[Pharmacokinetic evaluation of danshensu with in vivo microdialysis in freely moving rat's jugular vein].

OBJECTIVE

To investigate the pharmacokinetics of Danshensu with in vivo microdialysis in freely moving rat's jugular vein.

METHOD

three days after a microdialysis probe introducer was implanted into the jugular vein, a microdialysis probe was introduced to the blood vessel, and began to sample following a single intravenous injection (40 mg x kg(-1)) or a single oral dose (40 mg x kg(-1)) of Danshensu. All the samples were analyzed with HPLC. The concentration of Danshensu in blood were calculated according to the recovery of microdialysis probe and the concentration in dialysates. Pharmacokinetic parameters were than calculated with the concentration-time curve.

RESULT

For intravenous administration, t(1/2 zeta) = (69.62 +/- 33.42) min, AUC(0-infinity) = (3416.24 +/- 779.80) min x mg x L(-1), MRT(0-infinity) = (38.15 +/- 8.61) min, and for oral administration, Cmax = (7.42 +/- 3.08) mg x L(-1), tmax = (31.50 +/- 8.57) min, t(1/2 zeta) = (83.25 +/- 37.35) min, AUC(0-infinity) = (793.19 +/- 101.32) min x mg x L(-1), MRT(0-infinity) = (125.89 +/- 58.27) min. The oral bioavailability of Danshensu F = 22.56%.

CONCLUSION

In vivo microdialysis in freely moving rat's jugular vein is a useful tool to obtain a complete set of free drug concentrations to determine reliable pharmacokinetic parameters.