Fed and Fasted Administration of a Novel Extended‐Release Methylphenidate Orally Disintegrating Tablet Formulation for the Treatment of ADHD. Issue 2 (25th May 2017)

• Record Type: Journal Article
• Authors: Weisler, Richard H.; Stark, Jeffrey G.; Sikes, Carolyn
• Is Part Of: Clinical pharmacology in drug development. Volume 7:Issue 2(2018)
• Page Start: 160
• Page End: 167
• Publication Date: 2017-05-25
• Subjects: clinical trials -- pharmacokinetics and drug metabolism -- psychiatry -- methylphenidate -- orally disintegrating tablet -- clinical research -- drug delivery; Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.361
• Languages: English
• ISSNs: 2160-7648

Abstract

Abstract: Extended‐release methylphenidate is a first‐line treatment for attention‐deficit/hyperactivity disorder. A methylphenidate extended‐release orally disintegrating tablet (MPH XR‐ODT) has recently been developed. Here we report an open‐label, randomized, 2‐period, 2‐treatment crossover study to determine the effect of food on the bioavailability of a single 60‐mg dose of MPH XR‐ODT in healthy adults. Blood samples were collected predose through 36 hours postdose. Maximum plasma concentration (Cmax ), time to maximum plasma concentration (Tmax ), terminal elimination half‐life (T1/2 ), overall systemic exposure (AUClast and AUCinf ), and partial areas under the concentration curve (AUC0–3, AUC3–7, and AUC7–12 ) were calculated. In total, 48 participants completed the study. For total methylphenidate from MPH XR‐ODT, the lower limit of the 90% confidence interval (CI) around the geometric mean ratio (GMR, fed/fasted) for Cmax was below 80%, indicating a slightly decreased rate of absorption with food, whereas the 90%CIs around the GMRs of AUClast and AUCinf were within the 80%–125% limits, suggesting no food effect on exposure. The most common adverse events (AEs) were palpitations and decreased appetite. No serious, unusual, or unexpected AEs were reported. Thus, food had no substantial effect on overall bioavailability of MPH XR‐ODT, which may be an important factor for some patients.