Night-time bioavailability of levodopa/carbidopa/entacapone is higher compared to controlled-release levodopa/carbidopa.
OBJECTIVE
Controlled-release levodopa/carbidopa (CR-LC) is often used to provide prolonged control of night-time motor symptoms in patients with Parkinson's disease (PD). Levodopa/carbidopa/entacapone (LCE) provides higher bioavailability of levodopa compared with levodopa/carbidopa formulations and has been shown to be effective in PD patients with wearing-off symptoms. The aim of this study was to compare the bioavailability of levodopa after a single evening dose (administered at 10 p.m.) of LCE 200 or CR-LC 200.


METHODS
This was an open-label, randomized, crossover study in healthy subjects. The main pharmacokinetic (PK) parameters were AUC, Cmax, C6h and t1/2 of levodopa.


RESULTS
A single evening dose of LCE 200 was associated with significantly better bioavailability compared with CR-LC 200. In line with increased bioavailability of levodopa, LCE 200 induced more nausea.


CONCLUSIONS
The results of this study demonstrate that a single bedtime dose of LCE 200 provides higher bioavailability of levodopa compared to CR-LC 200.
Kuoppamäki
M
M
Orion Pharma, Turku, Finland. mikko.kuoppamaki@orionpharma.com
Sauramo
A
A
Korpela
K
K
Vahteristo
M
M
Kailajärvi
M
M
Lehtinen
T
T
Ellmén
J
J
D000293:Adolescent; D000328:Adult; D000978:Antiparkinson Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002230:Carbidopa / Q000008:administration & dosage; D002396:Catechols / Q000008:administration & dosage*; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D004334:Drug Administration Schedule; D004338:Drug Combinations; D005260:Female; D006207:Half-Life; D006801:Humans; D007980:Levodopa / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D009570:Nitriles / Q000008:administration & dosage*; D013997:Time Factors; D055815:Young Adult
D000978:Antiparkinson Agents; D002396:Catechols; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D009570:Nitriles; C009265:carbidopa, levodopa drug combination; D007980:Levodopa; C071192:entacapone; D002230:Carbidopa