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目的:采用HPLC梯度法考察屈螺酮控释阴道环中原辅料的相容性。方法:以医用硅橡胶弹性体为药物载体,采用热压硫化法制备包膜型屈螺酮阴道环及包膜型PVPK30屈螺酮固体分散体阴道环,紫外分光光度法测定2种阴道环的体外释放情况。HPLC梯度法考察屈螺酮原料药与辅料PVPK30和硅橡胶混合物在经光照、高温及高湿条件处理后的稳定性。结果:包膜型PVP固体分散体屈螺酮阴道环较包膜型屈螺酮阴道环体外释放度有明显提高,每日释放药物约为1.0mg,持续平稳释放时间可达21d。光照、高温、高湿条件下,屈螺酮原料药与拟定辅料PVPK30和硅橡胶无明显相互作用,相容性良好。结论:PVPK30能够提高屈螺酮阴道环的释放度,并且屈螺酮原料药与辅料PVPK30和硅橡胶混合物在经光照、高温及高湿条件处理后稳定,从而为进一步处方调整以及优化提供科学依据。
OBJECTIVE: To investigate the compatibility of raw materials of drospirenone-controlled vaginal ring with HPLC gradient method. Methods: Medical silicone elastomer was used as the drug carrier, and the vaginal rings of coated drospirenone vaginal ring and coated PVPK30 drospirenone solid dispersion were prepared by hot press vulcanization. The contents of two kinds of vaginal rings were measured by ultraviolet spectrophotometry In vitro release. HPLC gradient method was used to investigate the stability of the mixture of daptosone drug substance and auxiliary PVPK30 and silicone rubber after being treated under light, high temperature and high humidity conditions. Results: The release of drospirenone vaginal ring of coated PVP solid dispersions was significantly higher than that of vaginal dapsone. The daily release of drug was about 1.0 mg, and the sustained release time was up to 21 days. Under light, high temperature and high humidity conditions, there is no obvious interaction between drospirenone API and the proposed auxiliary PVPK30 and silicone rubber, and the compatibility is good. CONCLUSION: PVPK30 can improve the release of drospirenone ring, and the mixture of drospirenone and its adjuvant PVPK30 and silicone rubber is stable after being treated by light, high temperature and high humidity, thus providing a scientific basis for further prescription adjustment and optimization .