title: The single dose and steady-state pharmacokinetics of a vadocaine tablet in healthy human volunteers.
abstract: Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methyl-piperidyl)-propionanilide hydrochloride; INN vadocaine) is a novel compound with antitussive and local anesthetic actions. In this study, the single dose and steady-state pharmacokinetics of vadocaine hydrochloride tablet were evaluated in 28 healthy volunteers. In part 1, the pharmacokinetics of a single dose of vadocaine hydrochloride tablet were compared with the pharmacokinetics of a vadocaine hydrochloride solution. The peak concentrations of vadocaine were achieved at 1 h both after the tablet and the solution and there were no statistically significant differences in serum concentrations or in pharmacokinetic parameters. In part 2, the steady-state pharmacokinetics of vadocaine tablet were studied using the dosage of 30 mg vadocaine hydrochloride t.i.d. for four days. The peak concentrations of vadocaine were achieved on the 1st day at 1 h (61.5 +/- 6.1 ng/ml) and on the 4th day at 1.5 h (64.5 +/- 7.9 ng/ml). According to the serum concentrations and pharmacokinetic parameters, no cumulation of vadocaine was observed. Also no side-effects were reported during the study. In conclusion, vadocaine used in the tablet form is suitable for multiple dosing and the pharmacokinetic profile is almost similar to vadocaine administered in aqueous solution.
authors.affiliation: Medical Department, Orion Corporation, Orion Pharmaceutica, Kuopio, Finland.
authors.forename: M
authors.initials: M
authors.lastname: Silvasti
authors.forename: P
authors.initials: P
authors.lastname: Karttunen
authors.forename: H
authors.initials: H
authors.lastname: Tukiainen
authors.forename: M
authors.initials: M
authors.lastname: Mykkänen
authors.forename: U
authors.initials: U
authors.lastname: Hänninen
authors.forename: S
authors.initials: S
authors.lastname: Välttilä
mesh_terms: D000328:Adult; D000996:Antitussive Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D010880:Piperidines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D011897:Random Allocation; D012996:Solutions; D013607:Tablets
chemical_list: D000996:Antitussive Agents; D010880:Piperidines; D012996:Solutions; D013607:Tablets; C051410:vadocaine