药物动力学和生物利用度Sinemet CR:人类研究的摘要。

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叶KC,布什8月TF, DF, Lasseter KC,井DG,施瓦茨年代,史密斯我,提图斯

药物动力学和生物利用度Sinemet CR:人类研究的摘要。

神经学。1989年11月,39(11增刊2):25-38。

PubMed ID

2685649 (在PubMed

]

文摘

Sinemet CR的药物动力学,包含左旋多巴和卡比多巴的缓释制剂,研究在健康年轻和老年志愿者和帕金森症患者。Sinemet CR产生持续的等离子体水平左旋多巴、卡比多巴、3甲基多巴比传统Sinemet。在老年人中,相应的稳态等离子体水平波动与Sinemet CR窄范围比Sinemet管理。结果表明Sinemet CR左旋多巴的生物利用度为71%,与这些学科的Sinemet的生物利用度为99%。卡比多巴Sinemet CR的生物利用度为58%相对于Sinemet。2方案之间的系统性脱羧酶抑制相当的左旋多巴的肾清除率。左旋多巴的吸收较慢,与Sinemet Sinemet CR比所持续的时间更长。食品增加了左旋多巴的生物利用度Sinemet CR。这种增长是归因于增加胃保留时间。没有发生dose-dumping Sinemet CR nonfasting或空腹状态。左旋多巴的生物利用度较低比老年志愿者的青年志愿者。 This was attributed to an age-related decrease in gastric emptying and in 1st-pass metabolic decarboxylation in the gastrointestinal (GI) tract. In parkinsonian patients, as in healthy subjects, the Sinemet CR formulation produced more sustained levodopa plasma levels. These patients required a higher total daily dosage of Sinemet CR than of Sinemet for control of parkinsonian symptoms, but less frequent dosing was required during chronic therapy. Peak plasma levodopa levels increased proportionately with increasing Sinemet CR dosage. These observations were consistent with the pharmacokinetic characteristics of the formulation.

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药物

卡比多巴