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Pharmacokinetics of two novel bicalutamide formulations in healthy male volunteers
Authors:Cantarini Mireille  Fuhr Rainard  Morris Thomas
Affiliation:AstraZeneca, Parklands, Alderley Park, Macclesfield SK10 4TG, UK. mireille.cantarini@astrazeneca.com
Abstract:The oral bioavailability of two investigational formulations of bicalutamide was compared with the current clinical formulation. The first formulation was amorphous R-/S-bicalutamide in solid dispersion with a polymeric matrix of hydroxypropyl methylcellulose phthalate (HP55S) (R-/S-bicalutamide/HP55S); the second was R-bicalutamide alone in a solid dispersion with HP55S (R-bicalutamide/HP55S). Study 1 was a two-period, incomplete crossover study comparing a single dose of bicalutamide 150 mg with single 150 and 450 mg doses of R-/S-bicalutamide/HP55S in healthy male volunteers. Study 2 was a two-period, dose-escalation study of single doses of R-bicalutamide/HP55S in healthy male volunteers. Compared with bicalutamide 150 mg, both formulations appeared more bioavailable, with a faster rate of systemic absorption. The C(max) and AUC of R-bicalutamide/HP55S increased approximately proportionally with dose. The inter-subject variability of R-bicalutamide exposure for R-/S-bicalutamide/HP55S 150 mg increased 2.19-fold compared with bicalutamide 150 mg. Clinically insignificant increases in circulating luteinizing hormone and testosterone plasma concentrations were observed for both R-bicalutamide/HP55S and R-/S-bicalutamide/HP55S compared with bicalutamide 150 mg. Both new bicalutamide formulations were well tolerated.
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