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Abstract
An HPLC-EC assay was developed for EXP513, a substituted dihydropyridine inodilator. Inodilators are intended for congestive heart failure by increasing myocardial contractility and increasing peripheral vasodilation by blockage of vascular α-adrenergic receptors. The assay was linear between 5 and 2500 ng/mL in dog plasma and the CV for the intraday reproducibility at 5 ng/mL averaged 10.2 %. The recovery from dog plasma averaged 67 %. A pharmacokinetic study in dogs after PO and IV dosing showed that EXP513 was rapidly absorbed from the Gl tract, highly distributed into tissues and was quickly eliminated. The bioavailability of EXP513 at 30 mg/kg administered as a solution was 13.5 %. The haif-life of EXP513 in dogs after IV and PO administration averaged 2.8 and 2.5 hr, respectively.