MENOREST(R) - TECHNICAL DEVELOPMENT AND PHARMACOKINETIC PROFILE

Transdermal application of oestradiol enables the use of lower doses t han with the oral drug and avoids first-pass metabolism in the liver. First-generation transdermal delivery systems were of reservoir design . Menorest(R) is one of a new generation of patches, in which oestradi ol is dispersed in a micronized suspension throughout the adhesive mat rix. This design results in a very thin patch with good cosmetic accep tability. Pharmacokinetic studies indicate that Menorest(R) allows tra nsdermal release of oestradiol at a constant and reproducible rate at doses from 25-100 mu g/day. There is a linear relationship between the dose of oestradiol administered (which is determined by the surface a rea of the patch) and the plasma concentration of oestradiol. In contr ast to the standard reference reservoir patch, Estraderm(R), Menorest( R) maintains plasma oestradiol concentrations at or above the target l evel of 40 pg/ml throughout the 84-h dosing interval.