title: Development and stability of semisolid preparations based on a supercritical CO2 Arnica extract.
abstract: Conventional herbal drug preparations (HDP) based on Arnica montana L. have a low content of the active principles, sesquiterpene lactones, which show poor stability and low physical compatibility in semisolid formulations. Recently, an innovative supercritical carbon dioxide (CO2) extract with high sesquiterpene content has been marketed. Development of six semisolid preparations (cetomacrogol, polysorbate 60, polawax, anphyphil, natrosol and sepigel) based on this innovative CO2 extract is discussed. Stability of these preparations was investigated according to ICH guidelines. The evaluation of in vitro release of active constituents was performed using the cell method reported in the European Pharmacopoeia. Preliminary data on in vivo permeation of three selected formulations is demonstrated using the "skin stripping" test, according to the FDA, in healthy subjects. Analysis of sesquiterpene lactones within the extract and in vitro and in vivo studies was performed by RP-HPLC-DAD-MS method. The cetomacrogol showed the best release profile in the in vitro test, while in the in vivo test the best preparation resulted polysorbate 60 and polawax.
authors.affiliation: Department of Pharmaceutical Sciences, University of Florence, Via U. Schiff 6, 50019 Sesto Fiorentino-Florence, Italy. ar.bilia@unifi.it
authors.forename: Anna Rita
authors.initials: AR
authors.lastname: Bilia
authors.forename: Maria Camilla
authors.initials: MC
authors.lastname: Bergonzi
authors.forename: Giovanni
authors.initials: G
authors.lastname: Mazzi
authors.forename: Franco Francesco
authors.initials: FF
authors.lastname: Vincieri
mesh_terms: D000279:Administration, Cutaneous; D000328:Adult; D018650:Arnica / Q000737:chemistry; D002592:Cetomacrogol / Q000008:administration & dosage / Q000737:chemistry; D025924:Chromatography, Supercritical Fluid; D004355:Drug Stability; D004655:Emulsions; D005079:Excipients / Q000008:administration & dosage / Q000737:chemistry; D005260:Female; D006801:Humans; D010539:Permeability; D010936:Plant Extracts / Q000008:administration & dosage* / Q000737:chemistry*; D011136:Polysorbates / Q000008:administration & dosage / Q000737:chemistry; D012717:Sesquiterpenes / Q000032:analysis / Q000737:chemistry; D045789:Sesquiterpenes, Guaiane; D012869:Skin Absorption; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D004655:Emulsions; D005079:Excipients; D010936:Plant Extracts; D011136:Polysorbates; D012717:Sesquiterpenes; D045789:Sesquiterpenes, Guaiane; D013501:Surface-Active Agents; C026745:plenolin; C001329:helenalin; D002592:Cetomacrogol