Solid Oral Modified Release

• Modified-release dosage forms


  Drug released based on time course, and location
• Modified-release dosage forms


  • Reduction in drug blood levels fluctuation
  • Improve drug utilization
  • Reduction in overall healthcare costs
  • Enhanced convenience and compliance
  • Decrease the toxicity and occurrence of ADR
• Reasons for missed doses or too frequent doses


  • Less optimum drug therapy
  • Toxic levels with toxic side effects
• Delayed Release Dosage Forms


  • Drug release is other than the time of prompt administration
  • Dependent on pH (less acidic medium), enzyme (catalyze reactions), and time (erosion over time in GIT)
• Delayed Release Dosage Forms


  • Enteric coated tablets or capsules
• Rationale for Delayed Release Dosage Forms


  • Protection of drug from gastric fluids
  • Reduce gastric distress by drugs irritating the stomach
  • Facilitate gastrointestinal transit for drugs better absorbed in the intestines
• Enteric coating materials

  • Fats
  • Fatty acids
  • Waxes
  • Shellac
  • Cellulose acetate phthalate
• Delayed Release Dosage Forms should not be crushed or chewed
• Extended-Release Dosage Forms


  • Provides a prompt release of API followed by a gradual release of the remaining amount
  • Allows a reduction in dosing frequency from that necessitated by conventional dosage forms, such as a solution or an immediate-release dosage form
• Controlled release


  Systems provide some actual therapeutic control, whether temporal or prolonged
• Sustained release


  • Systems provide medication over an extended period
  • Goal: maintain the therapeutic blood levels
• Mechanisms of Extended-Release Dosage Forms


  • Coated Beads, Granules, and Microspheres
  • Multitablet System
  • Microencapsulation
  • Embedding Drug in Inert Plastic Matrix
• Coated Beads, Granules, and Microspheres

  • Lipid or synthetic coating
  • Aqueous coating
• Lipid or synthetic coating materials


  • Beeswax, carnauba wax, glyceryl monostearate, acetyl alcohol, ethyl cellulose
• Aqueous coating materials

  • Aquacoat ECD – aqueous colloidal dispersion of ethylcellulose polymer
  • Aquacoat CPD – aqueous dispersion based on cellulose acetate phthalate
  • Surelease – aqueous coating system utilizing ethylcellulose
• Multitablet System


  • Small spheroid compressed tablets placed in gelatin capsule shells
  • Coated for immediate release and uncoated for extended release
• Microencapsulation


  Encapsulating micromaterials by various polymers
• Repeat Action Tablet


  • Contains 2 medications in 1 dosage unit
  • Multi-compressed tablet
  • One immediate release and delayed release
• Targeted Release


  • Drug release is concentrated/isolated in a specific body region or tissue
  • For maximum absorption and metabolism
• Targeted Release


  • Liposomes
• Orally Disintegrating Tablets (ODT)


  • Developed to disintegrate rapidly in the saliva after oral administration
  • May be used without the addition of water
• Spansule- capsule that needs to be swallowed whole
• Push layer- Osmogene
• Constant rate- Controlled release

  Not at constant rate- Sustained release
• ADR- Adverse Drug Reaction