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  • Title: Anticoagulant activity of a peptide boronic acid thrombin inhibitor by various routes of administration in rats.
    Author: Hussain MA, Knabb R, Aungst BJ, Kettner C.
    Journal: Peptides; 1991; 12(5):1153-4. PubMed ID: 1800952.
    Abstract:
    The peptide boronic acid analog Ac-(D)Phe-Pro-boroArg-OH (I) is a potent and selective inhibitor of thrombin. The objective of this study was to determine whether I is active orally or when administered by alternative transmucosal routes. The measured effect was the time for clotting of plasma after initiation with thrombin. With this assay there was a narrow window from no measurable effect to the maximal effect, a clotting time greater than 300 seconds. Intravenous I at a 0.15 mg/kg dose in rats, a nasal 0.45 mg/kg dose, and 3 mg/kg doses administered orally, colonically, or rectally all produced maximal effects. Therefore, although bioavailability cannot be estimated, it is demonstrated that this peptide analog was absorbed by each of these routes.
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