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Related Experiment Videos

Human pharmacokinetic study of immediate-release (codeine phosphate) and sustained-release (codeine Contin) codeine

C J Band1, P R Band, M Deschamps

  • 1Faculty of Pharmacy, University of Montreal, Quebec, Canada.

Journal of Clinical Pharmacology
|September 1, 1994
PubMed
Summary

A new sustained-release codeine formulation (SRC) shows comparable bioavailability to immediate-release codeine phosphate (IRC). SRC provides delayed peak plasma levels, potentially improving pain management by maintaining higher drug concentrations over time.

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Area of Science:

  • Pharmacology
  • Clinical Pharmacy

Background:

  • Codeine is a widely used analgesic.
  • Optimizing codeine delivery can enhance pain management and patient outcomes.

Purpose of the Study:

  • To compare the pharmacokinetics, bioavailability, and side effects of a novel oral sustained-release codeine (SRC) formulation against immediate-release codeine phosphate (IRC).

Main Methods:

  • A double-blind, randomized, crossover study was conducted in 13 healthy adult volunteers.
  • Pharmacokinetic parameters (Cmax, Tmax, AUC, t1/2el) were analyzed using high-performance liquid chromatography.
  • Different dosing regimens were used for SRC (150 mg every 12 hours) and IRC (60 mg every 4 hours initially, then 30 mg every 4 hours).

Main Results:

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  • Both formulations demonstrated comparable bioavailability.
  • SRC exhibited delayed peak plasma levels (Tmax of 2.3 hours single dose, 3.2 hours steady-state) compared to IRC (Tmax of 1.1 hours for both).
  • Sustained-release codeine resulted in higher plasma concentrations over a broader time interval.

    • Conclusions:

    • The sustained-release formulation of codeine is absorbed with delayed kinetics, not limited by drug elimination.
    • SRC offers a promising alternative for pain management due to its prolonged drug release profile.