Pharmacokinetics and Pharmacodynamics of Oral Heparin Solid Dosage Form in Healthy Human Subjects
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Authors
Mousa, Shaker A.
Fuming Zhang,
Aljada, Ahmad
Chaturvedi, Seema
Takieddin, Majde
Haifeng Zhang,
Lianli Chi,
Cristina Castelli, M.
Friedman, Kristen
Goldberg, Michael M.
Issue Date
2007-12-01
Type
Article
Language
ENG
Keywords
Biology , Chemistry and chemical biology , Chemical and biological engineering , Biomedical engineering
Alternative Title
Abstract
The present investigation determined the molecular structure and the pharmacokinetic and pharmacodynamic profiles of oral unfractionated heparin containing oral absorption enhancer sodium N-[8-(2-hydroxybenzoyl) amino]caprylate, salcaprozate sodium (SNAC) and assessed the safety and tolerability of the orally dosed heparin solid dosage form versus other routes. Sixteen healthy men were included in this single-dose, 3-way crossover, randomized, open-label study. Disaccharide compositional analysis was performed using capillary high-performance liquid chromatography with electrospray ionization mass spectrometry detection. The pharmacodynamics of heparin were obtained from analysis of plasma anti-factor Xa, anti-factor IIa, activated partial thromboplastin time, and total tissue factor pathway inhibitor data. The molecular weight properties and the disaccharide composition of orally administered unfractionated heparin/SNAC and parenterally administered unfractionated heparin are identical and consistent with the starting pharmaceutical standard heparin. Furthermore, the anti-factor Xa/anti-factor IIa ratio achieved is of approximately 1:1. This is the first true pharmacokinetic study to measure the chemical compositions of heparin administered by different routes.
Description
Journal of Clinical Pharmacology, 47, 1508-1520
Note : if this item contains full text it may be a preprint, author manuscript, or a Gold OA copy that permits redistribution with a license such as CC BY. The final version is available through the publisher’s platform.
Note : if this item contains full text it may be a preprint, author manuscript, or a Gold OA copy that permits redistribution with a license such as CC BY. The final version is available through the publisher’s platform.
Full Citation
Pharmacokinetics and Pharmacodynamics of Oral Heparin Solid Dosage Form in Healthy Human Subjects, S. A. Mousa, F. Zhang, A. Aljada, S. Chaturvedi, M. Takieddin, H. Zhang, L. Chi, E. Arbit, M. C. Castelli, M.M. Goldberg, R. J. Linhardt, Journal of Clinical Pharmacology, 47, 1508-1520, 2007.
Publisher
American College of Clinical Pharmacology (ACCP)
Terms of Use
Journal
Volume
Issue
PubMed ID
DOI
ISSN
15524604
912700
912700