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Fluorescein-labelled sulodexide pharmacokinetics and urinary excretion were studied in the rat after intravenous administration. The compound showed a pharmacokinetic pattern similar to that of heparin and the plasmatic levels were linearly correlated with anti-factor Xa activity and logarithmically with lipoprotein lipase activation. The compound is well eliminated by urinary route; the urinary recovery was 50% in 24 h and 67% 48 h after administration. The results obtained indicate that fluorescein labelling of glycosaminoglycans may be a valid tool for pharmacokinetics and distribution studies in the laboratory animals.

The pharmacokinetics of acipimox was studied in 6 dialyzed uremic patients given single oral doses of 50 mg. Acipimox was not significantly eliminated outside dialysis, whereas during dialysis it was efficiently cleared with plasma, t 1/2 is about 2.6 hours. Accordingly, a dosage schedule of 50 mg or 100 mg of acipimox after each dialysis session was selected for a second, 4-week study in 14 uremic patients with hypertriglyceridemia. Acipimox plasma levels, monitored during the study, proved in agreement with those expected on a theoretical pharmacokinetic basis. A clear-cut reduction of serum triglyceride levels was also achieved.

STS 267 [1; 16 alpha-azido-3-methoxy-estra-1,3,5(10)-trien-17-one] was found to have lipid shifting and fertility inhibitory effects in rats. In preclinical studies the metabolic fate of 1 was investigated in the rat. Demethylation in 3-position, reduction of the 17-carbonyl to the 17 beta-hydroxyl group, and for the first time the epimerization of the 16 alpha-azido to the 16 beta-azido group were established following perfusion of STS 267 in the isolated rat liver. From the perfusion medium 16 alpha-azido-estra-1,3,5(10)-trien-3-ol-17-one (2), 16 alpha-azido-estra-1,3,5(10)-trien-3,17 beta-diol (3), 16 beta-azido-3-methoxy-estra-1,3,5(10)-trien-3,17 beta-diol (4) and 16 beta-azido-estra-1,3,5(10)-trien-3,17 beta-diol (5) as the main metabolite were isolated by TLC and identified by comparison with authentic samples. The extent of the hepatic extraction of 1 in the rat liver was significant lower compared with mestranol.