title: Double-layer weekly sustained release transdermal patch containing gestodene and ethinylestradiol.
abstract: The combination therapy of gestodene (GEST) and ethinylestradiol (EE) has shown advanced contraception effect and lower side effect. The present study was designed to develop a weekly sustained release matrix type transdermal patch containing GEST and EE using blends of different polymeric combinations. The multiple-layer technique was adopted in order to maintain a steady permeation flux for 7 days. The effects of polymer types, polymer ratios, permeation enhancers, drug loadings and drug ratios in different layers on the skin permeations of the drugs were evaluated using excised mice skin. Polariscope examination was carried out to observe the drug distribution behavior. The formulation with the mixture of polyvinyl alcohol (PVA) and polyvinyl pyrrolidone (PVP) (7:1) was found to provide the regular release and propylene glycol (PG) could enhance the permeation fluxes of drugs. Double-layer transdermal drug delivery system (TDDS) could sustain the steady permeation flux of drugs for 7 days when the ratio of drug in drug release layer and drug reservoir layer was 1:4 with the identical total drug amount. The in vitro transdermal permeation fluxes were 0.377 microg/cm(2)/h and 0.092 microg/cm(2)/h, for GEST and EE respectively. The uniformity of dosage units test showed that the distribution of drugs in the matrix was homogeneous, which was further demonstrated by the polariscope result. The developed transdermal delivery system containing GEST and EE could be a promising non-oral contraceptive method.
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
authors.forename: Yanli
authors.initials: Y
authors.lastname: Gao
authors.forename: Jinying
authors.initials: J
authors.lastname: Liang
authors.forename: Jianping
authors.initials: J
authors.lastname: Liu
authors.forename: Yan
authors.initials: Y
authors.lastname: Xiao
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D003692:Delayed-Action Preparations / Q000009:adverse effects / Q000737:chemistry* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods*; D004997:Ethinyl Estradiol / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051379:Mice; D009652:Norpregnenes / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D010539:Permeability; D011108:Polymers / Q000737:chemistry; D011817:Rabbits; D012869:Skin Absorption; D013997:Time Factors
chemical_list: D003692:Delayed-Action Preparations; D009652:Norpregnenes; D011108:Polymers; C033273:Gestodene; D004997:Ethinyl Estradiol