Comparative pharmacokinetics of breviscapine liposomes in dogs, rabbits and rats.
OBJECTIVE
To compare pharmacokinetics of intravenous breviscapine liposomes in Beagle dogs, rabbits and rats.


METHODS
Six Beagle dogs, 6 rabbits and 12 rats were intravenously administrated with breviscapine liposomes and commercial injection (breviscapine solution) by the crossover design (two periods), respectively. Plasma concentration of scutellarin, the main active component in breviscapine, at different time intervals was determined by reverse phase-HPLC. The pharmacokinetic parameters including area under the curve (AUC), clearance (CL(s)) and volume of distribution (V(c)) were calculated.


RESULTS
The plasma concentration-time profiles were fitted to a two-compartment model. Breviscapine liposomes exhibited significant difference from injection in CL((s)) and AUC, examined by a one-way analysis of variance (ANOVA). With regard to both breviscapine liposomes and commercial injection (free breviscapine), the logarithm values of AUC, CL(s) and V(c) were all related to the logarithm of the body weight by the allometric equation: Y=axW(b).


CONCLUSIONS
The allometric equation might be applied to extroplate dosage for human from animal data and also for dosage adjustment of breviscapine liposomes in order to achieve same AUC as commercial injection. Compared with the breviscapine solution, breviscapine liposomes delivered more scutellarin into the plasma.
Lv
Wenli
W
School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Guo
Jianxin
J
Ping
Qineng
Q
Song
Yunmei
Y
Li
Jin
J
D000704:Analysis of Variance; D000818:Animals; D047310:Apigenin / Q000097:blood*; D019540:Area Under Curve; D001835:Body Weight; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005965:Glucuronates / Q000097:blood*; D007275:Injections, Intravenous; D008081:Liposomes; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013045:Species Specificity; D013997:Time Factors; D014018:Tissue Distribution
D005419:Flavonoids; D005965:Glucuronates; D008081:Liposomes; C061097:breviscapine; C484876:scutellarin; D047310:Apigenin