Preparation and Evaluation of Intravaginal Ring Containing Drospirenone

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 preformulat...

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Main Authors: Ying Zhang, Chun-Xiao Li, Mei-Ying Ning, Xue-Yan Duan, Ying Liu
Format: Article
Language:English
Published: Wiley 2013-01-01
Series:Advances in Pharmacological Sciences
Online Access:http://dx.doi.org/10.1155/2013/192408
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author Ying Zhang
Chun-Xiao Li
Mei-Ying Ning
Xue-Yan Duan
Ying Liu
author_facet Ying Zhang
Chun-Xiao Li
Mei-Ying Ning
Xue-Yan Duan
Ying Liu
author_sort Ying Zhang
collection DOAJ
description 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.
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spelling doaj-art-bf51267ea3b3479f87ecbc02b70b87fb2025-02-03T07:25:30ZengWileyAdvances in Pharmacological Sciences1687-63341687-63422013-01-01201310.1155/2013/192408192408Preparation and Evaluation of Intravaginal Ring Containing DrospirenoneYing Zhang0Chun-Xiao Li1Mei-Ying Ning2Xue-Yan Duan3Ying Liu4Research Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, No. 12 Da Hui Si Haidian District, Beijing 100081, ChinaResearch Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, No. 12 Da Hui Si Haidian District, Beijing 100081, ChinaResearch Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, No. 12 Da Hui Si Haidian District, Beijing 100081, ChinaResearch Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, No. 12 Da Hui Si Haidian District, Beijing 100081, ChinaResearch Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, No. 12 Da Hui Si Haidian District, Beijing 100081, ChinaIn 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.http://dx.doi.org/10.1155/2013/192408
spellingShingle Ying Zhang
Chun-Xiao Li
Mei-Ying Ning
Xue-Yan Duan
Ying Liu
Preparation and Evaluation of Intravaginal Ring Containing Drospirenone
Advances in Pharmacological Sciences
title Preparation and Evaluation of Intravaginal Ring Containing Drospirenone
title_full Preparation and Evaluation of Intravaginal Ring Containing Drospirenone
title_fullStr Preparation and Evaluation of Intravaginal Ring Containing Drospirenone
title_full_unstemmed Preparation and Evaluation of Intravaginal Ring Containing Drospirenone
title_short Preparation and Evaluation of Intravaginal Ring Containing Drospirenone
title_sort preparation and evaluation of intravaginal ring containing drospirenone
url http://dx.doi.org/10.1155/2013/192408
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