非布索坦需要空腹吃吗？

(febuxostat) is a tablet, an anti-gout drug, and the first non-xanthine new generation xanthine oxidase inhibitor. It inhibits the activity of xanthine oxidase, prevents and reduces the synthesis of uric acid from hypoxanthine and xanthine, and thereby reduces blood uric acid. So, in order to fully exert its efficacy, does febuxostat need to be taken on an empty stomach?

The answer is no. Because the pharmacokinetic study of febuxostat shows that the drug is well absorbed after oral administration (bioavailability is 84%), and it is believed that the absorption of febuxostat from food or antacids is not clinically relevant, therefore, patients do not need to consider food intake when taking febuxostat, that is, it can be taken on an empty stomach or not.

In a 14-day study of febuxostat at 80 mg daily in healthy subjects, the absolute bioavailability of febuxostat was 84%, with a time to peak of 1.5 h and a peak concentration of 3.2 μg/mL. The plasma protein binding rate of febuxostat is as high as 99.2%, the average apparent volume of distribution Vd is 33 to 64 L, and the 24 h AUC is approximately 13.31 μg/(h·mL).

In vivo and in vitro studies have shown that febuxostat is mainly metabolized through oxidation and glucuronide acidification pathways, with an elimination half-life t of 5 to 8 hours and a clearance rate of CL of 10 to 12 L/h. Among them, 2% to 44% of the dose is metabolized by glucuronidation, 1% to 6% is directly excreted from the kidneys in the form of original drug, and 2% to 8% is oxidized by P450 enzymes in the liver. Its five metabolic oxidation products still have strong inhibitory power on xanthine oxidase, and their activity is equivalent to that of febuxostat.

In addition, some scholars gave it orally at a dose of 80 mg/d to subjects with normal liver function and those with liver and kidney damage. The study results showed that (febuxostat) can be taken by patients with liver and kidney damage.

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