1. Cyclodextrin
    • Hydrophobic interior
    • Hydrophillic cavity face
    • Does not form covalent bonds
  2. Applications of cyclodextrin
    • Increase drug solubility
    • Increase drug stability
    • Mask the taste of drug in solution
  3. Chemical Structure of three types of cyclodextrin
    • A: six sugar ring
    • B: seven sugar ring, most commonly used
    • G: eight sugar ring
  4. Chelates
    • Chemicals that form soluble complex molecules with certain metal ions
    • Increases drug stability
  5. EDTA
    Adding EDTA to drug formulations can prevent many types of chemical oxidation
  6. EDTA Chelation Therapy
    • EDTA forms complexes with toxin
    • Immune system recognizes EDTA as a threat and detroys EDTA + toxin
    • Used for lead and heavy metal poisoning
  7. Metal Complexes are held together by noncovalent bonds
  8. Noncovalent bonds are involved in the formation of inclusion compounds
  9. A-Cyclodextrin is a seven sugar ring
    • false
    • 6 sugars
  10. Three important properties of cyclodextrin that are responsible for its ability to increase drug solubility
    • cage like structure
    • interior hydrophobic, water insoluble drug can be entrapped in cavity
    • cavity entrances are hydrophillic
  11. Explain why chelate can increase drug stability in solution
    • chelate froms complex with metal ions in solution
    • metal ions are most detrimental in oxidation
    • after chelation metal ions exhibit deminished reactivity
  12. Cyclodextrin could be used to enhance physical and chemical stability of proteins. Why?
    • CD can minimize protein aggregation
    • Protein too large to be entrapped in CD
    • EDTA removes metal ions
  13. Four major interactions among biological molecues
    • Hydrogen bond
    • Electrostatic attractions
    • Van der Waals interactions
    • Hydrophobic forces
  14. Protein binding effects on drug action
    • distribution
    • Tissue penetration
    • clearance
    • interactions
  15. Which of the following can be used to describe the hydrogen bond

  16. Which of the following atoms are the electronegative atoms involved in hydrogen bond?

  17. Electrostatic attratction is proportional to the square of the distance between charges (T/F)
    False, Inversely proportional
  18. Protein Binding affects the distribution of small molecule drugs (T/F)
  19. Generally, only the free drug is available for diffusion and transport to its target cells (T/F)
  20. Which of the following interactions is the driving force for the folding of globular proteins?

  21. Which is the most abundant protein in the plasma

    A. Albumin
  22. Why EDTA chelation therapy is often administered together with essential nutrients?
    A. nutrient enhances binding of EDTA to toxin
    B.EDTA may remove important elements (protein, calcium, vitamins, etc.) from the body.
    C. Nutrient enhances ability of EDTA to remove toxin
    D. All
    EDTA may remove important elements (protein, calcium, vitamins, etc.) from the body.
  23. Explain how the drug/protein complex can act as a storage depot in the blood circulation.
    • only free drug can diffuse into target cells
    • drug/protein complex stays in blood for prolonged time
    • d/p complex is reversible during the circulation the complex will dissociate and release the gree drug.
  24. Diffusion
    mass transfer of individual molecules
  25. osmosis
    passage of water through a semipermeable membrane to dilute solution
  26. Ultrafiltration
    • separate nanosized particles or macromlecules by differentially permeable membrane
    • Cross flow filtration
    • Tangential Flow filtration
    • Water purification and food industry
  27. Osmotic Drug Release system
    Drug layer, push layer and semipermeable membrane
  28. advantage of ultrafiltration vs dead end filtration
    • Dead end results in a build up of product which may damage product
    • Ultrafiltration is faster, recovers more product and has a higher filtration rate.
  29. osmosis is the passage of solvent and solute through a semipermeable membrane (T/F)
    False, just solvent
  30. Dialysis is a separation process based on unequal rates of passage of solutes and solvent through differentially permeable membrane. (T/F)
  31. Which of the following processes is called cross-flow filtration or tangential flow filtration?

    C. Ultrafiltration
  32. Which of the following processes is similar to reverse osmosis?

    B. Ultrafiltration
  33. Which of the following require energy?

    A. Ultrafiltration
  34. Which of the following does not require a membrane?

  35. Eating salty food makes your thristy why?

  36. Two advantages of ultrafiltration in comparison to dead end filtration.
    • Higher filtration rate
    • Higher product recovery
  37. Fick's First Law

    J=D (dC/dx)
    • J= diffusion flux
    • D= diffusion coefficient
    • C= drug concentration
    • X= distance of movement perpendicular to the barrier
  38. Lag time
    time required for a drug to establish a uniform concentration gradient
  39. Biopharmaceutical classification system
    • High Permeability: 12
    • Low Permeability: 34
    • High Low
    • Solubility
  40. Dissolution
    process of releasing drug out of the solid formulation into solution
  41. Three unique structures of small intestine that account for its large surface area
    • Microvilli
    • Villi
    • Circular folds
  42. O2 and CO2 cross the cell membrane faster than H2O.
  43. Cell membrane is composed of two opposing layers of lipids, their hydrophillic tails face one another to form the bilayer core (T/F)
  44. Fick's First law of diffusion refers to a nonsteady-state flow. (T/F)
  45. The early stage of drug diffusion is the non-steady state condition
  46. What is the driving force for Fick's first law?

