A Comparison of the Pharmacokinetics of Methylphenidate Extended‐Release Orally Disintegrating Tablets With a Reference Extended‐Release Formulation of Methylphenidate in Healthy Adults. Issue 2 (25th May 2017)

• Record Type: Journal Article
• Authors: Childress, Ann; Stark, Jeffrey G.; McMahen, Russ; Engelking, Dorothy; Sikes, Carolyn
• Is Part Of: Clinical pharmacology in drug development. Volume 7:Issue 2(2018)
• Page Start: 151
• Page End: 159
• Publication Date: 2017-05-25
• Subjects: clinical research -- clinical trials -- drug delivery -- pharmacokinetics and drug metabolism -- psychiatry -- ADHD; Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.362
• Languages: English
• ISSNs: 2160-7648

Abstract

Abstract: Extended‐release (ER) methylphenidate (MPH) is a first‐line treatment for attention‐deficit/hyperactivity disorder. A methylphenidate extended‐release orally disintegrating tablet (MPH XR‐ODT) has recently been developed. This was a randomized, open‐label, 3‐period, 3‐treatment study comparing the bioavailability and absorption of 2 MPH XR‐ODT formulations with an MPH ER reference medication. Here we report the 2 treatments comparing the commercial MPH XR‐ODT formulation and reference medication. Following a ≥10‐hour fast, 42 healthy adults received 60 mg of reference medication or MPH XR‐ODT (2 × 30 mg). The following pharmacokinetic (PK) parameters were calculated for total methylphenidate ( d + l ): maximum plasma concentration (Cmax ), time to maximum plasma concentration (Tmax ), terminal half‐life (T1/2 ), and areas under the concentration–time curve from time zero to the time of the last quantifiable concentration (AUClast ), and from time zero extrapolated to infinity (AUCinf ). Secondary PK end points included partial AUCs. Safety was also assessed. Overall systemic exposure to methylphenidate after MPH XR‐ODT administration was similar to that of the reference product, and the concentration–time profiles for MPH XR‐ODT and the reference drug were similar, although the Cmax was 25% higher for MPH XR‐ODT. The most common treatment‐emergent adverse events were nausea (6) and anxiety (4), which were similar across treatments.