Study on pharmacokinetics of albendazole nanospheres in rats in vivo

OBJECTIVE To study the pharmacokinetics and bioavailability of albendazole nanospheres in rats by ig administration. METHODS Plasma concentrations of albendazole, albendazole sulphoxide and albendazole sulphone were determined using RP-HPLC method. The chromatographic conditions were a reversed-phase column using acetonitrile-0.25 mol·L-1 sodium acetate (45:55) as the mobile phase at a flow rate of 0.9 mL·min-1 .The separation was performed at room temperature,and detection wavelength was at 292 nm.The injection volume was 20μL. Pharmacokintic parameters were calculated.The relative bioavailability was evaluated. RESULTS The plasma concen-tration-time curves of albendazole sulphoxide (ABZSX) and albendazole sulphone (ABZSN) were fitted to a two-compartment open model.The pharmacokintic parameters of albendazole sulphoxide were as follows: peak time(tmax)(4.92±1.88)h,clearce(CL)(0. 18±0.038)mg·h-1/ (mg·L-1), the half life of elimination(t1/2β)(35.47±2.94)h.There were significant differences from the parameters after the oral administration of albendazole suspension.The relative bioavailability of albendazole sulphoxide was 320.5% .The parameters of albendazole sulphone peak time (tmax) was (6.59±1.97)h.The relative bioavailability of albendazole sulphone was 180.9% .CONCLUSION Nanospheres increase the gastrointestinal absorption, prolong the residence time of abendazole sulphoxide and sulphone in blood after oral administration. So it improves the bioavailability. The new dosage form is provided for the treatment of echinococcosis.