OBJECTIVE To study the absorption,distribution,excretion,bioavailability and protein binding of
nicotinylsalicylic acid in
dog,rabbit and mice.METHODS The HPLC assay was used to determine the
nicotinylsalicylic acid concentrations in biological samples.RESULTS The concentration-time curve of
Nicotinylsalicylic acid in dogs after an ig administration of 100 mg·kg~(-1) was discribed by a two-compartment open model with the elimination half-life of 0.61 h.The relative bioavailability of nicotinylsalicylic acid in rabbits was 64%.The level of nicotinylsalicylic acid was very low in mice heart,liver,brain and kidney,because it was metabolized to active nicotinic acid and salicylic acid.The protein binding rates of nicotinylsalicylic acid were in the range of 37.3%～57.4%.Nicotinylsalicylic acid at low level,and both of salicylic acid and nicotinic acid at high level were obtained in rabbit urine.CONCLUSION The absorption of nicotinylsalicylic acid is rapid,its half-life is short because it is metabolized to active nicotinic acid and salicylic acid in liver and plasma.The tissue distribution and protein binding is low.Nicotinic acid,salicylic acid and their metabolites are excreted by kidney.