Sasahara K, Nitanai T, Habara T, Morioka T, Nakajima E
J Pharm Sci. 1980 May;69(3):261-5. doi: 10.1002/jps.2600690304.
To estimate the absolute bioavailability of oral levodopa, plasma concentrations and urinary excretion of levodopa and its metabolites were determined in beagle dogs and in parkinsonian patients after intravenous and oral drug administration. The absolute bioavailability of orally administered levodopa was estimated to be about 35% in both dogs and patients; however, the total amount absorbed of intact drug and levodopa metabolites was estimated to be 80--90% of the administered dose. Due to the similarities of the pharmacokinetic characteristics of levodopa found in beagle dogs and in humans, beagle dogs can serve as a model to study bioavailability, absorption, and metabolic mechanisms.
为评估左旋多巴口服给药的绝对生物利用度,在比格犬和帕金森病患者静脉注射及口服给药后,测定了左旋多巴及其代谢产物的血浆浓度和尿排泄量。在犬和患者中,口服左旋多巴的绝对生物利用度估计均约为35%;然而,完整药物和左旋多巴代谢产物的总吸收量估计为给药剂量的80%-90%。由于在比格犬和人类中发现的左旋多巴药代动力学特征相似,比格犬可作为研究生物利用度、吸收和代谢机制的模型。