title: Preparation and evaluation of intravaginal ring containing drospirenone.
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.
authors: 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.
authors: Ying
authors: Y
authors: Zhang
authors: Chun-Xiao
authors: CX
authors: Li
authors: Mei-Ying
authors: MY
authors: Ning
authors: Xue-Yan
authors: XY
authors: Duan
authors: Ying
authors: Y
authors: Liu
references: Antiviral Res. 2010 Dec;88 Suppl 1:S55-66
references: 21109069
references: Antiviral Res. 2010 Dec;88 Suppl 1:S30-9
references: 21109066
references: AIDS. 2009 May 15;23(8):917-22
references: 19381077
references: J Control Release. 2003 Sep 4;91(3):465-76
references: 12932723
references: J Pharm Sci. 1975 Oct;64(10):1643-7
references: 1185530
references: Contraception. 2007 Aug;76(2):132-8
references: 17656183
references: Semin Reprod Med. 2010 Mar;28(2):133-9
references: 20352563
references: Antiviral Res. 2010 Dec;88 Suppl 1:S47-54
references: 21109068
references: Int J Pharm. 2006 Nov 15;325(1-2):82-9
references: 16884869
references: Contraception. 2011 Feb;83(2):107-15
references: 21237335
references: Int J Pharm. 1999 Apr 30;181(2):143-51
references: 10370210