Pharmacokinetic studies with a dual-release formulation of levodopa, a novel principle in the treatment of Parkinson's disease
Pharmacokinetic studies with a dual-release formulation of levodopa, a novel principle in the treatment of Parkinson's disease
复制标题
DOI：
10.1159/000007918
复制
发表时间：
1998-01-01
影响因子：
2.4
通讯作者：
Gasser, UE
中科院分区：
文献类型：
--
作者：
Dingemanse, J;Kleinbloesem, CH;Gasser, UE
本文报道的两项研究的目的是研究在给予具有双相药物递送特征的新型左旋多巴/苄丝肼制剂（Medopar（R）DR）后，片剂破碎和食物对左旋多巴和3-O-甲基多巴（3-OMD）的药代动力学的影响。两项研究均采用开放标签、随机、双向交叉设计，在12名健康年轻受试者中进行。左旋多巴和3-OMD在一片完整片剂或两片减半片剂后的药代动力学非常相似，平均C-max和t（max）分别为1.9 mg 1（-1）和1.2 h。在标准早餐后给予该制剂不影响左旋多巴的吸收程度，但增加了吸收速率。进食状态下的C-max和t（max）平均值分别为2.1 mg 1（-1）和1.3 h，空腹状态下为1.5 mg 1（-1）和2.5 h。食物的存在并没有显着影响高原左旋多巴水平约1和3小时后摄入。总之，新的左旋多巴/苄丝肼制剂在健康受试者中的释放特性仅在很小程度上受以下物质的伴随摄入的影响：
The objectives of the two studies reported here were the investigation of the influence of tablet breaking and food on the pharmacokinetics of levodopa and 3-O-methyldopa (3-OMD) after administration of a new levodopa/benserazide formulation with a biphasic drug delivery profile (Madopar(R) DR). Both studies had an open-label, randomised, two-way crossover design and were conducted in 12 healthy young subjects. The pharmacokinetics of levodopa and 3-OMD after one intact or two halved tablets were very similar with average C-max and t(max) 1.9 mg 1(-1) and 1.2 h, respectively. Administration of the formulation after a standard breakfast did not influence the extent of levodopa absorption but increased the absorption rate. C-max and t(max) were on average 2.1 mg 1(-1) and 1.3 h, respectively, in the fed condition and 1.5 mg 1(-1) and 2.5 h in the fasted condition. The presence of food did not markedly affect the plateau in levodopa levels between about 1 and 3 h after intake. In conclusion, the release characteristics in healthy subjects of the new levodopa/benserazide formulation are influenced only to a minor extent by concomitant intake of