Fourteen healthy male subjects (Sub) were allocated randomly to one of two treatment sequences (Seq) in a two period crossover design. The two treatment sequences were either one 40mg tablet, 1x40mg, given in the first treatment period followed by four 10mg tablets, 4x10mg, given simultaneously in the second treatment period (sequence 1/4), or the reverse ordering was administered (4/1). A washout period separated the treatment periods.
Two pharmacokinetic variables, area-under-the-plasma-concentration-vs.-time curve from zero to 72 hours, AUC (ng·hr/mL), and maximum plasma concentration, Cmax (ng/mL), were estimated for each subject in each treatment period from plasma levels of the parent compound (P), and its active metabolite (M), based upon plasma samples taken at pre dose and at various times up to 72 hours post dose.
Part 6 - Table 1 | |||||||||
Relative Bioavailability Study | |||||||||
Parent Compound (P) |
Metabolite (M) |
||||||||
AUC |
Cmax |
AUC |
Cmax |
||||||
Sub |
Seq |
1x40 |
4x10 |
1x40 |
4x10 |
1x40 |
4x10 |
1x40 |
4x10 |
|
|
|
|
|
|
|
|
|
|
1 |
1/4 |
925 |
1107 |
85.7 |
110.8 |
1325 |
1446 |
33.6 |
41.2 |
2 |
4/1 |
1125 |
1152 |
97.4 |
105.0 |
1677 |
1735 |
46.6 |
43.6 |
3 |
4/1 |
1952 |
1525 |
135.0 |
113.0 |
2810 |
2333 |
42.9 |
40.0 |
4 |
1/4 |
836 |
1144 |
69.1 |
94.7 |
1376 |
1624 |
33.3 |
36.0 |
5 |
1/4 |
1514 |
1164 |
111.0 |
88.6 |
2253 |
1757 |
43.2 |
39.6 |
6 |
4/1 |
1048 |
1167 |
72.6 |
79.1 |
1470 |
1681 |
33.8 |
31.6 |
7 |
4/1 |
1003 |
1271 |
80.0 |
94.8 |
1300 |
1594 |
28.3 |
32.0 |
8 |
1/4 |
574 |
636 |
55.0 |
73.7 |
854 |
915 |
28.6 |
29.5 |
9 |
4/1 |
2747 |
2834 |
176.0 |
176.0 |
3513 |
3797 |
49.6 |
54.9 |
10 |
1/4 |
726 |
828 |
55.9 |
72.0 |
1245 |
1239 |
25.1 |
27.6 |
11 |
1/4 |
1773 |
1399 |
137.0 |
119.0 |
2056 |
1785 |
43.3 |
37.8 |
12 |
4/1 |
1257 |
1520 |
99.8 |
112.0 |
1850 |
2059 |
35.2 |
38.4 |
13 |
4/1 |
1147 |
1119 |
81.7 |
91.7 |
1740 |
1721 |
31.6 |
36.0 |
14 |
1/4 |
673 |
825 |
51.8 |
60.0 |
1013 |
1195 |
20.3 |
20.9 |
Bradstreet, T. E. and Short, T. H. (2006) "Favorite Data Sets from Early Phases of Drug Research - Part 6." Proceedings of the Section on Statistical Education of the American Statistical Association.