Pharmacokinetics of geniposide through 4 routes of administration

Objective:In order to provide the basis for pharmaceutical applications in future,we studied the pharmacokinetics of geniposide after administration through 4 routes in rats,compared the properties of bioavailability and revealed the dynamic changes of geniposide in vivo.Methods:Geniposide(50,8,8 and 8 mg·kg-1) was administered through oral(ig),nasal(ns),intramuscular(im) and intravenous(iv) routes.Blood samples were obtained by orbital bleeding at a series of time points.Plasma geniposide concentrations were measured by RP-HPLC determination using external standards.Pharmacokinetic parameters were calculated using DAS software.Results:The kinetics matched to one-compartment model after ig and im administration,to two-compartment model after ns administration,and to Room model after iv injection.There were great differences in t1/2,Cmax and AUC0~t between ig and other administrations.The absolute bioavailability was F(ig)=9.74%,F(ns)=49.54% or F(im)=72.69%,respectively.Conclusion:From pharmacokinetic parameters and absolute bioavailability of geniposide,the order of superiority is imnsig administration.