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不同盐形式萘呋胺酯的血浆浓度及相对生物利用度。

Plasma concentrations and relative bioavailability of naftidrofuryl from different salt forms.

作者信息

Walmsley L M, Taylor T, Wilkinson P A, Brodie R R, Chasseaud L F, Alun-Jones V, Hunter J O

出版信息

Biopharm Drug Dispos. 1986 Jul-Aug;7(4):327-34. doi: 10.1002/bdd.2510070403.

Abstract

The relative bioavailability of the vasodilator naftidrofuryl from formulations containing its oxalate or citrate salt has been estimated using a specific HPLC assay, and a less specific fluorimetric assay, to measure plasma drug concentrations. The conclusions of the study were the same irrespective of the assay employed. The relative rate, but not the extent, of bioavailability of naftidrofuryl from the citrate salt (peak 1096 ng ml-1 at 0.76 h) was marginally greater (p = 0.003) than that from the oxalate salt (peak 922 ng ml-1 at 0.94 h). The degree of intersubject variability was similar after administration of either salt form. The mean half-life of naftidrofuryl was 1.8 h and its mean residence time was 2.5 h.

摘要

已使用特定的高效液相色谱法(HPLC)和特异性稍低的荧光测定法来测量血浆药物浓度,以此估算含有草酸萘呋胺酯或枸橼酸萘呋胺酯制剂中血管舒张剂萘呋胺的相对生物利用度。无论采用哪种测定方法,该研究的结论都是相同的。枸橼酸盐中萘呋胺的相对生物利用速率(而非程度)(在0.76小时时峰值为1096 ng/ml)略高于草酸盐(在0.94小时时峰值为922 ng/ml)(p = 0.003)。服用任何一种盐形式后,受试者间的变异程度相似。萘呋胺的平均半衰期为1.8小时,平均驻留时间为2.5小时。

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