Solid Oral and Non-oral Modified-Release

  1. One dose for immediate release and another dose for delayed release (or 2nd dose)
    Multiple layered or tablet within a tablet
    Repeat action
  2. Release is direct toward a specific body region, tissue, or site
    enteric coating
    Target release
  3. Rate controlled delivery systems
    • applicable to numerous dosage forms
    • rate of drug delivery is controlled by feature of the device
  4. MTC
    Minimum Toxic Concentration
  5. MEC
    Minimum effective concentration
  6. Advantages of Solid Oral Modified-Release
    • Reduction in drug blood level fluctuations
    • Frequency reduction in dosing
    • Enhanced convenience and compliance
    • Reduction in side effects
    • Reduction in overall helath care costs
  7. Disadvantages of Solid Oral Modified-Release
    • No flexibility in adjusting drug dose and or dosage regiment
    • Dose dumping
  8. What are the attributes of drugs that are good candidates for extended-release products
    • Neither very slow nor very fast rates of absorption and excretion (inherently long-acting drugs and short life)
    • Uniformly absorbed from GI tract
    • Administered in relatively small doses
    • Good margin of safety, wide therapeutic index
  9. Therapeutic index
    median toxic dose/median effective dose
  10. Oral extended-release products
    • Provide immediate release of one dose of drug for prompt therapeutic effect followed by gradual and continual release of additional doses to maintain effect over an extended period of time
    • Additional "maintenance" doses are released at a rate correspondent to the amount being metabolized and excreted
    • Dissolve in GI fluids
    • Maintain sufficient GI residence time
  11. Extended-release technolgoy
    • Coated beads, granules or microspheres
    • Multitablet system
    • Microencapsulated drug
    • Drug embedded in slwly eroding or hydrophilic matrix
    • Drug embedded in inert plastic matrix
    • Complex formation
    • Ion-exchange resins
    • Osmotic pump
  12. Doryx
    Coated doxycycline hyclate pellets
  13. Eric
    erythromycin delayed-release capsules with enteric coated pellets of erythromycin base
Card Set
Solid Oral and Non-oral Modified-Release
Dose Form Final