Collection Day (24-hr timepoint)

Donepezil (ng/mL)

M1 / M2 (ng/mL)

M4 (ng/mL)

M6 (ng/mL)

Oral Tablet

Patch

Oral Tablet

Patch

Oral Tablet

Patch

Oral Tablet

Patch

 

Day 1 (Oral) or Day 29 (Patch)

68.8

93.4

ND

1.1

ND

0.1

39.6

31.8

43.7

79.4

ND

2.1

0.1

0.2

18.7

29.3

45.2

91.4

ND

0.8

0.1

ND

17.9

26.3

62.5

127.6

ND

2.1

0.1

0.1

38.2

79.5

32.5

136.1

ND

2.0

ND

0.2

22.9

104.0

62.5

151.7

ND

7.9

0.1

ND

28.4

52.6

Mean ± SD

52.5 ± 12.9

113.3 ± 26.5

NA

2.7 ± 2.4

0.1 ± 0

0.2 ± 0.1

27.6 ± 18.7

53.9 ± 28.9

 

 

Day 274

5.0

12.8

ND

0.9

0.1

0.2

6.7

15.3

3.6

20.0

ND

0.9

0.1

0.1

4.6

6.4

1.3

39.2

ND

0.5

0.1

ND

3.9

13.5

3.7

13.1

ND

0.5

0.2

0.1

18.7

10.4

11.3

19.6

ND

0.2

0.1

0.1

20.1

15.9

5.5

38.2

ND

0.8

0.1

0.1

9.0

21.4

Mean ± SD

5.1 ± 3.1

 23.8 ± 10.9

NA

 0.6 ± 0.3

0.1 ± 0

0.1 ± 0

 10.5 ± 6.5

13.8 ± 4.7
NA = Not applicable; ND = not detectable; SD standard deviation
Table 5: Donepezil and Metabolite(s) Concentrations from Gottingen Mini-pigs Administered Donepezil HCl Tablet (10 mg) and Transdermal Patch (2-350 mg patches) for Nine Months.