TABLE 3

The pharmacokinetic parameters of TRZ, ROS, WAR, and MEP administered orally in cassette dosing after repeated intraperitoneal administration of RIF once daily for 4 days to the male PXB mice

Each value was determined from the data shown in Fig. 1. Data represent the mean ± S.D. of three mice.

RIF DoseCmaxt1/2AUC0-∞AUC Decrease
mg/kgng/mlhng · h/ml%
CYP3A4TRZVehicle824 ± 920.733 ± 0.0661210 ± 110
2643 ± 72*0.775 ± 0.055650 ± 117**46
10408 ± 45**0.699 ± 0.109561 ± 205***54
50531 ± 43***0.575 ± 0.028346 ± 27***71
CYP2C8ROSVehicle1970 ± 2401.07 ± 0.134960 ± 770
21920 ± 2101.10 ± 0.184120 ± 68017
101900 ± 3500.911 ± 0.0753690 ± 86026
501850 ± 3300.772 ± 0.0582630 ± 900*47
CYP2C9WARVehicle680 ± 26ND3830 ± 60
2640 ± 161ND3120 ± 83019
10709 ± 197ND3420 ± 61011
50715 ± 5ND3160 ± 40018
CYP2C19MEPVehicle951 ± 2500.757 ± 0.2491240 ± 230
2955 ± 1500.683 ± 0.144844 ± 17332
10894 ± 1020.660 ± 0.155876 ± 8430
50730 ± 610.524 ± 0.120685 ± 198*46
  • ND, not determined.

  • Statistically significant from the vehicle-treated group: * P < 0.05;

  • ** P < 0.01;

  • *** P < 0.001.