results The release percentage of etonogestrel and ethinylestradiol from Poloxamer188 solid dispersion was lower when the drugs loading amounts were higher,meanwhile drugs release percentage was higher when their loading amounts were lower.From the single-prescription solid dispersions,the release of ethinylestradiol was more complete than ethinylestradiol,but the release percentage of ethinylestradiol from the compound-prescription solid dispersion was only 1/3 of ethinylestradiol.The characteristic peaks of Poloxamer188 on the differential thermal analysis curve and the X-ray diffraction patterns were obvious while characteristic peaks of the drugs peak were not obvious,but the Poloxamer188 solid dispersion containing both etonogestrel and ethinylestradiol showed a special peaks pattern.Conclusion Poloxamer188,as a solid dispersion carrier for etonogestrel and ethinylestradiol,can solubilize the two drugs to a certain extent,and has showed certain sustained release profiles within 5 hours.The compound prescription has showed a novel composite behavior,and its release behavior is significantly different from that of the single prescription.