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Table 7 Murine plasma pharmacokinetic parameters of S733 and SJ311 after oral administration

From: Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

Dose (mg/kg)

(r)-SJ733

( +)-SJ733

(r)-SJ311

 

50

200

10

100

100

Cmax (µM)

10.1 ± 4.5

12.7 ± 3.2

1.38 ± 0.21

11.7 ± 1.2

10.5 ± 5.3

Tmax (h)

0.5

5

0.5

0.5

0.5

Half-life (h)

1.72

14.1

3.63

3.17

4.20

AUCinf (h µM)

28

155.7

4.27

53

42

CL/F (L/h/kg)

4.02

3.25

5.00

4.02

5.34

V/F (L/kg)

18.4

3.23

26.2

18.4

32.4

F (%)

70

98

65

80.8

23.1

  1. % F was calculated using the equation: (AUCinf PO / mean AUCinf IV) • (Dose IV / Dose PO). Cmax values are mean ± SD, n = 3 or 4. AUCinf, CL and V were estimated from mean plasma concentration values from different animals in a single study; error or SDs for the parameters were not estimated