[AR-L 115 BS, comparison of human metabolite pattern and biotransformation with other species].

Following oral administration of 14C labelled 2-[(2-methoxy-4-methylsulfinyl)phenyl]-1H-imidazo[4,5-b]pyridine (AR-L 115 BS) to the rat, rabbit, dog, rhesus monkey, baboon and man the metabolic pattern in plasma and urine was compared and human urinary metabolites were isolated. None of the animal species investigated shows a metabolic pattern identical to that of man. The plasma of rat, dog and rabbit shows wide variation of metabolites with high amounts of two unpolar metabolites of AR-L 115 BS (sulfoxide), namely M0/2 identical with AR-L 114 BS (sulfone with regard to AR-L 115 BS) and M0/1 identical with AR-L 113 BS (sulfide).

The use of stable isotopes to prove the saturable first-pass effect of methoxsalen.

Methoxsalen, administered orally shows a strong, albeit saturable first-pass effect, as demonstrated by classical dose linearity testing and by a new method, using stable isotopes and gas chromatographic mass spectrometric analysis. The therapeutic consequences of the first-pass effect are discussed.

The metabolism of 8-methoxypsoralen in man.

8-Methoxypsoralen is metabolized rapidly and completely in man. Most of the metabolites presently known have their origin in a metabolic attack on the furan moiety yielding an aryl-diol and aryl-acetic-acid and are excreted as conjugates.

[Complication rate under passive and active cure treatment of cardio-circulatory patients (author's transl)].

A comparison between the rate of complications under preferably passive balneotherapeutic cure treatment in 1967 and under preferably active physical training treatment in 1972 gave no significant difference. In spite of an increasing portion of heart patients the complication rate in the cardio-circulatory system under active treatment showed a slight decreasing tendency. On the contrary there were found differences when comparing the temporal frequency distribution of complications under cure treatment of both years.