[Comparative studies in man on the percutaneous absorption of diflucortolone valerate, betamethasone-17-valerate, beclomethasone dipropionate and fluocinolone acetonide]

Abstract

Percutaneous absorption of 6alpha,9-difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadience-3,20-dione (diflucortolone valerate, DFV, Nerisona), betamethasone 17-valerate (BV), beclomethasone dipropionate (BDP) and fluocinolone acetonide (FA) by damaged skin was examined on the backs of 4 healthy males from whom the stratum corneum had been removed by "stripping". The determination of percutaneous absorption was performed on the one hand by a method employing radioactive labelled compounds (DFV, BV) and measuring the elimination with the urine and faeces and on the other hand by photometric determination (DFV, BV, BD, fa) of the corticoid remaining on the skin immediately following application and at the end of a 24-h period of exposure. Direct measurement of the radioactivity in the urine and faeces revealed that percutaneous absorption from a new W/O emulsion takes place up to 2.2+/-0.8% in the case of DFV (0.1%) and to at least 12.2+/-3.3% in the case of BV (0.12%) within 24 h. The determination of percutaneous absorption via recovery from the skin produced the following results for the 4 corticoid preparations examined: DFV (14.8+/-4.2%) and BDP (14.0+/-4.3%) approximately equal, BV (23.5+/-4.1%) a marked increase and FA (39.2+/-2.4%) the highest level of absorption. This order for percutaneous absorption appears to correlate to the frequency of systemic side effects.