[Synthesis of Butyl 6alpha-Fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxo-1,4-pregnadien-21-oate (Fluocortin Butylester) (author's transl)].

Among the metabolites of fluocortolone (1) there was found the alpha-keto acid 4a. This acid, as well as the esters 4b--4k were synthesized and the butyl ester 4c was chosen for local anti-inflammatory therapy.

In vitro studies on enzymatic cleavage of steroid esters in the female organism.

The decreasing water-solubility of steroid esters concomitant with increasing chain lenth of monocarboxylic acids provides a prolonged therapeutic effect of the steroid. Whether a slow release of the steroid from an oily depot in the muscle or a secondary storage of the enter in the body fat ("deep compartment") are responsible for this prolonged action, is open to discussion. The aim of this study was to investigate the steriod ester cleaving enzyme activity of human subcutaneous fatty tissue.

Metabolism, kinetics and metabolic activity of the beta-cytotropic antidiabetic 4-(5-isobutylpyrimidinyl-2)-sulphamylphenylacetic acid-3-chloro-6-methoxyanilide sodium (glydanile sodium) in man after oral and intravenous administration.

The metabolism and pharmacokinetics of [3H]-labelled 4-(5-isobutylpyrimidinyl-2)-sulphamylphenylacetic acid-3-chloro-6-methoxyanilide sodium ([3H]-glydanile sodium) were investigated in three diabetics and six healthy volunteers after oral and i.v. administration.