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口服左旋多巴的肠道脱羧作用。药理制剂、剂量大小、给药顺序和食物摄入的影响。

Intestinal decarboxylation of orally administered L-dopa. Influence of pharmacological preparations, dose magnitude, dose sequence and food intake.

作者信息

Andersson I, Granerus A K, Jagenburg R, Svanborg A

出版信息

Acta Med Scand. 1975 Nov;198(5):415-20.

PMID:1199816
Abstract

The intestinal decarboxylation and the absorption of orally administered L-dopa have been studied in 20 parkinsonian patients in different conditions. The decarboxylation generally amounted to 50-70% of the dose given, i.e. only 30-50% of orally administered L-dopa reached the general circulation. The shape of the plasma concentration curve varied individually and with the resolvation time of the type of pharmacological preparation given. No obvious difference in the degree of intestinal decarboxylation was observed when tablets with different resolvation times were given but the net absorption of L-dopa was somewhat greater when it was given as a solution. The decarboxylation in the intestinal organs was found to be rather constant at different times of the day. Isocaloric meals, whether rich in protein or carbohydrate, caused a delay in absorption of L-dopa, but did not change the degree of decarboxylation. Diurnal variations in the clinical response to L-dopa, could, thus, not be related to diurnal variations in the decarboxylation in the intestinal organs. The delay in L-dopa absorption after meals may be misinterpreted as lack of response. At dosage with short intervals, the delay may cause an additive effect of two doses.

摘要

在20名帕金森病患者处于不同状态下时,研究了口服左旋多巴的肠道脱羧作用及吸收情况。脱羧作用一般占给药剂量的50 - 70%,即口服的左旋多巴仅有30 - 50%进入体循环。血浆浓度曲线的形状因人而异,且随所给药理制剂类型的溶解时间而变化。给予不同溶解时间的片剂时,未观察到肠道脱羧程度有明显差异,但左旋多巴以溶液形式给药时,其净吸收量略高。发现肠道器官的脱羧作用在一天中的不同时间相当稳定。等热量膳食,无论富含蛋白质还是碳水化合物,都会导致左旋多巴吸收延迟,但不会改变脱羧程度。因此,左旋多巴临床反应的昼夜变化与肠道器官脱羧作用的昼夜变化无关。餐后左旋多巴吸收延迟可能会被误解为无反应。在短间隔给药时,这种延迟可能会导致两剂药物的叠加效应。

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