Distribution and metabolic pathway of flualprazolam in rat

To probe into the distribution and metabolic pathway of flualprazolam plus its main metabolite (α - hydroxylflualprazolam) in rat. 40 SD rats were randomly divided into 4 groups and fasted for 12 hours, with the first group being fed of flualprazolam by gavage as per 0.45 mg/kg and having their respective blood collected from tail vein at different time and each one's urine received every day after administration. The second group was taken as the blank control to the first one. The third group was executed at 0.25h after drug administration, having their respective blood, heart, liver, lung, kidney, brain, spleen and muscle collected and extracted with rapid solvent extraction. The fourth group was the blank control against the third one. The distributing and metabolizing flualprazolam and α - hydroxyflualprazolam were detected through HPLC-MS/MS. Flualprazolam was found of rapid distributing and metabolizing in rats, reaching its highest blood concentration within 0.25h, having shown its sequential distribution in various organs as follows: kidney > brain > heart > liver > spleen > muscle > muscle > lung > blood. Yet, α - hydroxyflualprazolam demonstrated its discrepant organ-specific distributing order: liver > kidney > heart > spleen > lung > muscle > blood > brain. The experiment has showed the distribution and degradation of flualprazolam and its main metabolite in rats who were administered of flualprazolam by gavage, capable of providing scientific basis for flualprazolam to test in vivo and have its metabolic pathway analyzed.