Pharmacokinetics and bioequivalence of evodiamine butyryl derivative-loaded lipid nanoparticles in rats / 中草药

ABSTRACT

Objective To study the pharmacokinetic characteristics and bioequivalence of evodiamine butyryl derivative (EAB) and evodiamine butyryl derivative-loaded lipid nanoparticles (EABLN) in rats. Methods EABLN were prepared by a film ultrasound method, 16 male SD rats were randomly divided into two groups, and their blood were extracted from eye socket after they were intragastric administrated EAB or EABLN (100 mg/kg) for a given time period. Plasma concentration of EAB was determined by HPLC, then pharmacokinetic data, bioequivalence between EAB and EABLN were analyzed by DAS software. Results The main pharmacokinetic parameters of EABLN were listed, AUC(0-72 h), Cmax, and tmax were (11 535.39 ± 261.08) μg∙h/L, (886.73 ± 15.40) μg/L, and (2.00 ± 0.17) h, respectively. Relative bioavailability of EABLN to EAB was 143%, the bioequivalence of AUC(0-72 h) and Cmax in EAB and EABLN were eligible, but bioequivalence of tmax was not eligible. Conclusion EABLN improved the pharmacokinetics of EAB in rats, meanwhile, oral bioavailability of EAB was significantly increased, and there was not bioequivalence between EABLN and EAB.