ABSTRACT
OBJECTIVE: To study the pharmacokinetics and bioequivalence of hydroxysafflor yellow A (HSYA) and hydroxysafflor yellow A nanoemulsion (HYAN) in rats.METHODS: Twelve male rats were randomly divided into two groups. The rats were administered intragastrically with HSYA or HYAN, respectively, and then blood was collected from the venous plexus at different time points. HPLC method was used for the determination of HSYA blood concentration.RESULTS: The main pharmacokinetic parameters of HYAN were as follows: the area under curve (AUC0-24 h), peak concentration (ρmax), peak time (tmax) and clearance (CL) were (31.56±4.58) mg•L•h-1, (12.75±2.64) mg•L-1, (0.83±0.54) h and (1.89±0.93) L•h-1•kg-1, respectively. The AUC0-24 h, ρmax and tmax of HYAN increased by 5.49, 10.22 and 2.50 times, respectively, and the CL of HYAN was only 1/4 of that of HSYA. The 90% confidence intervals for AUC0-24 h and ρmax were not within the prescribed range of bioequivalence criteria.CONCLUSION: Relative to HSYA, the high plasma concentration and prolonged peak time of HYAN in vivo can significantly improve the oral bioavailability of HSYA. HSYA solution and HYAN are not bioequivalent.
ABSTRACT
OBJECTIVE: To study evodiamine complex nanoemulsion oil-in-water (EPBCN) in vitro and in vivo evaluation, about release in vitro and pharmacokinetics. METHODS: Release in pH 1.2 hydrochloric acid and pH 6.8 PBS solutions and oral bioavailability in rats of EPBCN would be studied. The bioequivalence between evodiamine (ED) and EPBCN was judged. RESULTS: In vitro release of EPBCN was about 2.61 times higher than that of ED. The oral bioavailability of EPBCN was 7.35 folds than that of ED. 90% confidence interval of area under concentration-time curve (AUC0-72 h) and peak concentration (ρmax) exceeded the standard range. CONCLUSION: EPBCN can remarkably increase the release in vitro and oral bioavailability in rats, and they do not have bioequivalence.