Multiple dose pharmacokinetic study of cicletanine in healthy volunteers.
Cicletanine hydrochloride, a furopyridine derivative, is a new type of antihypertensive drug. A pharmacokinetic study was performed in 8 non-patient subjects who were given 50 mg oral daily doses for 7 days. Cicletanine plasma levels were measured by HPLC. An open bicompartmental model was fitted to the experimental data using an extended non-linear regression method. Additionally plasma levels obtained after the first administration were used to determine pharmacokinetic parameters, which were considered as representative of a single dose administration. The results showed no significant differences between parameters estimated after the first dose and repeated dosing. Mean half-life values were 7.3 and 7.9 hours respectively. The mean peak and trough concentration values in the last interval studied were 1730 and 44 ng/mL respectively. The accumulation index was negligible (1.15). The similarity in the values obtained after the first and repeated administration suggests that cicletanine displays a linear pharmacokinetic behaviour at a dose of 50 mg.
Peraire
C
C
Pharmacokinetic Department, LASA Laboratories, S.A., Sant Feliu de Llobregat, Spain.
Torrent
J
J
Pruñonosa
J
J
Azcona
O
O
Nomen
M
M
Obach
R
R
D000328:Adult; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D004232:Diuretics / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D008297:Male; D008954:Models, Biological; D011725:Pyridines; D013056:Spectrophotometry, Ultraviolet
D000959:Antihypertensive Agents; D002214:Capsules; D004232:Diuretics; D011725:Pyridines; C038068:cicletanine