Tissue
(µg eq/g) (n=3)

Oral (30 mg/kg)

Transdermal (~61.3 mg/kg3)

2h

8h

24h

72h

168h

360h

2h

8h

24h

72h

168h

360h

Blood/Plasma

0.75

1.23

0.63

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

Adrenal Gland

7.32

6.96

4.98

0.26

LOQ

LOQ

LOQ

2.55

6.10

2.76

LOQ

LOQ

Eye

20.55

31.85

48.75

37.13

18.93

19.91

LOQ

1.70

37.77

47.54

13.69

28.29

Liver

9.80

10.07

8.27

0.30

LOQ

LOQ

LOQ

1.96

4.58

3.39

LOQ

LOQ

Pituitary

10.32

9.13

5.91

0.44

1.10

LOQ

LOQ

LOQ

6.98

LOQ

LOQ

LOQ

Skin-Pigmented

7.27

13.29

10.62

20.09

LOQ

LOQ

LOQ

LOQ

1.68

17.19

LOQ

LOQ

Skin-Unpigmented

2.15

2.14

1.31

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

Thyroid
/Parathyroid

8.32

12.68

2.93

0.96

0.31

LOQ

LOQ

1.86

3.32

1.42

1.54

LOQ

Bone

0.76

0.68

0.86

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

LOQ

2.10

Stomach

473.73

422.16

59.74

LOQ

LOQ

LOQ

LOQ

2.40

LOQ

48.18

4.16

LOQ

Small Intestine

378.90

46.60

322.26

0.76

LOQ

LOQ

LOQ

8.71

38.82

37.77

1.99

LOQ

Large Intestine

1.31

96.26

161.54

4.07

LOQ

LOQ

LOQ

1.94

42.51

21.06

LOQ

LOQ

Dose Site4

NA

LOQ

35.28

91.71

24.64

LOQ

LOQ

Stratum Corneum5

NA

NA

109.81

17.78

13.12

1.33

1.20

LOQ = below limit of quantitation
NA = not applicable to route of administration
3dose estimated based upon residual patch analysis
4 pigmented skin + unpigmented skin at the dose site
5 expressed as per cent of dose (mean dose of 61.3 mg/kg based upon residual patch analysis)

Table 2a: Mean Radioactivity in Blood, Plasma, Selected Tissues and Stratum Corneum (Transdermal only) from Long-Evans Rats Administered a Single Oral 14C-Donepezil or 24-h Transdermal Patch Containing 14C-Donepezil.