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

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...

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Bibliographic Details
Published in:Journal of clinical pharmacology 2007-12, Vol.47 (12), p.1508-1520
Main Authors: Mousa, Shaker A., Zhang, Fuming, Aljada, Ahmad, Chaturvedi, Seema, Takieddin, Majde, Zhang, Haifeng, Chi, Lianli, Castelli, M. Cristina, Friedman, Kristen, Goldberg, Michae M., Linhardt, Rober J.
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
anticoagulants
Caprylates - chemistry
Capsules
Chromatography, High Pressure Liquid
Cross-Over Studies
Gelatin - chemistry
Health aspects
Heparin
heparin composition
Heparin, Low-Molecular-Weight - administration & dosage
Heparin, Low-Molecular-Weight - chemistry
Heparin, Low-Molecular-Weight - pharmacokinetics
Humans
Injections, Intravenous
Injections, Subcutaneous
Male
Middle Aged
Oral heparin
pharmacodynamics
Pharmacokinetics
Pharmacology
solid dosage form
Spectrometry, Mass, Electrospray Ionization
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Summary: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.
ISSN:0091-2700
1552-4604
DOI:10.1177/0091270007307242