2013•Traditional Chinese Drug Research and Clinical PharmacologyRequires access
Pharmacokinetics Study of Tetramethylpyrazine Self -emulsifying Sustained -release Solid Dispersion in Rabbits
WU Junhong
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Abstract
Objective To compare pharmacokinetics and relative bioavailability of Tetramethylpyrazine self-emulsifying sustained-release solid dispersion(TMP-SESD) and Tetramethylpyrazine sustained-release solid dispersion(TMP-SD)in rabbits.Methods Single dose of TMP-SESD or TMP-SD was orally given to 6 rabbits in a randomized crossover control study.The TMP concentration in plasma was determined by high performance liquid chromatography,and pharmacokinetic parameters and relative bioavailability were calculated by DAS 2.1 software.Results The main pharmacokinetic parameters for TMP-SESD and TMP-SD were as follows:tmax was 4 h and 6 h,Cmax was 3.217± 0.4581 mg.L-1 and 6.105±0.298 mg.L-1;AUC0-∞ was 63.877±3.786 mg.L-1.h and 39.067±2.971 mg.L-1.h,re spectively.The relative bioavailability of TMP-SESD was(163.5±9.58)% as compared with TMP-SD.Conclusion The pharmacokinetic parameters of TMP in rabbits accord with the two-compartment model,and Cmax and AUC0-∞ of TMP-SESD are all higher than those of TMP-SD,and TMP-SESD has a higher bioavailability during the first absorption after TMP-SESD or TMP-SD administration.