Pharmacokinetic profile of talipexole in healthy volunteers is not altered when it is co-administered with Madopar (co-beneldopa).
OBJECTIVE
To investigate the pharmacokinetics of talipexole hydrochloride tablets and the potential influence of Madopar (benserazide and levodopa combination; co-beneldopa) tablets on talipexole's pharmacokinetics when the two tablets are co-administered orally to healthy Chinese volunteers.


METHODS
A sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to measure talipexole concentration in human plasma in an open-label, randomized, two-way crossover, single-dose study, with 1-week washout period. Healthy Chinese volunteers were randomized to receive talipexole tablets either alone or together with Madopar tablets by oral administration after an overnight fast. Serial blood samples were collected for a period of 36 h after the administration. Pharmacokinetic parameters C(max), t(max), t(1/2z), mean residence time (MRT), AUC(0-tau), AUC(0-infinity), CL(z)/F and V(z)/F were determined under the non-compartmental model. Pharmacokinetic values of talipexole administered alone to the subjects were compared with those administered simultaneously with Madopar to determine whether or not the differences were statistically significant.


RESULTS
The subjects experienced mild gastrointestinal irritation when talipexole was administered alone as well as together with Madopar. For talipexole hydrochloride, there were no significant differences in the pharmacokinetic values between the two administrations. No pharmacokinetic differences based on gender were observed either.


CONCLUSIONS
A single oral dose of Madopar co-administered with talipexole does not significantly change talipexole's pharmacokinetics in human.
Zhang
T T
TT
Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
Song
M
M
Hang
T J
TJ
Xu
X F
XF
Wen
A D
AD
Yang
L
L
Jia
L
L
D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D001381:Azepines / Q000493:pharmacokinetics*; D001545:Benserazide / Q000494:pharmacology*; D002681:China; D002853:Chromatography, Liquid / Q000379:methods; D018592:Cross-Over Studies; D015259:Dopamine Agents / Q000494:pharmacology; D018491:Dopamine Agonists / Q000493:pharmacokinetics*; D004338:Drug Combinations; D004347:Drug Interactions; D005260:Female; D006207:Half-Life; D006801:Humans; D007980:Levodopa / Q000494:pharmacology*; D008297:Male; D013607:Tablets; D053719:Tandem Mass Spectrometry / Q000379:methods
D001381:Azepines; D015259:Dopamine Agents; D018491:Dopamine Agonists; D004338:Drug Combinations; D013607:Tablets; C005177:benserazide, levodopa drug combination; D007980:Levodopa; D001545:Benserazide; C024763:talipexole