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Reversible Crystallization of Argatroban after Subcutaneous Application in Pigs
Joint Authors
Source
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-6, 6 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-09-03
Country of Publication
Egypt
No. of Pages
6
Main Subjects
Abstract EN
Argatroban is a thrombin inhibitor used as anticoagulant in patients with heparin-induced thrombocytopenia.
It is usually administered as an intravenous bolus followed by infusion.
Nevertheless, its pharmacokinetics after subcutaneous administration is unknown.
The aim of this study was to assess the pharmacokinetics of two different formulations of argatroban in pigs after subcutaneous administration.
Antithrombotic activity in plasma was determined by ecarin chromogenic assay.
To visualize the formation of crystals, argatroban was administered to rats into the subcutaneous tissue exposed after removing the skin, and the injection site was photographed at different times.
After subcutaneous administration of a sorbitol/ethanol formulation of argatroban in pigs was observed a slow absorption phase was followed by long-lasting levels of this inhibitor.
Cmax and AUC(0-24) showed dose-dependent increases, while elimination half-life and tmax value did not change significantly with dose.
In contrast, saline-dissolved argatroban showed a faster absorption phase followed by a shorter elimination half-life.
Argatroban dissolved in sorbitol/ethanol leads to long-lasting plasma levels due to the formation and permanent dissolution of a crystalline depot at the injection place.
This represents a simple way to deliver argatroban continuously over an extended period which can be beneficial for prophylaxis or treatment of chronic coagulations disorders.
American Psychological Association (APA)
Lopez, Mercedes& Nowak, Goetz. 2012. Reversible Crystallization of Argatroban after Subcutaneous Application in Pigs. Thrombosis،Vol. 2012, no. 2012, pp.1-6.
https://search.emarefa.net/detail/BIM-480778
Modern Language Association (MLA)
Lopez, Mercedes& Nowak, Goetz. Reversible Crystallization of Argatroban after Subcutaneous Application in Pigs. Thrombosis No. 2012 (2012), pp.1-6.
https://search.emarefa.net/detail/BIM-480778
American Medical Association (AMA)
Lopez, Mercedes& Nowak, Goetz. Reversible Crystallization of Argatroban after Subcutaneous Application in Pigs. Thrombosis. 2012. Vol. 2012, no. 2012, pp.1-6.
https://search.emarefa.net/detail/BIM-480778
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-480778