title: Kinetics of buccal absorption of propafenone single oral loading dose in healthy humans.
abstract: Buccal absorption has an advantage when compared with other administration routes because of its rapid onset of action. We examined the pharmacokinetics of buccal-absorbed propafenone in healthy humans. 1. After a single oral administration of 150 mg of propafenone, the average peak concentration of propafenone was 27.9+/-2.5 ng/ml, and that of 5-hydroxypropafenone was 61.7+/-6.6 ng/ml (n=5). The times to reach peak serum concentrations of propafenone and 5-hydroxypropafenone were 1.8+/-0.1 hr and 1.5+/-0.2 hr, respectively. 2. After a buccal absorption of 150 mg of propafenone, the time to reach peak serum concentration of propafenone was 16.9+/-2.3 min (n=8). The average peak concentration of propafenone was 30.4+/-1.4 ng/ml (n=8), and the concentrations of 5-hydroxypropafenone were below the detection limit in all subjects. The rapid upstroke of serum concentrations of propafenone by buccal administration may cause rapid onset of pharmacological conversion.
authors.affiliation: Department of Pharmacy, Tama-Nagayama Hospital, Tokyo, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Sasaki
authors.forename: S
authors.initials: S
authors.lastname: Koumi
authors.forename: R
authors.initials: R
authors.lastname: Sato
authors.forename: M
authors.initials: M
authors.lastname: Murata
authors.forename: K
authors.initials: K
authors.lastname: Nagasawa
authors.forename: E
authors.initials: E
authors.lastname: Sakurai
authors.forename: N
authors.initials: N
authors.lastname: Hikichi
authors.forename: H
authors.initials: H
authors.lastname: Hayakawa
mesh_terms: D000042:Absorption / Q000502:physiology*; D000278:Administration, Buccal; D000328:Adult; D000368:Aged; D006801:Humans; D008297:Male; D008875:Middle Aged; D009061:Mouth Mucosa / Q000378:metabolism*; D011405:Propafenone / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D011405:Propafenone