Clinical pharmacology and pharmacokinetics of once-daily hydromorphone hydrochloride extended-release capsules

J Clin Pharmacol. 2005 May;45(5):547-54. doi: 10.1177/0091270005274552.

Abstract

Hydromorphone hydrochloride extended release (HHER) is a multiparticulate melt-extrusion pellet capsule formulation administered q24h. Study 1 investigated the bioavailability of 24-mg HHER fed, as well as 24-mg and 12-mg HHER and 8-mg hydromorphone hydrochloride immediate-release (HHIR) tablets fasting. No clinically significant food effect was observed on hydromorphone C(max) or AUC for the 24-mg HHER, and dose proportionality (AUC) was demonstrated between 12- and 24-mg HHER. Study 2 demonstrated dose strength proportionality for 3 x 12-mg HHER versus 1 x 32-mg HHER. Study 3 evaluated 12-mg HHER q24h versus 3-mg HHIR q6h at steady state. HHER produced relatively constant steady-state concentrations over 24 hours. HHER and HHIR were equivalent for AUC(ss). C(ssmax) was 26% lower for HHER than HHIR, C(ssmin) was 43% higher for HHER, and peak-to-trough fluctuation was 126% for HHER versus 328% for HHIR, which are ideal attributes of a once-daily oral extended-release dosage form. HHER administration resulted in fewer adverse events than HHIR in study 3.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Analgesics, Opioid / administration & dosage
  • Analgesics, Opioid / adverse effects
  • Analgesics, Opioid / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Delayed-Action Preparations
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Female
  • Food-Drug Interactions
  • Half-Life
  • Humans
  • Hydromorphone / administration & dosage
  • Hydromorphone / adverse effects
  • Hydromorphone / pharmacokinetics*
  • Male

Substances

  • Analgesics, Opioid
  • Delayed-Action Preparations
  • Hydromorphone