Ceutics Exam #1

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leamusic
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274036
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Ceutics Exam #1
Updated:
2014-05-11 14:01:24
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Ceutics Exam
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Ceutics Exam #1
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Ceutics Exam #1
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  1. Bioavailability Factor of PO drugs
    • Drug substance physiologic properties
    • Dosage form characteristics
    • Pharmaceutical excipients
    • Physiologic factors & pt characteristics
  2. Drug substance physiologic properties
    • Particle size
    • Crytalline or amorphous form
    • Lipid/water solubility
    • Hydration
    • Salt form
    • pH & pKa
  3. Dosage form characteristics
    • Disintegration rate
    • Dissolution rate
    • Product age & storage
  4. Pharmaceutical excipients
    • Filler
    • Binders
    • Coatings
    • Lubricants
    • Surface active agents
    • Disintegrating agents
  5. Physiologic factors & pt characteristics
    • Gastric emptying time
    • Intestinal transit time
    • GI abnormality/pathologic condition
    • Gastric contents
    • Food 
    • Fluid
    • GI pH 
    • Drug metabolism (gut & 1st pass)
  6. Sublingual Route 
    Advantages (2)
    • Often faster absorption than PO
    • Avoid 1st pass metabolism
  7. Sublingual Route
    Disadvantages (3)
    • Drug taste
    • Degradation by salivary enzymes (amylase)
    • Unintended swallowing
  8. Pulmonary route 
    Advantages
    • Fast absorption - avoids 1st pass
    • Allows for local treatment or systemic treatment
  9. Pulmonary route
    Disadvantages
    • Large variability in dose delivery to alveoli 
    • Large variability in pt techniques for device utilization 
    • Narrow particle size distribution required for optimal therapeutic effect 
    • Anatomical barriers to reaching alveoli
  10. ADME
    • Absorption
    • Distribution
    • Metabolism
    • Excretion 
    • (LADME:Liberation)
  11. Phase I Metabolism
    • CYP450
    • Site: smooth ER fo liver, lung, & kidney 
    • Oxidation
    • Reduction 
    • Hydrolysis
  12. Phase II Metabolism
    • Conjugation, generally increases hydrophilicity for excretion by kidney or via bile
    • Methylation
    • Sulphation 
    • Acetylation
    • Glucuronidation 
  13. Phase III Metabolism
    • Transporters
    • Site: liver, intestine, kidney, brain
  14. Low bioavailability causes
    1st pass effect

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