Spectrophotometric determination of desoximetasone in ointment using 1,4-dihydrazinophthalazine

The proposed method is based on coloured hydrazone formation with 1,4-dihydrazinophthalazine as a reagent. Heating at 85 degrees C for 2 h was found necessary to ensure optimal hydrazone formation in the presence of hydrochloric acid. The yellow hydrazone product has an absorption maximum at 380 nm. A linear relationship between absorbance and concentration was established in the concentration range 3.19 x 10(-6)-3.19 x 10(-5) mol l(-1) (the regression equation was y = 0.013 167 3 + 0.019 025 9x; correlation coefficient r = 0.9991; n = 6). The detection limit was 1.2 mu g ml(-1) (molar absorptivity found was 1.97 x 10(4) l mol(-1) cm(-1)). The reliability of the proposed method was checked at three different concentrations; the relative standard deviation (RSD) varied from 1.03 to 2.01%. The described method applied to the determination of desoximetasone in ointment gave precise and reproducible results; the recovery was 98.55% with RSD = 2.40% (n = 10).5th International Symposium on Drug Analysis, Sep 12-15, 1995, Louvain, Belgiu

A PAMPA Assay as Fast Predictive Model of Passive Human Skin Permeability of New Synthesized Corticosteroid C-21 Esters

The permeation properties of twenty newly synthesized α-alkoxyalkanoyl and α-aryloxyalkanoyl C-21 esters of standard corticosteroids: Fluocinolone acetonide, dexamethasone, triamcinolone acetonide and hydrocortisone were established using a PAMPA assay (70% silicone oil and 30% isopropyl myristate). The data were compared with parent corticosteroids with addition of mometasone furoate and hydrocortisone acetate. All newly synthesized corticosteroid C-21 esters have effective permeability coefficients higher then -6, mostly followed with high values of retention factors and low permeation. The examined compounds were grouped through relationship between obtained retention factors and permeation parameters (groups I–III). The classification confirmed group I (membrane retentions as well as permeation lower then 30%) for all corticosteroid standards except mometasone furoate, a potent topical corticosteroid which, with high membrane retention (81%) and low permeation (7.7%) fits into group III. The largest number of new synthesized corticosteroids C-21 esters, among them all fluocinolone acetonide C-21 esters, have high membrane retentions (32.4%–86.5%) and low permeations (1.3%–27.1%), fitting in group III. The classification was related to previously obtained anti-inflammatory activity data for the fluocinolone acetonide C-21 esters series. According to the PAMPA results the new synthesized esters could be considered as potential new prodrugs with useful benefit/risk ratio