Bioequivalence of Aripiprazole Oral Soluble Films and Orally Disintegrating Tablets in Healthy Participants: A Crossover Study

Abstract

Schizophrenia is a serious mental disorder with high disability rates, and antipsychotics, especially second-generation ones like aripiprazole, are the cornerstone of treatment. As a novel formulation, oral soluble films (OSF) offer an alternative to tablets or capsules, improving patient compliance. This study aimed to assess the bioequivalence, pharmacokinetic (PK) properties, and safety of aripiprazole OSF and aripiprazole orally disintegrating tablets (ODT) in healthy Chinese participants. A single-dose, randomized, open-label, and crossover study was conducted. Participants received 10 mg of test aripiprazole OSF (Qilu Pharmaceutical) and reference aripiprazole ODT (Otsuka Pharmaceutical) under fasting and fed states. The fasting trial comprised a three-sequence, three-period design, while the fed trial comprised a two-sequence, two-period design. In the fasting trial, after single oral dosing of aripiprazole OSF (with water), aripiprazole OSF (without water), and aripiprazole ODT, C_max were 55 ± 10 ng/mL, 54 ± 10 ng/mL, and 48 ± 13 ng/mL, respectively; the AUC_0-72h were 1857 ± 377 h·ng/mL, 1823 ± 350 h·ng/mL, and 1745 ± 405 h·ng/mL, respectively. In the fed trial, after single oral dosing of aripiprazole OSF and ODT with water, the C_max were 43 ± 9 ng/mL and 43 ± 10 ng/mL, respectively; AUC_0-72h were 2024 ± 387 h·ng/mL and 1994 ± 426 h·ng/mL, respectively. In terms of bioequivalence evaluation, the 90% confidence intervals of the geometric mean ratio of the main PK parameters of aripiprazole OSF and ODT in the fasting and fed states were all within the acceptable equivalence range (80%–125%). Both formulations were well-tolerated. In conclusion, aripiprazole OSF and ODT reached bioequivalence, and aripiprazole OSF demonstrates significant potential for application in the treatment of psychiatric disorders.