[Comparison of kinetic behavior in both plasma and tissue after intravenous administration of alpha-asarone in lipid emulsion and aqueous solution in rats and mice].
OBJECTIVE
To compare the pharmacokinetics and tissue distribution of alpha-asarone in lipid emulsion and aqueous solution for injection and study the feasibility of lipid emulsion of alpha-asarone as the parenteral drug delivery system.


METHODS
HPLC was used to determine the drug concentration in rat plasma and mice tissues after intravenous (i.v.) administration of lipid emulsion and aqueous solution of alpha-asarone at a single dose (40 mg x kg(-1)), respectively.


RESULTS
The plasma concentration-time profiles of lipid emulsion and aqueous solution of alpha-asarone after intravenous administration of them are similar and the drug concentration-time data were fitted to a two-compartment open model. The results of tissues distribution showed that distribution contents of alpha-asarone from lipid emulsion and aqueous solution in vivo are similar in lungs but lipid emulsion increased the uptake in livers and spleens, and decreased the uptake in hearts and kidneys for alpha-asarone.


CONCLUSIONS
The plasma concentration-time profiles of alpha-asarone in lipid emulsion and aqueous solution are similar, but lipid emulsion significantly altered the tissue distribution of alpha-asarone, which may be beneficial to decrease its potential toxicity to heart and kidney.
Guo
Dan-Dan
DD
West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Hou
Shi-Xiang
SX
Mao
Sheng-Jun
SJ
He
Jun-Yao
JY
Zhao
Rong-Li
RL
Li
Yuan-Bo
YB
D000081248:Allylbenzene Derivatives; D000818:Animals; D000840:Anisoles / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D004655:Emulsions / Q000737:chemistry*; D005260:Female; D007275:Injections, Intravenous; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D000081248:Allylbenzene Derivatives; D000840:Anisoles; D004655:Emulsions; D008055:Lipids; C012195:asarone