Pharmacokinetics and bioavailability of a sustained-release diltiazem formulation (Mono-Tildiem LP 300 MG) after repeated administration in healthy volunteers.
The usual dosage regimen of diltiazem (Tildiem) is 60 mg 3-4 times a day. A sustained-release formulation has been developed (Mono-Tildiem LP 300 mg) in order to allow a single daily administration. Two repeated dosing studies were performed in healthy volunteers. The absolute bioavailability of sustained-release diltiazem LP 300 mg was investigated using concomitant i.v. administration of 13C-labelled drug: absolute bioavailability of the "once a day" formulation was 35%. The second study compared sustained-release diltiazem LP 300 mg with the standard formulation of diltiazem. The results showed that the diltiazem plasma concentrations obtained after the LP formulation remained stable between 2 and 14 h after administration and were compatible with a once a day administration. Relative bioavailability of sustained-release diltiazem LP 300 mg was 79.3% compared with diltiazem. Therefore, a unitary dose of sustained-release diltiazem LP 300 mg was chosen as the dose equivalent to the daily dose administered with the standard diltiazem formulation.
Bianchetti
G
G
Department of Chemical and Pharmaceutical Development, Synthélabo Recherche (LERS), Bagneux, France.
Dubruc
C
C
Sultana
V
V
Houin
G
G
Rosenzweig
P
P
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D004110:Diltiazem / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D010599:Pharmacokinetics; D013997:Time Factors; D014838:Volunteers
D004110:Diltiazem