Kuoppamäki M, Sauramo A, Korpela K, Vahteristo M, Kailajärvi M, Lehtinen T, Ellmén J
Orion Pharma, Turku, Finland.
Int J Clin Pharmacol Ther. 2010 Nov;48(11):756-60. doi: 10.5414/cpp48756.
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.
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.
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.
The results of this study demonstrate that a single bedtime dose of LCE 200 provides higher bioavailability of levodopa compared to CR-LC 200.
控释左旋多巴/卡比多巴（CR-LC）常用于对帕金森病（PD）患者的夜间运动症状进行长期控制。与左旋多巴/卡比多巴制剂相比，左旋多巴/卡比多巴/恩他卡朋（LCE）能使左旋多巴具有更高的生物利用度，并且已证明对有剂末现象的PD患者有效。本研究的目的是比较单次晚间剂量（晚上10点给药）的200毫克LCE和200毫克CR-LC后左旋多巴的生物利用度。
这是一项在健康受试者中进行的开放标签、随机、交叉研究。左旋多巴的主要药代动力学（PK）参数为AUC、Cmax、C6h和t1/2。
与200毫克CR-LC相比，单次晚间剂量的200毫克LCE具有显著更好的生物利用度。与左旋多巴生物利用度增加一致，200毫克LCE引起更多恶心。
本研究结果表明，与200毫克CR-LC相比，单次睡前剂量的200毫克LCE可使左旋多巴具有更高的生物利用度。
