PMID: 11932963Apr 5, 2002Paper

Pharmacokinetics and dose proportionality of BMS-204352 after intravenous administration to dogs

Biopharmaceutics & Drug Disposition
Rajesh KrishnaN R Srinivas

Abstract

BMS-204352 is a novel maxi-K channel opener that is being developed for the treatment for stroke. The current study was designed to evaluate the dose proportionality and pharmacokinetics of BMS-204352 in dogs. In an open, three-way crossover study, three beagle dogs received a single intravenous dose of BMS-204352 as a 6-min infusion into the femoral vein at 0.4, 0.9, and 2.0 mg/kg dose levels. There was at least a 1-week washout period between treatments. Serial blood samples were collected for up to 32 h post dose and plasma samples were analyzed for the concentrations of intact BMS-204352 using a validated liquid chromatographic mass spectrometric (LC/MS) method. Pharmacokinetic analysis was performed using a non-compartmental method. Results indicated that peak BMS-204352 concentrations (C(max)) and area under the plasma concentration-time curves (AUC) values increased in a dose proportional manner. Mean residence time (MRT, 18.2-21.9 h) and elimination half-life (T(half), 13.5-17 h) did not change with dose. There was no dose dependency in the mean BMS-204352 total body clearance (CLT, 134-158 ml/h/kg) and mean steady state volume of distribution (VSS, 2839-3291 ml/kg). The high VSS value indicated that BMS-204352 was dist...Continue Reading

References

Oct 1, 1980·Journal of Pharmacokinetics and Biopharmaceutics·S Riegelman, P Collier
Jul 1, 1993·Pharmaceutical Research·B Davies, T Morris
Apr 27, 2001·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J A CheneyT K McIntosh
Mar 14, 2002·Biopharmaceutics & Drug Disposition·Rajesh KrishnaNimish N Vachharajani

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Citations

Sep 6, 2002·Biopharmaceutics & Drug Disposition·Rajesh KrishnaNuggehally Srinivas
Oct 27, 2004·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Donglu ZhangLewis J Klunk

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