Jejunal permeability and hepatic extraction of fluvastatin in humans

Clinical Pharmacology and Therapeutics
A LindahlH Lennernäs

Abstract

The primary objective was to investigate the effective permeability and the hepatic extraction of fluvastatin, a new 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, during a jejunal perfusion in humans. The secondary objective was to investigate the relationship between human jejunal effective permeability values and physicochemical properties for four different drugs. Nine healthy male volunteers were included in the study, which consisted of two sequential study parts. In the first part, the jejunal effective permeability of fluvastatin, antipyrine, metoprolol, and atenolol was assessed with use of the regional jejunal perfusion approach (150 minutes, 2.0 ml/min). After a washout period of at least 5 days, the same subjects received an intravenous infusion of fluvastatin (20 minutes, 2.0 mg). Plasma samples were taken in both parts of the study and were analyzed for the content of fluvastatin. The mean hepatic extraction of fluvastatin was 67% after the jejunal perfusion and 73% after the intravenous infusion. The half-life of fluvastatin was approximately 60 minutes after both administration routes. The jejunal effective permeability and the fraction absorbed both correlated (r2 = 0.968, p < 0.05; and r2...Continue Reading

References

Jul 1, 1992·Journal of Clinical Pharmacology·F L TseA Troendle
Feb 1, 1990·British Journal of Clinical Pharmacology·S M SinghviD A Willard
Jan 1, 1990·Drug Metabolism Reviews·D E Duggan, S Vickers
Apr 4, 1986·Science·M S Brown, J L Goldstein
Jan 1, 1986·The Journal of Membrane Biology·A Walter, J Gutknecht
Oct 1, 1995·Gastroenterology·R M SchwartzM D Levitt
Oct 1, 1995·Clinical Pharmacology and Therapeutics·C TransonP Dayer
Mar 1, 1995·Pharmaceutical Research·H LennernäsR Hällgren
Oct 1, 1993·The Journal of Pharmacy and Pharmacology·R D Purves
Sep 1, 1993·Journal of Pharmaceutical Sciences·F L TseW S Yardley
Nov 21, 1993·Biochimica Et Biophysica Acta·K Ziegler, S Hummelsiep
Mar 1, 1993·British Journal of Clinical Pharmacology·H LennernäsL K Paalzow
May 1, 1996·Clinical Pharmacology and Therapeutics·K E ThummelG R Wilkinson

❮ Previous
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Citations

Mar 17, 2001·British Journal of Pharmacology·K BogmanJ Drewe
Aug 16, 2006·Expert Opinion on Drug Safety·Atul TiwariKasim Mookhtiar
Oct 31, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·H Lennernäs
May 8, 2007·International Journal of Pharmaceutics·Ebba BergmanHans Lennernäs
Apr 6, 2005·The Journal of Pharmacy and Pharmacology·Hans Lennernäs, Bertil Abrahamsson
Dec 19, 2016·Biochimica Et Biophysica Acta. Biomembranes·L F GaliullinaV V Klochkov
Aug 18, 2001·Journal of Cardiovascular Pharmacology and Therapeutics·R SiekmeierW Jaross
May 23, 2001·Clinical Pharmacokinetics·C D Scripture, J A Pieper
Oct 9, 2003·Clinical Pharmacokinetics·Hans Lennernäs
Feb 23, 2019·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Keith A RiccardiRui Li
Oct 31, 2009·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Takao WatanabeYuichi Sugiyama
Aug 6, 2014·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Rui LiHugh A Barton
Jul 20, 2007·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Kazuho SakamotoJunko Kimura
Feb 13, 2003·British Journal of Clinical Pharmacology·Christer TannergrenHans Lennernäs
Jul 1, 1997·The Journal of Pharmacy and Pharmacology·H Lennernäs
Jul 27, 1999·British Journal of Clinical Pharmacology·R SandströmH Lennernäs
Aug 28, 1998·The Journal of Pharmacy and Pharmacology·A LindahlH Lennernäs
Jun 14, 2003·The Journal of Pharmacy and Pharmacology·Hans Lennernäs
Nov 4, 2020·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Yi-An BiManthena V S Varma
Nov 25, 2020·International Journal of Molecular Sciences·Christopher MurphyAlvaro Garcia
Apr 2, 1998·Journal of Pharmaceutical Sciences·A L UngellH Lennernäs
Apr 21, 1998·Journal of Pharmaceutical Sciences·H Lennernäs
Aug 1, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yoshie MasaokaShinji Yamashita
Sep 29, 2020·Journal of Medicinal Chemistry·David A TessManthena V S Varma
Dec 17, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Anna LundahlHans Lennernäs

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