The relationship between buspirone bioavailability and dose in healthy subjects

Abstract

Dose dependency of the pharmacokinetics of buspirone, a new anxiolytic agent, was tested in 24 healthy volunteers. Each subject received 10, 20, and 40 mg doses according to a randomized, three‐way crossover design with a 7‐day interval between treatments. Buspirone AUC values at 10, 20, and 40 mg doses were in the ratio of 1:1.7:3.5 while C_max values, had a ratio of 1:1.9:3.7. The dose normalized (10 mg basis) AUC and C_max values, T_max values, and half‐lives were not significantly different (p > 0.05) among the doses. Buspirone half‐life did not change as a function of dose (mg kg⁻¹). It was concluded that buspirone exhibits linear pharmacokinetics following doses in the therapeutic range.