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Pharmacokinetics, Tolerability, and Safety of Aripiprazole following Multiple Oral Dosing in Normal Healthy Volunteers

From the Otsuka Maryland Research Institute, Rockville, Maryland (Dr. Mallikaarjun, Dr. Bramer) and Bristol-Myers Squibb, Princeton, New Jersey (Dr. Salazar). Dr. Salazar is a fellow of the American College of Clinical Pharmacology.

Two 14-day, placebo-controlled, double-blind studies evaluated the fasting pharmacokinetics, safety, and tolerability of aripiprazole, a new antipsychotic, in healthy male subjects. In Study 1, 37 subjects were randomized to aripiprazole 5 mg, 10 mg, 15 mg, 20 mg, or placebo once daily. In Study 2, 11 subjects were randomized to aripiprazole, titrated from 10 to 30 mg/day, or placebo. Aripiprazole had linear pharmacokinetics over 5 to 30 mg/day, which were described by a two-compartment open model, with first-order absorption. In Study 1, mean elimination half-life ranged from 47 to 68 hours with aripiprazole, with apparent systemic clearance (CL/F) of approximately 3.45 L/h. In Study 2, mean elimination half-life was 59 hours (CL/F approximately 4.0 L/h). Adverse events were generally mild to moderate, were transient in nature, and commonly occurred within the first 3 days of dosing. Clinical laboratory assessments, electrocardiogram, electroencephalogram, and prolactin levels showed no clinically significant changes during the studies.

Key Words: Pharmacokinetics • aripiprazole • healthy volunteers • drug safety

Address for reprints: Dr. Suresh Mallikaarjun, Otsuka Maryland Research Institute, 2440 Research Boulevard, Rockville, MD 20850.

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