Preparation of self-emulsified artemisinin and its pharmacokinetics in rabbits / 第二军医大学学报

ABSTRACT

Objective: To prepare self-emulsified artemisinin and to investigate its pharmacokinetics in rabbits. Methods: The optimized formula was screened using an orthogonal experimental design, tertiary-phase diagram and solubility test; the extents of emulsification and emulsifying time were taken as the indices. The plasma concentrations of indirubin were determined by HPLC method. The crude artemisinin was taken as control and the pharmacokinetic parameters were compared between the 2 groups. Results: The artemisinin self-emulsifying drug delivery system(SEDDS) was composed of arternisinin, Tween-85, ethyloleate, and ethanol. The mean retention times (MRT) was 4. 628 h for crude artemisinin and 4. 750 h for self-emulsion. Pharmacokinetic study in rabbits demonstrated that the SEDDS of artemisinin greatly enhanced the bioavailability of artemisinin via oral administration. Conclusion: SEDDS can greatly increase the in vitro dissolution and in vivo absorption of artemisinin.