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Percutaneous penetration and anti-inflammatory activity of desfluorotriamcinolone acetonide

University of British Columbia

Desonide, a new topical anti-inflammatory and antipruritic steroid, has been investigated for its clinical, vasoconstrictor and in vitro percutaneous penetration properties, and compared to betamethasone 17-valerate, triamcinolone acetonide and hydrocortisone. The clinical and vasoconstrictor bioassay tests place desonide quantitatively among the most effective topical anti-inflammatory agents, possibly because of its relatively rapid skin penetration rate. The significance of the study is (a) it provides definitive data on topical anti-inflammatory effectiveness of desonide and (b) it reveals that, contrary to current opinion, fluorination of the steroid molecule may be unnecessary for topical anti-inflammatory activity, and that 9 °C-fluorination in prednisolone acetonides impedes rather than favours their skin penetration rates. New data on octanol/water partition coefficients and an unsuccessful effort of adopting the Martin (1968) oxime derivative spectrophotofluorometric technique for desonide assays are also included.

Text

2011-04-07

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http://hdl.handle.net/2429/33373

Pharmaceutical Sciences

University of British Columbia

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