包膜型PVP_K30屈螺酮固体分散体阴道环相关研究

Study on capsulated drospirenone treated by PVP solid dispersion IVR

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 study the compatibility of intravaginal ring （IVR） containing drospirenone by HPLC gradient method. METHODS Capsulated drospirenone IVR and capsulated drospirenone which was treated by PVP solid dispersion IVR were obtained by using hot vulcanization method with silicone elastomer as the matrix polymer. In vitro drug release testing was conducted in a dissolution apparatus, and release samples were determined by the UV-uis spectrophotometry. The stabilities of drospirenone and PVP, silicone rubber were inspected by HPLC gradient method under the condition of 60 ℃, relative humidity of 75% and illuminated at 4 500 Lx respectively for 5 d and 10 d. RESULTS Compared with capsulated vaginal ring device, the daily release quantity of capsulated drospirenone-PVP IVR in vitro increased and sustained 21 days at the release rate of 1.0 mg·d^-1. Under strong light, high temperature, high humidity conditions, drospirenone raw materials and for mulation excipients PVPK30 and silicon rubber had no significant interactions, and indicated good compatibility. CONCLUSION PVP could improve the drospirenone release from the intravaginal ring and the formulation was stable, so as to provide a scientific basis for adjustment and optimization of prescription.