Intranasal absorption of the platelet glycoprotein IIb/IIIa receptor antagonist, DMP 755, and the effect of anesthesia on nasal bioavailability

Journal of Pharmaceutical Sciences
M A HussainS A Mousa

Abstract

Intranasal absorption and bioavailability of DMP 755, a peptidomimetic, platelet glycoprotein IIb/IIIa receptor antagonist, were examined in anesthetized and lightly sedated dogs. Nasal bioavailability was determined by measuring plasma concentrations relative to those after intravenous dosing. DMP 755 is an ester prodrug, and bioavailability reflects concentrations of the acid hydrolysis product. Nasal bioavailability in dogs anesthetized with pentobarbital was 85 +/- 4%, whereas in dogs anesthetized with the short-acting anesthetic propofol, bioavailability was 32 +/- 7%. Nasal bioavailability was greater than the reported oral bioavailability of DMP 755 in dogs, and was quite consistent. Because anesthesia affects nasal bioavailability, an effect that may depend on the absorption half-life of the test compound, a conscious or lightly sedated animal model is preferred.

References

Nov 11, 1992·Trends in Pharmacological Sciences·A J NicholsJ Samanen
Jul 1, 1991·Pharmaceutical Research·N G SchipperF W Merkus
Aug 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·Z M RuggeriT S Zimmerman
Oct 16, 1986·The New England Journal of Medicine·D J FitzgeraldG A FitzGerald
Jun 1, 1985·Journal of the American College of Cardiology·V FusterJ H Chesebro
Sep 1, 1981·American Heart Journal·M D RubensteinD C Harrison

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Citations

May 17, 2005·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Joke P M in 't VeenFrans W H M Merkus
Dec 1, 2001·Expert Opinion on Biological Therapy·G S TirucheraiA K Mitra
Dec 12, 2003·Journal of Drug Targeting·Mascha P Van den BergFrans W H M Merkus
Jun 6, 2009·Journal of Pharmaceutical Sciences·Neil R Mathias, Munir A Hussain
Sep 2, 2003·Journal of Pharmaceutical Sciences·Paul A MoenchRonald L Smith

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