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美多芭HBS在患者中的单剂量药代动力学以及食物和抗酸剂对志愿者中美多芭HBS吸收的影响。

Single-dose pharmacokinetics of Madopar HBS in patients and effect of food and antacid on the absorption of Madopar HBS in volunteers.

作者信息

Malcolm S L, Allen J G, Bird H, Quinn N P, Marion M H, Marsden C D, O'Leary C G

机构信息

Roche Products Ltd, Welwyn Garden City, Hertfordshire, UK.

出版信息

Eur Neurol. 1987;27 Suppl 1:28-35. doi: 10.1159/000116172.

Abstract

Pharmacokinetic studies in parkinsonian patients and healthy volunteers have shown that Madopar HBS behaves as a slow-release formulation of L-dopa and benserazide. In comparison with standard Madopar the rate of absorption is reduced, providing lower peak concentrations of L-dopa. The drug is released and absorbed over a period of 4-5 h, thus maintaining substantial plasma concentrations for 6-8 h after dosing. Although the bioavailability after oral dosing is reduced as compared with standard Madopar (60-70%), this difference seems to be due to incomplete absorption rather than altered disposition of the drug. The presence or absence of food in the stomach has no effect on the absorption of L-dopa from Madopar HBS, but administration of antacids further reduces the bioavailability (45%).

摘要

帕金森病患者和健康志愿者的药代动力学研究表明,美多芭缓释片(Madopar HBS)表现为左旋多巴和苄丝肼的缓释制剂。与标准美多芭相比,其吸收速率降低,左旋多巴的峰值浓度较低。药物在4 - 5小时内释放和吸收,给药后6 - 8小时内维持较高的血浆浓度。虽然口服给药后的生物利用度与标准美多芭相比有所降低(60 - 70%),但这种差异似乎是由于吸收不完全而非药物处置改变所致。胃内有无食物对美多芭缓释片中左旋多巴的吸收没有影响,但服用抗酸剂会进一步降低生物利用度(45%)。

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