    A. Concentration gradient
  47. The diffusion coefficient of a drug depends on:

    D. All
  48. Biopharmaceutical classification systems classifies drugs in terms of their:

    A. Solubility and permeability
  49. Which of the following BSC classes is poorest candidate for oral administration?
    A. 1
    B. 2
    C. 3
    D. 4
    4 is worst, 1 is best
  50. Absorption of BSC class 2 drugs can be improved in the presence of fatty food. Why?
    • Fatty food induces bile secreation.
    • Bile enhances drug solubility.
  51. Disintegration Test
    To determine wheter tablets or capsules disintegrate within the prescribed time when placed in a liquid medium
  52. Dissolution
    process by which drug molecules are released from solid phase into a solution phase.

    • only drugs in solution can exert effects
    • dissolution is the limiting step in absorption
    • dissolution rate reflects the amount of drug dissolved over a given time period
  53. Diffusion layer model
    • stationary layer of solvent in which the solute molecules exist in concentration from Cs to C.
    • Diffusion layer can be considered as a diffusion barrier as the membrane in the diffusion process.
  54. Higuchi Model
    • Q= drug released per unit area of exposed surface
    • A= total amount of drug in unit volume of matrix
    • D=Diffusion coefficient of the drug in matrix
    • Cs= solubility of drug in polymeric matrix
    • T=time
  55. Biorelevant medium
    Media represents gastric or intestinal environments
  56. Shelf Life
    taime at which the active ingredient has decreased to 90% of its original concentration (t90)
  57. Half Life
    Time at which active ingredient has decreased to 50% of its original concentration (t1/2)
  58. 5 forms of drug instability
    • I. Chemical Stability
    • II. Toxicologic Stability
    • III. Therapeutic stability
    • IV. Physical stability
    • V. Microbiologic Stabilty
  59. Major pathways for chemical instability (3)
    • Hydrolysis
    • Oxidation
    • Photolysis
  60. Ideal storage conditions for drugs
    • cool
    • dry
    • dark
  61. Transporter responsible for drug resistance in cancer chemotherapy:

    A. Efflux
  62. Most accurate method ot study intestinal drug transportation/absorption.

    D. In vivo
  63. Stress may affect drug absorbtion in GI tract (T/F)
  64. Poor drug absorption in the stomach is mainly because of its small surface area (T/F)
  65. Most drugs are absorbed in the GI tract by the active transport mechanism (T/F)
  66. Transporters are not involved in passive diffusion (T/F)
  67. Dissolution profile is more dependent on the chemical structure of the active pharmaceutical ingredient (T/F)
    False, determined by formulation chemical structure -> absorption
  68. Three examples of modified release dosage:
    • Extended Release
    • Enteric coated
    • Delayed Release
  69. 2 differences between carrier-mediated passive transport and active transport
    • carrier mediated passive transport
    • no energy required
    • transport drug from high to low concentration
    • Active energy is needed
    • can transport from low to high
  70. Schematic diagram of drug release process from a tablet by disintegration and dissolution
    • Tablet or capsule-----------------V
    • Disintegration
    • Granules or aggregates---->Disolution ----->Drug In Solution-----(absorption)--->Drug in Blood
    • Deaggregationother fluid and tissues
    • Fine Particles----------------------^
  71. First order Rate reaction
  72. Stress testing
    exaggerated storage conditions
  73. Meeting the disintegration test assures the drug release from the formulation (T/F)
  74. Dissolution is the limiting step in the absorption of drugs with low permeability.
  75. Dissolution provides information on drug absorption across the GI tract (T/F)
  76. USP apparatus 1 is a basket method for the dissolution test
  77. According to Higuchi model, the amount of drug released is proportional to
    A. T
    B. T2
    C. T1/2
    D. T 1/3

    C. T1/2
  78. Wich of the following aparatus is the first choice for immediate release formulation?
  79. Pharmaceutical product should be kept in refridgerator to increase stability (T/F)
  80. Bathroom is a good place to store product (T/F)
  81. SLEP is available to retail pharmacy (T/F)
  82. Stability testing needs to be conducted int he same container closure system proposed for marketing (T/F)
  83. Which mechanism is most often responsible for chemical degradation?

    B. Hydrolysis
  84. Most common shelf life of products?
    1-2 yr
    2-3 yr
    3-4 yr
    4-5 yr
    2-3 yr
  85. which of the following tests is used to identify the likely degradation products?

    B. Stress test
  86. What is the storage condition for the accelerated testing of drug products intended for storage at room temperature?

  87. What is the testing frequency for accelerated stability testing?

    C. 0, 3 and 6 months
  88. Zero Order degradation
    • C vs T
    • Linear
    • Decline over time
  89. First order degredation
    • lnC vs C
    • Linear
    • Decline
  90. Five forms of instability which can lead to the rejection of a drug product
    • Chemical
    • Physical
    • theraputic
    • toxicologic
    • microbiologic
  91. 4 strategies to prevent oxidation in pharmaceutical product
    • fill container with inert gas
    • add chelating agent
    • keep at low temp
    • add antioxidants
  92. What is the DP?

    Vinyl acetate MW=86
    Poly (vinyl acetate) MW=172,000
    DP = 172,000/86 = 2000
  93. Protein is a natural polymer, it is composed of 20 different types of amino acids. Select the best description of protein from each category:
    • Copolymer
    • Linear
    • Random
  94. 3 strategies of using polymer in controlled drug release
    • bioderadable carrier
    • rate controlling membrane
    • diffusion matrix
  95. Excipients are used in most drug formulations and they are essential to product performance (T/F)
  96. Drug permeability in a polymer's crystalline region is better than that in the amorphous region (T/F)
  97. All polymers have Tg and TM. (T/F)
  98. Glass transition can only be observed in amorphous region (T/F)
  99. Polymer with high Tg
    has ring group
  100. Why does a polymer have Tg and Tm?
    amorphous region and crystaline region
Card Set