Pharmacokinetic comparison of orally-disintegrating metoclopramide with conventional metoclopramide tablet formulation in healthy volunteers.

摘要

BACKGROUND: Oral tablet formulations of metoclopramide are effective therapies for gastroparesis and gastro-oesophageal reflux disease; however, difficulty swallowing tablets or nausea/vomiting may reduce patient adherence to therapy. Because of this, a metoclopramide orally-disintegrating tablet (ODT) has been developed. AIM: To evaluate the bioequivalence of a single administration of a 10-mg metoclopramide ODT and a conventional 10-mg oral metoclopramide tablet in healthy volunteers. METHODS: In a randomized, single-dose, crossover study, healthy volunteers received single administration of 10-mg metoclopramide ODT and 10-mg conventional metoclopramide tablet, with a 7-day interval between treatments. Serial blood samples were collected before dosing and during 24 h post-treatment. RESULTS: Forty-one volunteers completed both treatment arms. Metoclopramide ODT was bioequivalent to conventional tablets; 90% CIs for geometric mean treatment ratios of C(max) [91.6% (90% CI, 87.7-95.8%)], AUC(last) [97.3% (90% CI, 94.5-100.2%)] and AUC(inf) [97.6% (90% CI, 94.5-100.8%)] were within the predefined range. Of the 44 volunteers included in the safety analysis, 9 (20%) reported AEs after ODT, compared with 13 (30%) after conventional tablets. CONCLUSION: In healthy volunteers, single administration of 10-mg metoclopramide ODT was well tolerated and bioequivalent to single administration of a conventional 10-mg metoclopramide tablet.