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Table 4 Distribution, concentration and half-lives of [14C] dihydroartemisinin (DHA) in total, free, glucuronide and other conjugation fractions in plasma or urine following a single intravenous dose at 3 mg/20 μCi/kg in rats.

From: Pharmacokinetics, tissue distribution and mass balance of radiolabeled dihydroartemisinin in male rats

Time

Total

Free fraction

Glucuronide conjugation

Other conjugation fraction

Plasma (n = 5)

    

0

0.00

0.00

0.00

0.00

0.017

3446.38 ± 396.35

2253.63 ± 537.31

403.87 ± 124.77

583.17 ± 155.52

0.083

2279.43 ± 213.77

925.14 ± 226.81

413.56 ± 69.46

589.70 ± 102.30

0.167

2090.86 ± 180.56

697.05 ± 88.04

480.62 ± 49.17

818.11 ± 88.12

0.25

1987.48 ± 378.69

685.05 ± 193.99

360.93 ± 65.83

684.75 ± 161.05

0.50

1489.58 ± 231.59

461.20 ± 56.83

305.81 ± 26.23

627.62 ± 59.19

0.75

654.49 ± 87.56

157.51 ± 28.11

131.60 ± 29.09

341.12 ± 66.12

1.0

514.20 ± 139.37

105.36 ± 55.10

122.76 ± 36.01

348.30 ± 125.91

1.5

419.48 ± 17.06

75.83 ± 9.85

74.17 ± 11.64

268.16 ± 14.76

2

589.26 ± 154.02

90.58 ± 33.58

110.13 ± 44.55

407.78 ± 112.11

3

466.65 ± 82.13

74.40 ± 16.25

80.73 ± 14.20

321.61 ± 69.08

6

584.41 ± 65.49

51.49 ± 15.64

49.34 ± 22.19

363.63 ± 162.04

8

481.59 ± 79.35

49.44 ± 13.34

57.72 ± 13.56

388.11 ± 72.73

24

253.62 ± 78.47

14.46 ± 3.15

20.04 ± 5.05

188.12 ± 47.66

48

79.17 ± 6.71

7.41 ± 3.24

8.55 ± 1.68

77.07 ± 14.36

72

64.38 ± 14.66

4.89 ± 1.83

4.31 ± 1.19

48.23 ± 12.74

96

35.26 ± 6.54

2.09 ± 1.39

2.25 ± 0.87

25.39 ± 7.32

192

13.48 ± 3.65

1.01 ± 0.92

0.76 ± 0.72

14.49 ± 1.62

   AUC (ng·h/ml)

21708 ± 2695

2188.2 ± 286.4

2177.6 ± 299.6

14193.6 ± 6838.7

   t1/2 (hr)

15.49 ± 1.64

4.01 ± 0.99

6.66 ± 1.04

20.25 ± 1.32

   % of total

100.2 ± 12.68

10.08 ± 1.32

10.03 ± 1.38

79.14 ± 8.22

Urine (n = 5)

    

0

0.00

0.00

0.00

0.00

0.04

37186.4 ± 8200.9

2253.63 ± 113.44

1611.28 ± 756.20

21546.88 ± 8219.11

0.33

228363.9 ± 20101.9

2693.12 ± 1293.63

8359.94 ± 1428.22

39881.66 ± 5139.02

1.0

123776.8 ± 38621.3

535.48 ± 339.64

732.58 ± 373.98

10784.80 ± 6618.73

2.0

42340.5 ± 8839.2

184.08 ± 70.94

97.20 ± 50.00

2003.77 ± 1218.99

3.0

14248.3 ± 6958.5

86.77 ± 56.02

29.60 ± 15.80

655.31 ± 605.27

4.0

6355.5 ± 1351.3

43.20 ± 26.91

17.54 ± 11.47

278.99 ± 208.65

5.0

4984.6 ± 1922.7

35.21 ± 39.14

12.70 ± 9.90

310.60 ± 306.84

6.0

4006.4 ± 2925.2

22.16 ± 28.94

7.77 ± 3.88

289.69 ± 338.11

7.0

1451.9 ± 149.2

9.75 ± 4.98

6.21 ± 2.92

147.26 ± 104.46

8.0

780.1 ± 344.4

5.77 ± 3.86

3.28 ± 1.66

91.76 ± 59.41

   AUC (ng·h/ml)

43624 ± 10214

2213.6 ± 933.4

5069.3 ± 928.2

35657.7 ± 9342.1

   t1/2 (day)

1.36 ± 0.25

1.25 ± 0.11

1.30 ± 0.16

1.64 ± 0.11

   % of total

98.43 ± 23.38

5.11 ± 1.45

12.22 ± 3.14

82.67 ± 3.96

  1. AUC = area under curve; t1/2 = half-life