Bioavailability of two selegiline hydrochloride tablet products.
The bioavailability of two selegiline HCl (CAS 14611-52-0) tablet products was compared in a single-blind, single-dose, randomised, two-way, cross-over study with 25 healthy volunteers. A test preparation of selegiline HCl (4 x 5 mg tablets) was compared to a reference preparation of selegiline HCl (4 x 5 mg tablets). The volunteers were randomised receiving each treatment once. Two clinic days were separated by a wash-out period of between 6 and 14 days. The variable AUC(0-infinity) was the primary characteristic of the extent of formation (bioavailability) of the selegiline metabolites, desmethylselegiline and methamphetamine. For desmethylselegiline the point estimate (90% confidence interval) of the "test/reference" mean ratio for the variable Cmax is 98.4% (91.2% to 106%), for AUC(0-infinity) 103% (97.6% to 109%), and for Cmax/ AUC(0-infinity) 95.6% (89.4% to 102%). For methamphetamine the point estimate (90% confidence interval) of the "test/reference" mean ratio for the variable Cmax is 101% (96.8% to 105%), for AUC(0-infinity) 102% (95.3% to 109%), and for Cmax/AUC(0-infinity) 99.0% (91.5% to 107%). The results of this study indicate that the test preparation is bioequivalent to the reference preparation with respect to both the rate and extent of formation of desmethylselegiline and methamphetamine.
Müller
F O
FO
Farmovs Research Centre for Clinical Pharmacology and Drug Development, Department of Pharmacology, University of the Orange Free State, Bloemfontein, South Africa.
Schall
R
R
Hundt
H K
HK
Joubert
A
A
Middle
M V
MV
Muir
A R
AR
Duursema
L
L
Groenewoud
G
G
Swart
K J
KJ
D000293:Adolescent; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D018765:Dopamine Uptake Inhibitors / Q000493:pharmacokinetics; D004311:Double-Blind Method; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D008694:Methamphetamine / Q000493:pharmacokinetics; D008996:Monoamine Oxidase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D012642:Selegiline / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D013607:Tablets
D018765:Dopamine Uptake Inhibitors; D008996:Monoamine Oxidase Inhibitors; D013607:Tablets; D012642:Selegiline; D008694:Methamphetamine