Abstract:
AimTo prepare the breviscapine liposomes and study the pharmacokinetics of breviscapine liposomes in Beagle dogs. MethodsThe cross-over design (two periods) was employed. Six Beagle dogs were administrated a single intravenous dosage of 28 mg of breviscapine liposomes and reference preparation, respectively, scutellarin in plasma of 6 dogs at different sampling time was determined by RP-HPLC. The pharmacokinetic parameters were calculated by 3P97 program and compared by statistic analysis. ResultsThe mean concentration-time curves of breviscapine liposomes and reference preparation were both fitted to two-compartment model with the main pharmacokinetic parameters as follows:
T1/2α were (4.4±0.7) min and (1.8±1.3) min respectively;
T1/2<>> were (55±27) min and (28±23) min respectively; Vc were (1 580±265) mL and (2 460±2 200) mL respectively; CLs were (88±10) mL·min-1 and (324±69) mL·min-1 respectively; and AUC0-720 were (363±42) μg·min·mL-1 and (102±19) μg·min·mL-1 respectively. The T1/2α, CLs and AUC0-720 of breviscapine liposomes all had significant difference from those of reference preparation, after the data were examined by a one-way analysis of variance (ANOVA). ConclusionCompared with the reference preparation, breviscapine liposomes had a much more higher concentration in plasma and contained characteristic of sustained-release, which ameliorated the pharmacokinetic properties of scutellarin.