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Butyl 6alpha-fluoro-11beta-hydroxy-3,20-dioxo-16alpha-methyl-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) is a recently developed corticosteroid, its distinguishing properties being that it is non-embryotoxic and has practially no systemic effects. In the course of 6 multicentre studies fluocortin butylester was tested in the forms of cream, ointment and fatty ointment in a comparison with corresponding formulations containing fluocortolone (Ultralan) caproate or pivalate, or hydrocortisone acetate. The total study population comprised 1705 patients with various dermal disorders. The results of these double-blind contralateral studies permit the conclusion that the efficacy of the Vaspit preparations ranges between those of fluocortolone and hydrocortisone acetate. Considering the risks involved with local corticosteroid therapy in children the development of a local corticosteroid with the properties of fluocortin butylester must be acknowledged as an advance.

6alpha,9-Difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolone valerate, Nerisona) 0.1% as a cream, ointment and fatty ointment was investigated in a double-blind contralateral design in 925 patients in comparison to fluocortolone (Ultralan), fluocortolone caproate and fluocortolone pivalate in three concurrently performed studies. The results of the contralateral study show Nerisona cream and ointment to be more effective (P less than 0.01) than Ultralan. The fatty ointment was also superior, but the difference was statistically significant (P less than 0.05) only in the indication psoriasis. No differences could be established in the less sensitive absolute assessment. The therapeutic success rate of 76-92% according to strict criteria-only complete healing and distinct improvement were counted as a success-clearly demonstrates the efficacy of the preparations. The local side effects recorded-mainly irritation and burning- were of a mild nature.

Therapeutic efficacy and practicability of an interval treatment were investigated in a multi-center study in a total of 1573 patients with psoriasis or eczema, respectively. Fluocortolone monohydrate as Syracort and Syracerin as steroid-free "partner drug" were applied at 4-13-day intervals. The findings and established results substantiate equivalent therapeutic success in comparison with consistent treatment. Starting from the premise that the risk of steroid-induced skin lesions can be reduced, if not avoided, by interval application of topical corticoids one may consider steroid application at intervals as superior to consistent therapy.

The antiinflammatory efficacy of butyl 6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (fluocortin butylester, Vaspit) as a 0,75% ointment was tested in comparison with 1% hydrocortisone acetate ointment in the model of the pyrexal erythema. Fluocortin butylester appeared to be significantly superior to hydrocortisone acetate.

The pharmacokinetics of fluocortolone (Ultralan oral) and its effect on plasma cortisol levels were investigated during long-term treatment of patients with rheumatic and haematological diseases with different doses of fluocortolone. Fluocortolone was administered in the morning and plasma levels of fluocortolone and cortisol were measured in samples obtained 1.5, 3, 4, and 5 h p. adm. by means of specific radioimmunoassays. Maximum concentrations of fluocortolone in plasma (Cmax) and areas under the fluocortolone plasma level curves (AUC) increased linearly with the dose. The peak time (tmax = 2.04 +/- 0.85 h) and the plasma half-life (t1/2 = 1.53 +/- 0.52 h) were independent of the dose administered. Cortisol suppression as indicated by morning cortisol levels below 50 ng/ml plasma was not observed with doses below 10 mg/d.

Diflucortolone valerate was administered to 35 psoriatic patients of both sexes in 0.3% concentration as a W/O emulsion in comparison with various commercially available preparations to study its action in the psoriasis plaque test according to Scholtz and Dumas. The study showed the test substance to be equipotent with the halcinonide, clobetasol-17-propionate and desoximetasone preparations and significantly superior to those containing betamethasone-17,21-dipropionate, betamethasone-17-valerate and fluocinonide.