Pharmacokinetics of geniposide through 4 routes of administration

YANG Ming; CHEN Xiao-yan; ZHANG Hai-yan; WANG Jian-min; LU Qian; SONG Wei

Abstract：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 bioavail-ability 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 t_(1/2) , C_(max) and AUC_(o-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 im > ns > ig administration.