Collection Day (24-hr timepoint)

Parent / Metabolite (ng/mL)

Donepezil

M1

M2

M4

M6

Oral

Topical

Oral

Topical

Oral

Topical

Oral

Topical

Oral

Topical

 

 

Day 7

1.78

104.69

ND

0.05

0.10

0.57

0.34

21.23

ND

1.40

4.80

111.99

ND

ND

0.04

0.50

0.38

14.98

ND

1.45

5.98

131.11

ND

0.02

ND

0.57

0.53

17.09

ND

0.86

7.86

183.52

ND

ND

ND

0.74

0.04

11.35

ND

3.80

18.02

219.99

ND

ND

ND

0.84

0.11

8.48

ND

5.50

9.76

121.02

ND

ND

ND

0.44

0.07

5.02

ND

1.77

Mean ± SD

8.03 ± 5.60

145.39 ± 46.02

NA

0.03

0.07

0.61 ± 0.15

0.25 ± 0.20

13.03 ± 5.92

NA

2.46 ± 1.80

 

 

Day 86

1.56

82.10

ND

0.26

ND

0.55

0.29

0.55

0.0204

10.53

11.32

120.67

0.04

0.21

0.12

0.55

0.83

0.28

0.0680

15.05

30.19

120.39

0.06

0.21

0.24

0.60

2.65

0.40

0.3054

14.29

13.16

151.37

0.07

0.30

0.14

0.93

0.67

5.08

0.3955

8.94

18.30

169.53

0.12

0.28

0.20

1.11

0.45

6.14

0.5415

8.61

12.09

128.41

0.08

0.13

0.14

0.68

0.45

1.46

0.3015

5.44

Mean ± SD

14.44 ± 9.44

128.75 ± 29.95

0.07± 0.03

0.23 ±0.06

0.17 ± 0.05

0.74 ± 0.23

0.89 ± 0.88

10.48 ± 3.65

0.27 ± 0.20

2.32 ± 2.60

NA = Not applicable; ND = not detectable; SD standard deviation
Table 4: Donepezil and Metabolite(s) Concentrations from Sprague-Dawley Rats Administered Donepezil HCl Orally (10 mg/kg) and Topically (250 mg/kg) for Three Months.