Study On Pharmacokinetic And Tissues Distribution Of Viaminate In Rats

ObjectiveTo study the pharmacokinetic and tissue distribution of viaminate in rats after intragastric administration, which provide data for the safety, effectivity and indication enlargement of the clinical medication of viaminate, and to study that whether the isomeride of viaminate existed in vivo, which may provide the possible direction for the new medicine research work.MethodsSerum, heart, liver, kidney, brain, spleen, lung, brain, muscle, skin, fat, skeleton, testis, uterus and ovary samples were obtained at different times after intragastric single dose of viaminate (125 mg/kg) and the possible isomeride of viaminate was detected by liquid chromato-graphy-mass spectrometry. The serum concentration-time curve and the pharmacokinetic parameters were calculated with DAS2.0 practical pharmacokinetics program.Results1. The mean serum concentration-time curves of viaminate after oral administrtion a single dose(125 mg/kg) in rat could be fitted to the model of two-compartment model with a weight of 1. 0. Pharmacokinetic parameters of viaminate at single dose of 125 mg/kg in rat were as follows : t_1/2β= (2.22±0.52) h; T_max =(0-83±0.13) h; C_max=(3.90±1.05)μg/mL.2. After administrtion, viaminate can be distributed in many tissues or organs in rat after 15 min. At 1 h, the concentrations of viaminate were highest in fat, followed by skin and muscle, lowest in testiculus and skeleton. The concentrations were decreased obviously after 7 h.3. A new compound with the same molecular weight of viaminate can be detected in the plasma and skin tissues of rat in 1 h after intragastric administration.Conclusions1. Viaminate can be quickly absorbed in vivo of rat and then be eliminated relatively fast.2. Viaminate can be distributed in various tissues or organs of rat. The concentration of viaminate in most tissues is higher than that in plasma.3. A new compound with the same molecular weight of viaminate can be produced in vivo of rats after intragastric administration. The new compound may be a isomeride of viaminate.