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2011-01-31 21:39:24

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  1. Advantages and disadvantages of each drug delivery route: Oral
    • Advantages
    • Most common. The simplest, easiest, most economical method of administration.
    • High patient accaptance and adherence to a regimin.
    • Disadvantages
    • First pass effect
    • Not suitable for the drugs poorly absorbed or significantly destroyed in GI tract.
  2. Advantages and disadvantages of each drug delivery route: Parenteral
    • Advantages
    • Reliability, precision of dosage, timed control of onset of action
    • Disadvantages
    • Disconfort, possibility of infection, tissue damage, need trained personnel
  3. Advantages and disadvantages of each drug delivery route: Mucosal
    • Advantages
    • Avoid the first pass effect, relative ease and convenience
    • Disadvantages
    • Small area of absorption (nasal, oral), taste (oral)
    • Delivery limited by molecular weight of a drug
    • Local tissue irritation, sensitivity to pathologic conditions
  4. Advantages and disadvantages of each drug delivery route: Transdermal
    • Advantages
    • Easy to apply and remove
    • Avoid the first pass metabolism
    • Disadvantages
    • Lag time to reach steady state (2-6 hrs)
    • Limited by polarity, size of the drug
    • My need permeation enhancement via chemical and/or physical means
  5. Advantages and disadvantages of each drug delivery route: Targeted
    • Advantages
    • Reduce sede effects of drugs on heathy tissues and enhance drug uptake by targeted cells
    • Disadvantages
    • ?
  6. Advantages and disadvantages of each drug delivery route: Local
    • Advantages
    • Reduced systemic side effects
    • Reduced dose requirement
    • Disadvantages
    • Need to know the locations to be treated
  7. Medical motivations of drug delivery systems
    • Increase efficacy, enable activities
    • Decrease toxicity
    • Increase patient compliance, convenience
    • Enabling tools
  8. Economic motivations of drug delivery systems
    • Increase patent life, market share with unique drug delivery systems
    • Increase patient and physician acceptance
    • Avoid costs of developing a new chemical entity
  9. List three areas where tablets transport.
    • Stomach
    • SI
    • Colon
  10. List pH of main parts of GI Tract
    • Stomach: 1-3
    • SI: 5-8
    • Colon: 5-8
  11. List GI transit times for tablets
    • Cumulative (hrs)
    • Stomach: 0.5
    • Jejenum: 1.75
    • Ileum: 3.25
    • ICJ 4.5
    • Colon: 24.5
  12. List surface area of GI tract (m^2)
    • Duodenum: 2 (where most abs happens)
    • Jejnum: 180
    • Ileum: 280
    • Colon: 1.5
  13. Define enteric coating
    A coating around a tablet that will keep it from dissolving until it reaches SI (ph ~7)
  14. Summarize the five factors that affect absorption of drugs from tablets
    • Permeability-how easy drug goes through membrane
    • Dissolution-dissolving
    • Efflux-along with metabolism, destroys drug
    • Metabolism
    • Formulation-how smart tablets are made (this controls dissolution)
  15. Know that solid form affects dissolution
  16. Know that drugs can exist in polymorphs, solvates, and amorphous solid forms
  17. Know that amorphous forms give higher bioavailability than crystalline forms
  18. Know the steps in development of the optimum solid form
  19. Know the parameters of the unit cell (a, b, c….)
  20. Know the estimated cost of the ritonavir problem
  21. Know steps in controlling the solid form
  22. Know that an X-ray diffraction pattern is a fingerprint that can be used to identify a solid form
  23. Know the four aspects of formulation
  24. Know the factors used to select the best salt of Ketoprofen
  25. Know why the solubility of a carboxylic acid increases at high pH
  26. In the case study know why we want amorphous drug
  27. Know at least 3 types of tablets
    • Simple Uncoated Tablets
    • No coating
    • Aspirin
    • Effervescent Tablets
    • Alka-seltzer
    • Sugar Coated Tablets
    • Prefilm coating
    • Advil
  28. Know that granulation enlarges the particles and improves flow
  29. Know that the more binder the larger the particles
  30. Know that in a noninteracting formulation the drug particles are not altered or changed
  31. Know that content uniformity means that each tablet/capsule contains between 85-115%
  32. Know that the KV problem involved oversize tablets
  33. Know that capsules are classified as either hard or soft
  34. Know two advantages and two disadvantages of capsules
    • Advantages:
    • Hard shell capsules allow for a degree of flexibility of formulation not obtainable with tabs
    • Bioequivalence studies of tablet formulations may be conveniently blinded by inserting tablets into capsules
    • Disadvantages:
    • More costly
    • More likely to become lodged in esophagus
  35. Know best ways to prevent esophageal adhesion
    • Take medication with water
    • Continuous flow of saliva
    • Remain standing for 90 secs
  36. Know the largest and smallest capsule sizes
    • Largest: 000 (1.096 g/cm^3)
    • Smallest: 5 (0.104 g/cm^3)
  37. Know steps in capsule filling
    • Step 1 Rectification: The empty capsules are oriented so that all point the same direction
    • Step 2 Separation of caps from bodies
    • Step 3. Dosing of fill material.
    • Step.4. Replacement of caps and ejection of 
    • filled cap‐sules:
    • Step 5. Ejection of the Capsules
  38. Know formulation design for first in human testing
    • First in human studies are done during drug 
    • Development
    • The dose is based on the No Observed Adverse Event Level seen in Animals
    • If possible the drug is placed in a capsule without other ingredients
    • This means the drug must be in its most soluble form that is stable and handleable
  39. Know specifications for capsules for first in human testing
    Specifications: moisture, assay, impurities, dissolution
  40. Know advantages & disadvantages of soft gelatin capsules
    Look up
  41. Know that soft gelatin capsules can contain a suspension or a liquid