Pharmacokinetics and bioavailability of @entity206 - XXXX in @entity7858 .

@entity1597 @entity7858 @entity1598 @entity207 @entity206
The pharmacokinetics and bioavailability of @entity206 - @entity207 ( @entity1597 - @entity1598 ) were studied in six healthy male-castrate @entity7858 ( @entity7858 ) after intravenous (i.v.) or oral (p.o.) drug administration of 15 mg/kg @entity1597 - @entity1598 using a crossover design with a 2-week washout period. After 90 days one group (n = 3) was given a p.o. dose of 30 mg/kg @entity1597 - @entity1598 and the other group (n = 3) was given a p.o. dose of 60 mg/kg @entity1597 - @entity1598 . After i.v. administration of 15 mg/kg of @entity1597 - @entity1598 the mean initial plasma concentration (C0) was 10.75 +/- 2.12 microg/mL for @entity206 ( @entity1597 ) and 158.3 +/- 189.3 microg/mL for @entity207 ( @entity1598 ). Elimination half-lives were 0.74 +/- 0.1 h for @entity1597 and 2.2 +/- 0.6 h for @entity1598 . The mean residence times were 1.45 +/- 0.72 h for @entity1597 and 2.8 +/- 0.6 h for @entity1598 . The areas under the respective concentration vs. time curves (AUC) were 2.49 +/- 1.62 microg h/mL for @entity1597 and 124 +/- 60 microg h/mL for @entity1598 . Total clearance (Clt) for @entity1597 was 21.63 +/- 9.85 and 1.90 +/- 0.77 mL/min kg for @entity1598 . The volume of distribution at steady state was 2.32 +/- 1.15 L/kg for @entity1597 and 0.35 +/- 0.09 L/kg for @entity1598 . After intragastric administration of 15, 30 and 60 mg/kg the peak concentration (Cmax) of @entity1598 were 1.9 +/- 0.8, 2.6 +/- 0.4 and 2.8 +/- 0.7 microg/mL, respectively. The AUC was 9.1 +/- 5, 25.9 +/- 3.3 and 39.1 +/- 4.1 microg h/mL, respectively. Based upon these AUC values and correcting for dose, the respective bioavailabilities were 7.7, 10.5 and 7.94%. @entity206 was not detected in plasma after intragastric administration. These data demonstrate that therapeutic concentrations of @entity1597 - @entity1598 are not achieved after p.o. administration to @entity7858 .
