title: Preparation and in vitro/in vivo evaluation of gestodene (GEST) intravaginal ring.
abstract: Preparation and in vitro/in vivo evaluation of gestodene (GEST) intravaginal ring (IVR) formulations which can release a constant dose of GEST during 3 weeks were investigated. In present study a reservoir gestodene intravaginal ring, including a gestodene silicone elastomer core and the non-active silicone layer, was reported, which was manufactured by reaction injection moulding at 80°C for 20 min. The raw materials compatibility experiments showed that the silicone elastomer core carrier wouldn't interact with drugs. In vitro release samples were determined by HPLC and the experiment was performed under sink conditions. The equation of cumulative release verse time was Y=64.76χ+5.44 (r=0.9998), performing zero-order release at about the target dose of 60 µg/day over 21 days. Drug release increased with temperature elevating from 45 to 55°C, which could be attributed to optimizing the prescription. In addition, the pharmacokinetic and safety studies of gestodene intravaginal ring were evaluated in female New Zealand White rabbits. The GEST in plasma was analyzed by LC-MS/MS and the results proved that the correlation between in vitro and in vivo was relatively well.
authors.affiliation: Research Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, Da Hui Si Haidian District, Beijing, PR China / Graduate School of Peking Union Medical College; No. 9, Dongdan No. 3 Avenue, Beijing, PR China.
authors.forename: Chunxiao
authors.initials: C
authors.lastname: Li
authors.affiliation: Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, Da Hui Si Haidian District, Beijing, PR China / Graduate School of Peking Union Medical College; No. 9, Dongdan No. 3 Avenue, Beijing, PR China.
authors.forename: Meiying
authors.initials: M
authors.lastname: Ning
authors.affiliation: Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, Da Hui Si Haidian District, Beijing, PR China / Graduate School of Peking Union Medical College; No. 9, Dongdan No. 3 Avenue, Beijing, PR China.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Yao
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, China.
authors.forename: Yankun
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Research Center of Biomaterial and Novel Drug Delivery Systems, National Research Institute for Family Planning, Da Hui Si Haidian District, Beijing, PR China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
mesh_terms: D000282:Administration, Intravaginal; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D003280:Contraceptives, Oral, Synthetic / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000295:instrumentation*; D004867:Equipment Design; D005260:Female; D066298:In Vitro Techniques; D007436:Intrauterine Devices, Medicated; D008954:Models, Biological; D009652:Norpregnenes / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits; D012826:Silicone Elastomers; D012995:Solubility; D053719:Tandem Mass Spectrometry; D014621:Vagina / Q000187:drug effects
chemical_list: D003280:Contraceptives, Oral, Synthetic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D009652:Norpregnenes; D012826:Silicone Elastomers; C033273:Gestodene