MORGAN, Timothy,WILKINS, Nina,KLOSE, Kathryn,FINNIN, Barrie,REED, Barry
申请号：
ES03729716
公开号：
ES2589077T3
申请日:
2003.06.24
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A pharmaceutical composition for transdermal administration comprising: from 0.1% to 10% by weight of one or more physiologically active agents selected from testosterone and fentanyl； from 0.1% to 10% by weight of one or more dermal penetration enhancers where the dermal penetration enhancer is a nonvolatile lipophilic liquid having a vapor pressure of less than 10 mm Hg at atmospheric pressure and at temperature of 32 ° C, said dermal penetration enhancer has a molecular weight in the range of 200 to 400 daltons； and from 85% to 99.8% by weight of a volatile solvent selected from the group consisting of ethanol, isopropanol, and mixtures thereof； and wherein the combination of a physiologically active agent and a dermal penetration enhancer is such that, with the evaporation of the volatile solvent, the composition forms a deposit within the stratum corneum having at least 10% amorphous phase, said deposit it contains the dermal penetration enhancer and the physiologically active agent； and where the formation of the amorphous deposit is determined by in vitro DSC and bright field microscopy； wherein the DSC is then performed allowing the volatile solvent to evaporate from a sample of 5 μl of the composition, again applying additional 5 μl samples until a sufficient amount of physiologically active agent residue and dermal penetration enhancer remain , which is maintained at room temperature and 33% relative humidity for 24 hours； and wherein the light field microscopy is performed after evaporation of the volatile solvent for 24 hours of a sample of 5 µl of the pipetted composition on a glass slide at 32 ° C and relative ambient humidity.Una composición farmacéutica para la administración transdérmica que comprende: de 0,1% a 10% en peso de uno o más agentes fisiológicamente activos seleccionados de testosterona y fentanilo； de 0,1% a 10% en peso de uno o más potenciadores de la penetración dérmica en donde el potenciador de la penetración dérmica es un líquido l
