PHRD5925 Pharmaceutics Lecture 18 - Controlled-Release Oral Dosage Forms

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  1. coated w/ polymers that resist sln in gastric fluid but disintegrate in the intestine
    enteric-coated dosage forms
  2. 3 instances when enteric coating is used
    • 1) drugs not stable in stomach
    • 2) drugs needed further down past stomach
    • 3) drugs that irritate the stomach
  3. enteric coatings are predominantly ____-charged polymers
  4. what type of absorption window would benefit from ER dosage form?
    BROAD absorption window
  5. what type of clearance would benefit from ER dosage from?
    FAST blood clearance
  6. what type of absorption rate would benefit from ER dosage form?
    FAST absorption (changes RLS to drug release, not absorption)
  7. controlled by polymer coating solubility, thickness, porosity
    diffusion (coating)- controlled release
  8. matrix is a polymer - prevents rapid dissolution by binding the drug or slowing water penetration
    erosion (matrix)-controlled release
  9. long chain polymers that form 3D network & expand upon hydration, thereby releasing the drug
    hydrogels as matrix for controlled release
  10. controlled-release dosage form used when rapid onset is also needed
    multistage release system
  11. dosage form w/ drilled hole in tablet containing osmotically active compartment
    OROS (osmotic-controlled release oral system)
  12. good candidates for OROS
    • short half life
    • potent drugs
    • water soluble
    • prolonged effect needed
  13. 2 mechanisms of bioadhesion
    • 1) adherence by hydration
    • 2) adherence by charge
  14. 2 most common mucoadhesive polymers
    • 1) crosslinked polyacrylic acid (carbopol, carbomer)
    • 2) chitosan
  15. 2 other strategies to retain drug in narrow absorption window
    • 1) bioadhesives
    • 2) GRDD (gastro-retentive drug delivery)
  16. common excipients for controlled release forms
    hypromellose, cellulose
  17. unintended, rapid drug release in a short period of time of the entire amount of drug contained in a modified release dosage form
    dose dumping
  18. primary reason for solid dose form instability
    presence of moisture
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PHRD5925 Pharmaceutics Lecture 18 - Controlled-Release Oral Dosage Forms
2014-04-21 09:03:25
Controlled Release Oral Dosage Forms

Controlled-Release Oral Dosage Forms
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