Frontiers in Drug Design and Discovery

Volume: 4

Methylphenidate Extended-Release Capsules: A New Formulation for Attention-Deficit Hyperactivity Disorder

Author(s): Pilar García-García, Francisco López-Muñoz, Juan D. Molina, Roland Fischer and Cecilio Alamo

Pp: 228-246 (19)

DOI: 10.2174/978160805202810904010228

* (Excluding Mailing and Handling)


In recent years Attention Deficit Hyperactivity Disorder (ADHD) has been the focus of growing interest, and different drugs have been introduced for its treatment. Thus, there is a range of medication for ADHD, but new formulations are necessary for more individualized therapy. The choice will depend upon the circumstances and detailed assessment. A new extendedrelease formulation of methylphenidate (Medikinet®) has increased the drugdelivery treatment options for ADHD. Medikinet® combines the advantages of immediate-release (IR) and extended-release (ER) formulations of methylphenidate, with rapid onset and prolonged duration of action (7-8 h), in a single dose intended for once-daily administration. The concentration-time profile is achieved through the particular formulation of Medikinet®, whose hardgelatine capsule contains 50% enteric-coated and 50% uncoated pellets, providing both a first, immediate release and a second, delayed release. The coated pellets only dissolve at a pH < 5.5 and release the active drug in a sustained way into the intestine. There is no difference in the bioavailability of the IR/ER product when administration follows a normal or high-calorie breakfast. Medikinet® also shows a bioavailability comparable to that of the b.i.d. 10 mg immediate release regime, as well as a high level of efficacy and good tolerability. In this review, we describe the pharmacokinetics of Medikinet® and compare its characteristics with those of other formulations used for treating ADHD.

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