[The pharmacokinetics of hypolipemic agents. 10. The dehalogenation of the hypolipemic agent ciprofibrate]. / Zur Pharmakokinetik von Lipidsenkern, 10. Mitt.: Zweiter Beitrag zur Frage der Dehalogenierung des Lipidsenkers Ciprofibrat.

rac-2 described as a metabolite of rac-1 was synthesized in four steps starting with rac-3. Partial dehalogenation occurs with LiAlH4. A new structure assignment of the resulting stereoisomers resulted from NMR spectroscopy. After oral administration of rac-1 in multiple dose studies to volunteers, rac-2 could not be detected within the limitations of sensitivity of HPLC (UV-detector) in plasma or in urine.

[The pharmacokinetics of hypolipemic agents. 6. Is 2-(4-(2,2-dichlorocyclopropyl)-phenoxy)-propane a metabolite of the hypolipemic ciprofibrate?]. / Zur Pharmakokinetik von Lipidsenkern, 6. Mitt.: Ist 2-(4-(2,2-Dichlorcyclopropyl)-phenoxy)-propan ein Metabolit des Lipidsenkers Ciprofibrat?

According to earlier investigations 2-(4-(2,2-dichlorocyclopropyl)-phenoxy)-propane (4) ought to be a metabolite of the hypolipidemic agent ciprofibrate (1). However, 4 could not be detected in plasma or in urine after administration of a dose of 2100 mg 1 during the course of a multiple-dose-study. Therefore, the compound described in literature must be an unknown one and the existence of 4 as a metabolite of 1 is excluded.

[The pharmacokinetics of antilipemic agents. 5. Is 2-(4-hydroxyphenoxy)-2-methylpropionic acid a metabolite of the antilipemic ciprofibrate?]. / Zur Pharmakokinetik von Lipidsenkern, T. Mitt. Ist 2-(4-Hydroxyphenoxy)-2-methyl-propionsäure ein Metabolit des Lipidsenkers Ciprofibrat?

After oral administration of Ciprofibrate (1) to volunteers (n = 5) only its glucuronide, but no 1 and no 2-(4-Hydroxyphenoxy)-2-methyl-propionic acid (3) could be detected in the fresh urine. Its formation from 1 seems to be impossible on the basis of established biochemical reactions. Therefore, its presence in the urine of volunteers reported by other authors is refuted.