title: Effect of selected fluorinated drugs in a "ringing" gel on rheological behaviour and skin permeation.
abstract: The purpose of the present study was to investigate the influence of different drugs exhibiting different solubility on the viscoelastic properties and on the skin diffusion profile of a ringing gel. In a preliminary rheology study with the placebo gel predominating elastic properties were confirmed and a temperature influence was indicated. Fluconazole, fludrocortisone-acetate, flumethasone-pivalate, flutamide and flufenamic-acid each 1% (w/w) were incorporated into the preparation and oscillatory measurements were performed at temperatures of 25, 28, 32 and 37 degrees C. In all drug containing formulations a high elastic G' value predominated the viscous G'' value. The highest G' value could be obtained with the incorporated flumethasone-pivalate. Additionally in almost all cases the G' values decreased with increasing temperature compared to the placebo gel. Additionally in vitro standard diffusion experiments using Franz-type cells and porcine skin were performed. Following rank order of the cumulative drug release after 48 h was obtained: fluconazole>flufenamic-acid>flumethasone-pivalate>flutamide>fludrocortisone-acetate. Furthermore an excellent chemical stability of all incorporated drugs was confirmed over 10 weeks.
authors.affiliation: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, Vienna, Austria.
authors.forename: Sonja
authors.initials: S
authors.lastname: Höller
authors.forename: Claudia
authors.initials: C
authors.lastname: Valenta
mesh_terms: D000818:Animals; D004058:Diffusion; D004355:Drug Stability; D015725:Fluconazole / Q000737:chemistry / Q000493:pharmacokinetics; D005438:Fludrocortisone / Q000737:chemistry / Q000493:pharmacokinetics; D005439:Flufenamic Acid / Q000737:chemistry / Q000493:pharmacokinetics; D005443:Flumethasone / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D017611:Fluorine Compounds / Q000737:chemistry*; D005485:Flutamide / Q000737:chemistry / Q000493:pharmacokinetics; D005782:Gels; D057927:Hydrophobic and Hydrophilic Interactions; D066298:In Vitro Techniques; D009821:Oils / Q000737:chemistry; D010232:Paraffin / Q000737:chemistry; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D012881:Skin Temperature; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013552:Swine; D014783:Viscosity; D014867:Water / Q000737:chemistry
chemical_list: D017611:Fluorine Compounds; D005782:Gels; D009821:Oils; D004364:Pharmaceutical Preparations; D013501:Surface-Active Agents; D014867:Water; C005565:flumethasone pivalate; D005439:Flufenamic Acid; D005485:Flutamide; D010232:Paraffin; C015418:paraffin oils; D015725:Fluconazole; D005443:Flumethasone; D005438:Fludrocortisone