代谢
这种药物的有效代谢物是替唑沙尼(去乙酰硝唑沙尼)。硝唑沙尼代谢途径的初始反应是水解成替唑沙尼,随后通过结合,主要是通过葡萄糖醛酸化成替唑沙尼葡萄糖醛酸苷。这种药物的口服悬浮液生物利用度与口服片剂不相等。与片剂相比,悬浮液的生物利用度为70%。与食物一起服用时,血浆中替唑沙尼和替唑沙尼葡萄糖醛酸苷的AUCt增加了近两倍,最大浓度增加了近50%,与空腹服用相比。当口服悬浮液与食物一起服用时,替唑沙尼和替唑沙尼葡萄糖醛酸苷的AUC增加了大约50%,Cmax增加了不到10%。
The active metabolite of this drug is tizoxanide (desacetyl-nitazoxanide). The initial reaction in the metabolic pathway of Nitazoxanide is hydrolysis to tizoxanide, followed by conjugation, primarily by glucuronidation to tizoxanide glucuronide. The oral suspension bioavailability of this drug is not equivalent to that of the oral tablets. Compared to the to the tablet, the bioavailability of the suspension was 70%. When administered with food, the AUCt of tizoxanide and tizoxanide glucuronide in plasma is increased to almost two-fold and the maximum concentration is increased by almost 50% compared to when ingested without food. When the oral suspension was ingested with food, the AUC of tizoxanide and tizoxanide glucuronide increased by approximately 50% and the Cmax increased by less than 10%.
来源:DrugBank