Zur Pharmakokinetik von Lipidsenkern, 6. Mitt.: Ist 2‐(4‐(2,2‐Dichlorcyclopropyl)‐phenoxy)‐propan ein Metabolit des Lipidsenkers Ciprofibrat?

Oelschläger, H.; Rothley, D; Hellwich, Karl‐Heinz; Schmidt, Wolfgang

doi:10.1002/ardp.19893221011

Cited by 4 publications

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References 5 publications

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“…So unterliegt rac-1 z. B. keiner Etherspaltung unter Bildung von R,S-4-(2,2-Dichlorcyclopropyl)phenol [2]. Untersuchungen an Probanden hatten bereits früh gezeigt, daß wahrscheinlich nur ein renal eliminiertes O-Acylglucuronid gebildet wird [3], das erstmalig als kristallines Diastereomerengemisch vom Schmelzbereich 67−78°C in hydrophobisierter Form isoliert werden konnte [4].…”

Section: Introductionunclassified

Konjugationsreaktionen von Ciprofibrat bei Menschen und Versuchstieren

Oelschläger

Müller

Hellwich

et al. 2011

Arzneimittelforschung

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An open problem of the lipid lowering agent ciprofibrate (rac-2-[4-(2,2-dichlorocyclopropyl)-phenoxy]-2-methylpropanoic acid, CAS 52214-84-3) is its metabolism concerning the conjugation with amino acids and glucuronic acid. It could be solved by syntheses of the needed reference compounds--unknown up to now--and administration of ciprofibrate to volunteers and rats. Unexpectedly the conjugation compounds with amino acids are stable in vitro and in metabolism. There was no evidence for any conjugation reaction with amino acids by investigating samples of urine and faeces. On the contrary the urine of humans contains 90-97% of beta-O-acylglucuronide, whereas rat urine shows only 10% of the calculated amount.

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Section: Introductionunclassified

Konjugationsreaktionen von Ciprofibrat bei Menschen und Versuchstieren

Oelschläger

Müller

Hellwich

et al. 2011

Arzneimittelforschung

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Ciprofibrat: Erythrozytenverteilungskoeffizient und Bindung an Serumproteine

Czejka

1991

Archiv der Pharmazie

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The in vitro binding of the lipid lowering agent Ciprofibrat (1) to different plasma protein fractions and its red blood-cell partition coefficient were investigated. The binding-rate to albumin and alpha-globulin is dose-dependent (first order kinetic) and amounts to about 95% for albumin and to 25% for alpha-globulin. The affinity of 1 to beta- and gamma-globulin is non-specific and dose-independent (average binding-rate 8% and 10%, respectively). 1 shows only a weak affinity to erythrocytes, therefore, the red blood-cell partition coefficient is 0.02.

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Zur Pharmakokinetik von Lipidsenkern, 10. Mitt.: Zweiter Beitrag zur Frage der Dehalogenierung des Lipidsenkers Ciprofibrat

Oelschläger

Hellwich

Rothley

1994

Archiv der Pharmazie

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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.

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Zur Pharmakokinetik von Lipidsenkern, 6. Mitt.: Ist 2‐(4‐(2,2‐Dichlorcyclopropyl)‐phenoxy)‐propan ein Metabolit des Lipidsenkers Ciprofibrat?

Cited by 4 publications

References 5 publications

Konjugationsreaktionen von Ciprofibrat bei Menschen und Versuchstieren

Konjugationsreaktionen von Ciprofibrat bei Menschen und Versuchstieren

Ciprofibrat: Erythrozytenverteilungskoeffizient und Bindung an Serumproteine

Zur Pharmakokinetik von Lipidsenkern, 10. Mitt.: Zweiter Beitrag zur Frage der Dehalogenierung des Lipidsenkers Ciprofibrat

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