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含屈螺酮阴道环的制备与评价

Preparation and evaluation of intravaginal ring containing drospirenone.

作者信息

Zhang Ying, Li Chun-Xiao, Ning Mei-Ying, Duan Xue-Yan, Liu Ying

机构信息

Research Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, No. 12 Da Hui Si Haidian District, Beijing 100081, China.

出版信息

Adv Pharmacol Sci. 2013;2013:192408. doi: 10.1155/2013/192408. Epub 2013 Jan 17.

DOI:10.1155/2013/192408
PMID:23401679
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3562644/
Abstract

In the present study, we investigated the feasibility of the vaginal administration of drospirenone silicone IVR. The in vitro release characteristics of matrix-type and reservoir-type IVR were compared under sink conditions in 21 days. At the same time, API excipients compatibility and preformulation study was performed by HPLC, IR, and DSC methods. Biocompatibility of reservoir system was evaluated by tolerability on tissue level in rats. It was found that, under strong light exposure, high temperature, and high humidity conditions, drospirenone and excipients had no significant interactions. The daily release of reservoir-type IVR was about 0.5 mg/d sustaining 21 days, which significantly decreased the burst effect compared with the matrix system. When drospirenone was modified by the PVPk30 in the reservoir system formulation, the daily release rate increased to 1.0 mg/d sustaining 21 days. The cumulative release of reservoir-type IVR was fitted to zero release equation. In addition, biocompatibility of drospirenone IVR system in this dosage is safe. It is feasibility feasibile to further developed for safe, convenient, and effective contraceptive drug delivery with reduced dosing interval.

摘要

在本研究中，我们研究了阴道给药屈螺酮硅胶宫内缓释系统（IVR）的可行性。在漏槽条件下比较了基质型和储库型IVR在21天内的体外释放特性。同时，采用高效液相色谱法（HPLC）、红外光谱法（IR）和差示扫描量热法（DSC）进行了活性成分与辅料的相容性及处方前研究。通过大鼠组织水平的耐受性评估储库系统的生物相容性。结果发现，在强光照射、高温和高湿条件下，屈螺酮与辅料无显著相互作用。储库型IVR的日释放量约为0.5mg/d，持续21天，与基质系统相比，显著降低了突释效应。在储库系统制剂中用聚维酮K30（PVPk30）修饰屈螺酮时，日释放率提高到1.0mg/d，持续21天。储库型IVR的累积释放符合零级释放方程。此外，该剂量的屈螺酮IVR系统生物相容性良好。进一步开发安全、方便、有效的避孕药递送系统并缩短给药间隔是可行的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6d6/3562644/7a2c68f686a2/APS2013-192408.011.jpg
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Intravaginal ring delivery of the reverse transcriptase inhibitor TMC 120 as an HIV microbicide.作为一种HIV杀微生物剂的逆转录酶抑制剂TMC 120的阴道环给药。
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Design of a silicone reservoir intravaginal ring for the delivery of oxybutynin.用于递送奥昔布宁的硅树脂储库型阴道环的设计
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