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二氟尼柳的硫酸盐共轭物:其在大鼠体内的合成及全身稳定性

The sulphate conjugate of diflunisal: its synthesis and systemic stability in the rat.

作者信息

Dickinson R G, King A R, Hansen-Møller J

机构信息

Department of Medicine, University of Queensland, Royal Brisbane Hospital, Australia.

出版信息

Xenobiotica. 1991 May;21(5):635-40. doi: 10.3109/00498259109039503.

Abstract
  1. Diflunisal (DF) is metabolized in rats and humans primarily to its acyl glucuronide, phenolic glucuronide and sulphate conjugates. 2. DF sulphate was synthesized and administered i.v. to conscious bile-exteriorized rats at 10 mg DF equiv./kg. 3. DF sulphate was excreted almost exclusively in urine, and its systemic hydrolysis, monitored by glucuronidation of liberated DF, was quantitatively negligible. 4. Systemic stability of DF sulphate was therefore similar to DF phenolic glucuronide, and contrasted with the systemic instability of DF acyl glucuronide.
摘要
  1. 双氯芬酸(DF)在大鼠和人类体内主要代谢为其酰基葡萄糖醛酸、酚类葡萄糖醛酸和硫酸盐结合物。2. 合成了DF硫酸盐,并以10毫克DF当量/千克的剂量静脉注射给清醒的胆管外引流大鼠。3. DF硫酸盐几乎完全经尿液排泄,通过游离DF的葡萄糖醛酸化监测其全身水解,在数量上可忽略不计。4. 因此,DF硫酸盐的全身稳定性与DF酚类葡萄糖醛酸相似,与DF酰基葡萄糖醛酸的全身不稳定性形成对比。

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