PAMPA-Phosphatidylcholine
Papp (10-6 Cm/S)
(Mean± SEM)
In silico prediction (QPlog BB)
Experimental
(log BB) [14]
Olanzapine
CNS+
312.4
2
1.8
30.76 ± 0.78
27.77 ± 1.3
0.814
-
Duloxetine
CNS+
297.4
4
9.34
1.32
28.33 ± 0.36
31.44 ± 0.68
0.469
-
Carbamazepine
CNS+
236.3
2.45
9.3
1.78
23.32 ± 0.12
14.97 ± 0.42
-0.2
-0.14
Diphenhydramine
CNS+
255.4
3.27
9.0
1.61
22.78 ± 0.04
17.56 ± 1.63
0.54
-
Desipramine
CNS+
266.4
4.9
10.1
1.28
20.88 ± 0.21
23.63 ± 0.42
0.5
1.2
Diazepam
CNS+
284.7
2.9
3.3
2.8
20.76 ± 0.63
21.04 ± 1.55
0.258
0.52
Alprazolam
CNS+
308.8
4.9
2.8
1.26
11.81 ± 0.32
8.65 ± 0.54
0.09
0.04
Imipramine
CNS+
280.4
4.8
9.4
2.4
13.34 ± 0.15
11.93 ± 0.32
0.662
1.07
Promazine
CNS+
284.4
4.3
4.2
2.52
8.97 ± 0.13
9.77 ± 0.23
0.733
1.23
Caffeine
CNS+
194.2
-0.5
0.6
0.02
4.73 ± 0.09
4.87 ± 0.07
-0.262
-0.06
Amitriphyline
CNS+
277.4
4.9
9.4
2.77
5.03 ± 0.18
4.51 ± 0.11
0.722
0.89
Chlorpromazine
CNS+
318.9
4.8
9.3
3.38
2.62 ± 0.06
2.62 ± 0.06
0.916
1.06
Dopamine
CNS-
153.2
0.9
8.93
-0.80
1.03 ± 0.09
1.38 ± 0.10
-1.669
-
Atenolol
CNS-
266.3
0.5
9.6
-1.29
0.87 ± 0.17
1.08 ± 0.01
-1.152
-0.87
Ofloxacin
CNS-
361.4
2.1
-0.62
0.72 ± 0.02
0.16 ± 0.03
-1.482
-
Norfloxacin
CNS-
319.3
0.42
-0.81
0.39 ± 0.10
0.28 ± 0.03
-1.699
-
Table 2: The physicochemical properties and permeability values of the drugs used in the validation of the PAMPA Porcine brain lipids and Phosphatidylcholine vesicle
membrane models.
