Pharmacokinetics and Pharmacodynamics of Oral Heparin Solid Dosage Form in Healthy Human Subjects

Mousa, Shaker A.
Fuming Zhang,
Aljada, Ahmad
Chaturvedi, Seema
Takieddin, Majde
Haifeng Zhang,
Lianli Chi,
Cristina Castelli, M.
Friedman, Kristen
Goldberg, Michael M.
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Biology , Chemistry and chemical biology , Chemical and biological engineering , Biomedical engineering
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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.
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.
Journal of Clinical Pharmacology, 47, 1508-1520
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The Linhardt Research Labs.
The Shirley Ann Jackson, Ph.D. Center for Biotechnology and Interdisciplinary Studies (CBIS)
American College of Clinical Pharmacology (ACCP)
The Linhardt Research Labs Online Collection
Rensselaer Polytechnic Institute, Troy, NY
Journal of Clinical Pharmacology
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