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水溶性纤维卵叶车前子壳在重复给药后可提高左旋多巴(与卡比多巴合用)的生物利用度。

The hydrosoluble fiber Plantago ovata husk improves levodopa (with carbidopa) bioavailability after repeated administration.

作者信息

Diez M Jose, Garcia Juan J, Prieto Carlos, Fernandez Nelida, Sahagun Ana, Sierra Matilde

机构信息

Area de Farmacologia, Universidad de Leon, 24071, Leon, Spain.

出版信息

J Neurol Sci. 2008 Aug 15;271(1-2):15-20. doi: 10.1016/j.jns.2008.03.007. Epub 2008 May 12.

Abstract

The influence of treatment duration (7 or 14 days) with Plantago ovata husk/levodopa/carbidopa in the bioavailability and other pharmacokinetic parameters of levodopa were evaluated in rabbits. Fiber was administered at two different doses, 100 and 400 mg/kg, and the dosage of levodopa/carbidopa was 20:5 mg/kg. These doses were administered once a day. When 100 mg/kg of fiber was administered, the mean AUC value obtained for levodopa increased 20.2% from day 1 to day 7, and 27.2% from day 1 to day 14; C(max) was 8.6% higher on day 7 and 11.7% higher on day 14. When administering 400 mg/kg of fiber, the increase in AUC values was 17.6% on day 7 and 24.9% on day 14, and that of C(max) 11.1% on day 7 and 11.3% on day 14. The concentration determined immediately before drug administration (C(min)) increased progressively with the duration of treatment, and the highest increase (53.2%) was observed on day 14 with 100 mg/kg of fiber. There was also a delay in levodopa elimination (higher MRT and lower Cl) in a fiber-dose dependent manner. In summary, we found that there was an improvement in the extent of levodopa absorbed with higher final concentrations and that levodopa elimination was slower with the administration of P. ovata husk.

摘要

在兔子中评估了卵叶车前子壳/左旋多巴/卡比多巴治疗持续时间(7天或14天)对左旋多巴生物利用度和其他药代动力学参数的影响。以两种不同剂量(100和400mg/kg)给予纤维,左旋多巴/卡比多巴的剂量为20:5mg/kg。这些剂量每天给药一次。当给予100mg/kg纤维时,左旋多巴的平均AUC值从第1天到第7天增加了20.2%,从第1天到第14天增加了27.2%;第7天C(max)高8.6%,第14天高11.7%。当给予400mg/kg纤维时,AUC值在第7天增加17.6%,在第14天增加24.9%,C(max)在第7天增加11.1%,在第14天增加11.3%。给药前即刻测定的浓度(C(min))随治疗持续时间逐渐增加,在第14天给予100mg/kg纤维时观察到最高增加(53.2%)。左旋多巴消除也存在延迟(较高的MRT和较低的Cl),且呈纤维剂量依赖性。总之,我们发现随着最终浓度升高,左旋多巴吸收程度有所改善,并且给予卵叶车前子壳后左旋多巴消除更慢。

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