Department of Neurology, Feinberg School of Medicine, Northwestern University, Chicago, IL, USA.
Parkinson's Disease and Movement Disorders Center, Department of Neurology, Feinberg School of Medicine, Northwestern University, Abbott Hall 11th Floor, 710 North Lake Shore Drive, Chicago, IL, 60611, USA.
Curr Neurol Neurosci Rep. 2016 Apr;16(4):34. doi: 10.1007/s11910-016-0635-8.
Levodopa (LD) is the most effective medication to treat Parkinson's disease (PD). However, motor fluctuations and drug-induced dyskinesia compromise the long-term success of levodopa therapy in PD. These response complications are due, at least in part, to fluctuating LD plasma levels (as a result of erratic gastric emptying, variable jejunal absorption, and most importantly, the short half-life of LD) with standard levodopa formulations. Keeping levodopa concentrations as constant as possible is the target for improving the pharmacokinetics and developing new ways of LD administration. In this article, we review novel oral and non-oral LD formulations including the ones that have successfully completed phase 3 clinical trials and have come to market and ones that are still in earlier phases of clinical development.
左旋多巴（LD）是治疗帕金森病（PD）最有效的药物。然而，运动波动和药物诱导的运动障碍使 LD 治疗 PD 的长期效果受到影响。这些反应并发症至少部分是由于标准 LD 配方中 LD 血浆水平的波动（由于胃排空不规则、空肠吸收变化，最重要的是 LD 半衰期短）引起的。保持 LD 浓度尽可能稳定是改善药代动力学和开发 LD 新给药途径的目标。在本文中，我们综述了新型口服和非口服 LD 制剂，包括已完成 3 期临床试验并已上市的制剂，以及仍处于临床开发早期阶段的制剂。
