在健康受试者口服延胡索酸酯的药物动力学。

文章的细节

引用

复制到剪贴板

Litjens NH, Burggraaf J,范Strijen E, van Gulpen C,玛蒂H,舒梅克RC, van Dissel JT,含硫的HB, Nibbering PH

在健康受试者口服延胡索酸酯的药物动力学。

Br中国新药杂志。2004年10月,58 (4):429 - 32。doi: 10.1111 / j.1365-2125.2004.02145.x。

PubMed ID

15373936 (在PubMed

]

文摘

目的:在健康受试者延胡索酸酯的药物动力学特征。方法:十个受试者接受一个延胡索酸酯平板dimethylfumarate(包含120毫克和95毫克的calcium-monoethylfumarate)标准化后的禁食状态,早餐以随机的顺序。之前和在固定间隔剂量后,血液样本被吸引和monomethylfumarate的浓度,生物活性代谢物,以及dimethylfumarate和反丁烯二酸测定用高效液相色谱法。结果:延迟时间后,瞬时增加血液中血清浓度monomethylfumarate被观察到,而dimethylfumarate和反丁烯二酸浓度仍低于检出限。tlag 240分钟(60 - 603分钟;95%可信区间(CI) 139、471)短后,平板电脑是一个一夜之间迅速(90分钟;射程60 - 120分钟;95%可信区间66、107)比用早餐(300分钟;射程180 - 723分钟;95%可信区间0,1002)。 The tmax was 241 min (range 60-1189 min, 95% CI 53, 781) shorter when the tablet was taken after an overnight fast (182 min; range 120-240 min; 95% CI 146, 211) than when taken with breakfast (361 min; range 240-1429 min; 95% CI 0, 1062). The mean Cmax for monomethylfumarate in the blood of fasting subjects was to 0.84 mg l(-1) (range 0.37-1.29 mg l(-1); 95% CI 0.52, 1.07) and did not differ from that in fed subjects (0.48 mg l(-1); range 0-1.22 mg l(-1); 95% CI 0, 5.55). CONCLUSIONS: The pharmacokinetics of monomethylfumarate in healthy subjects after a single tablet of fumarate are highly variable, particularly after food intake. Further experiments exploring the pharmacokinetics of oral fumarates are warranted in order to elucidate the mechanisms underlying variability in response in patients.

DrugBank数据引用了这篇文章

药物

Diroximel延胡索酸酯