PHRD5925 Pharmaceutics Lecture 19 - Parenteral Delivery

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daynuhmay
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271320
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PHRD5925 Pharmaceutics Lecture 19 - Parenteral Delivery
Updated:
2014-04-21 05:26:22
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Parenteral
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Parenteral
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  1. 5 criteria for parenteral formulations
    • 1) sterile
    • 2) non-pyrogenic
    • 3) neutral pH
    • 4) tonicity
    • 5) colloidal stability
  2. 2 approved methods for water purification
    • 1) reverse osmosis
    • 2) distillation
  3. excipients that prevent oxidation (3)
    • antioxidants
    • EDTA
    • kept under inert air
  4. most stable type of glass
    borosilicate glass
  5. 3 processes of lyophilization
    • 1) freezing
    • 2) primary drying (sublimation)
    • 3) secondary drying (desorption)
  6. function of primary sublimation
    remove non-bound water
  7. function of secondary desorption
    remove bound water
  8. additives for lyophilization
    • bulking agent (mannitol)
    • cryoprotectant
  9. physical instability challenges posed by peptide/protein drugs
    • denaturing/unfolding
    • aggregation
    • surface adsorption
  10. chemical instability challenges posed by peptide/protein drugs
    • deamidation
    • cleavage
    • oxidation
    • disulfide formation
  11. protein/peptide drug modification that prolongs half-life due to decreased excretion and more resistance to degradation
    PEGylation
  12. challenges of developing nucleic acid therapeutics (3)
    • serum stability of nucleic acid
    • stability of drug product 
    • delivery into cell & nucleus
  13. most useful drug form for anticancer drugs
    intravenous drug delivery
  14. 3 types of intravenous drug delivery systems
    • 1) antibody-drug conjugate
    • 2) polymer-drug conjugate
    • 3) nanoparticles
  15. size of controlled-release nanoparticles
    10-500nm
  16. common excipients for IV drug delivery
    • poly-lactic acid (PLA)
    • albumin
    • phospholipids
    • polysacharrides
    • PEG
    • combo of above
  17. vesicles made of phospholipids & PEG that form bilayers and stably trap drug inside
    liposomes

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