Single‐ and Multiple‐Dose Pharmacokinetics of an Oral Once‐a‐Day Osmotic Controlled‐Release OROS® (methylphenidate HC1) Formulation

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Abstract
Methylphenidate is used for the treatment of attention deficit hyperactivity disorder (ADHD). OROS® (methylphenidate HCl) is an osmotic controlled‐release delivery system designed for once‐daily oral dosing. The pharmacokinetics of OROS® (methylphenidate HCl) 18 mg qd, sustained‐release (SR) methylphenidate 20 mg qd, and the immediate‐release (IR) formulation given as three 5 mg doses every 4 hours (tid) were compared in adults. In addition, the single‐ and multiple‐dose pharmacokinetics of the OROS® formulation were studied. Following OROS® (methylphenidate HCl), there was a gradual increase in the mean methylphenidate plasma concentrations with peak concentrations noted at 6 to 8 hours. With the SR formulation, peak plasma concentrations were noted at ∼4 hours. Following the IR regimen, methylphenidate plasma concentrations fluctuated in tandem with oral dosing; peak concentrations were noted at 6.5 hours. The terminal half‐life of methylphenidate was similar for the three formulations. The dose‐normalized methylphenidate Cmax for OROS® (methylphenidate HCl) was significantly lower than for IR and SR methylphenidate. The bioavailability of methylphenidate and PPA from OROS® (methylphenidate HCl) relative to the IR and SR formulations was complete. Mean methylphenidate AUC and terminal half‐life were similar after single (32.9 ng•h/mL and 3.9 hours) and multiple doses (35.2 ng•h/mL and 3.9 hours) of OROS® (methylphenidate HCl).

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