title: Determination of plasma protein binding of propafenone in rats, dogs and humans by highly sensitive gas chromatography-mass spectrometry.
abstract: A highly sensitive method for the determination of propafenone in plasma has been established using gas chromatography-mass spectrometry with the deuterium-labelled compound as an internal standard. Plasma levels as low as 1 ng/ml were measured using 0.5-ml plasma samples. Plasma protein binding of the drug in rats, dogs and humans in vitro and in vivo was determined by the proposed method. About 90% of the drug was bound to the plasma protein in all species in vitro (20-500 ng/ml) and 69-88% in rats, 90-95% in dogs and 77-89% in humans after oral administration of the drug at doses of 50 mg/kg, 5 mg/kg and 200 mg per person, respectively.
authors.forename: S
authors.initials: S
authors.lastname: Higuchi
authors.forename: C
authors.initials: C
authors.lastname: Urano
authors.forename: S
authors.initials: S
authors.lastname: Kawamura
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000097:blood*; D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D004285:Dogs; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D008297:Male; D011405:Propafenone; D011427:Propiophenones / Q000097:blood*; D011485:Protein Binding; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity
chemical_list: D000319:Adrenergic beta-Antagonists; D001798:Blood Proteins; D011427:Propiophenones; D011405:Propafenone