Gloor M, Shabafrouz H
Dermatologica. 1983;166(2):69-74. doi: 10.1159/000249839.
Comparative measurements of in vitro agent release using hydrophilic, intermediate, and lipophilic acceptor phases and in vivo measurements of the blanching effect with triamcinolone acetonide are reported. White petrolatum, wool alcohols ointment, and polyethylene glycol ointment served as donator phases. The results demonstrate that the lipophilic acceptor phase (isopropyl palmitate) is most representative for the in vivo acceptor phase. Conclusions cannot be drawn regarding in vivo effectiveness from measurements of agent release to the hydrophilic (phosphate buffer, pH 6) and intermediate (n-octanol) acceptor phases. In vitro measurements of agent release have a screening character and must usually be supplemented by very elaborate penetration models of the human skin for a definitive evaluation of an ointment.
报告了使用亲水性、中等亲脂性和疏水性接受相进行的体外药物释放比较测量,以及曲安奈德的体内变白效应测量。白凡士林、羊毛醇软膏和聚乙二醇软膏用作供体相。结果表明,疏水性接受相(棕榈酸异丙酯)最能代表体内接受相。从药物释放到亲水性(pH 6的磷酸盐缓冲液)和中等亲脂性(正辛醇)接受相的测量结果无法得出关于体内有效性的结论。体外药物释放测量具有筛选性质,通常必须辅以非常精细的人体皮肤渗透模型,才能对软膏进行最终评估。