Pharmacokinetics of abiraterone acetate released from a tablet based on lipid matrix in beagle dogs.

Abstract

Objective: To compare the pharmacokinetic behavior of abiraterone acetate after oral administration of a lipidbased formulation tablet and a reference preparation, and to study the relative bioavailability of abiraterone acetate released from the lipid matrix-based tablet. Methods: Beagle dogs received a single dose orally. The experimental dosage was 75 mg/tablet, and the reference dosage was 250 mg/tablet. Six beagle dogs in each group were investigated with the method of 3 × 3 cross-administration. Blood plasma was collected and centrifuged before administration and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 h after administration, and the plasma samples were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Results: The half-life (T1/2) values of lipid-based formulation (LBF) abiraterone acetate tablet samples (75 mg/tablet) and reference tablets (250 mg/tablet) after oral administration were 3.42 and 4.27 h, respectively, while the area under the concentration time curve (AUC0-t) (h·ng/mL) values were 107.71 and 52.83, respectively. The F value of the relative bioavailability was 704.80%. Conclusion: The preparation method based on lipid matrix can significantly improve the bioavailability of abiraterone acetate tablets, which is a feasible method to improve the bioavailability of biopharmaceutical classification system (BCS) class<small>IV</small> drugs.