PHA 327-Suppositories

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Author:
kyleannkelsey
ID:
219240
Filename:
PHA 327-Suppositories
Updated:
2013-05-12 13:39:47
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PHA 327 Suppositories
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PHA 327-Suppositories
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  1. What are suppositories?
    • Solid dosage forms intended for insertion to the rectum, vaginal cavity or urethra
    • Systemic or local effects
    • Liquefies after insertion
  2. How large are infant rectal suppositories?
    1 gram
  3. How large are adult rectal suppositories?
    2 grams
  4. What is the shape of rectal suppositories?
    Cylindrical and tapered at one or both ends
  5. What is the shape of vaginal suppositories?
    • Cone shaped
    • Oviform
  6. What is the weight of most Vaginal suppositories?
    3-5 grams
  7. What are vaginal suppositories also called?
    Pessaries
  8. What are urethral suppositories also called?
    Bougies
  9. What is the shape of urethral suppositories?
    Pencil shaped
  10. What situations are rectal suppositories indicated for?
    • Oral route not available
    • The drug is not useful when applied orally
  11. What are the disadvantages of rectal suppositories?
    • Slow/incomplete absorption
    • Intra/inter subject variation
    • Local irritation
    • Difficult to manufacture
    • Long prep time
    • Stringent storage conditions
  12. What are rectal suppositories intended for?
    • Constipation
    • Hemorrhoids
  13. What are rectal suppositories used for systemically?
    • Analgesics
    • Antispasmodics
    • Tranquilizers and Sedatives
  14. What are the physiological factors that affect suppository absorption?
    • Size
    • Content
    • Composition
  15. What are the Physicochemical factors that affect suppository absorption?
    • Solubility
    • Concentration
    • Particle size
    • Partition coefficient
    • Degree of ionization
  16. What are the Physiochemical factors that affect suppository absorption?
    • Melting point
    • Solubility
    • Reactivity
    • Polymorphism
  17. Describe the Retum:
    • 5-20 cm in length
    • 2-3mL of mucous fluid prior to defecation
    • No villi or microvilli
  18. What three physiological issues can effect rectal suppository absorption?
    • Tissue dehydration
    • Colonic obstruction
    • Diarrhea
  19. When using a systemic suppository, what must be done prior to insertion?
    Evacuation
  20. Why is evacuation needed prior to use of systemic suppositories?
    To increase absorption
  21. How can evacuation be carried out?
    Evacuation enema
  22. Why is it advisable to keep the suppository in the lower part of the rectum?
    To avoid the upper hemorrhoid vein, as it leads to portal circulation
  23. What part of the rectum should patients be advised to put the suppository in and why?
    • The lower part (nearest to anus)
    • To avoid portal circulation
  24. What percent of drug administered rectally goes directly into circulation?
    50-70%
  25. What are the names of the Hemorrhoid veins?
    Upper, middle and lower
  26. What veins absorb rectal suppository drugs?
    Hemorrhoid veins
  27. What happens to rectal drugs after absorption?
    • Available for systemic effect
    • Some pass portal circulation
    • NO LIVER
  28. What is the pH of rectal fluids?
    7-8
  29. What is the effective buffer capacity of the rectal fluids?
    None
  30. The rectal mucosa is preferentially permeable to what type of drugs?
    Unionized
  31. How can rectal absorption be enhanced physiologically?
    By changing the pH to one where the most drug is unionized
  32. When selecting a base and determining the release of the drug from that base, what factors should you evaluate?
    The Lipid water partition coefficient
  33. A lipophilic drug will not release well in the hydrophilic rectal fluids if it is in what type of base?
    Fatty base
  34. What type of drugs can be used in suppository Fatty bases?
    Water soluble salts
  35. What type of base would you use for a lipophilic drug or a hydrophilic drug?
    Water soluble base
  36. What is the most common water soluble suppository base?
    PEG
  37. What is the rate limiting step suppository absorption?
    • Partitioning of the drug from the suppository base
    • NOT THE RATE AT WHICH THE DRUG CREATES A SOLUTION IN THE RECTAL FLUIDS
  38. Will the rate of absorption continue to rise with higher rectal concentration?
    No, plateaus
  39. What happens to the suppository base after insertion?
    Melts or softens
  40. What can affect the melting or softening of suppository bases?
    The exipients
  41. What are the properties of an ideal suppository base (7)?
    • Melts at 37.5 degrees C in presence of mucous secretiosn
    • Easy to handle, doesn't break or melt
    • Does not leak from rectum
    • Stable in storage
    • Non-irritating
    • Compatible
    • No meta-stable forms
  42. What are the three classifications of suppository bases?
    • Oleaginous
    • Water soluble
    • Water dispersible
  43. Give two examples of oleaginous bases:
    • Cocoa butter (Theobroma oil)
    • Cocoa butter substitutes
  44. Give two examples of Water soluble bases:
    • Polyethylene glycol mixes
    • Glycerinated gelatin
  45. Give two examples of Water dispersible bases:
    • Polyethylene glycol derivatives
    • Cocoa butter substituted with surfactants
  46. Describe the appearance of Cocoa butter:
    yellowish white with chocolate scent
  47. What is Cocoa butter composed of?
    Glycerol esters of various FAs
  48. What is the most widely used rectal suppository base?
    Cocoa butter
  49. Why is Cocoa butter so widely used?
    It meets most of the requirements of an ideal base
  50. What are the four main advantages of Cocoa butter?
    • Melts at 30-36 degrees C
    • Rapid melting and cooling
    • Non-irritating
    • Miscible with many drugs
  51. What is the disadvantage of Cocoa butter/Oleaginous bases?
    • Polymorphism
    • Adherence to the mold
    • Softening point to low for hot climates
    • Poor water absorption
    • Melting point lowered by soluble exipients
  52. Describe how Water soluble bases work:
    • Do not melt at body temperature
    • Dissolve in body secretions
  53. What is Glycerol suppository base B.P. made of?
    • 14% gelatin
    • 70% Glycerol
    • QS 100% with water
  54. What is glycerol-geltin base U.S.P. composed of?
    • 20% gelatin
    • 70% Glycerol
    • QS 1005 with water
  55. What type of base is Hygroscopic?
    Glycerinated gelatin bases
  56. What is Hygroscopic?
    Tendency to absorb water
  57. What are polyethylene glycols composed of?
    Ethylene oxide and water of various lengths
  58. What do the numerical designations after PEG indicate?
    The average MW
  59. What PEG MWs are clear colorless liquids?
    300, 400 and 600
  60. What PEG MWs are Semisolids?
    600-1000
  61. What PEG MWs are wax-like white solids?
    Over 1000, increasing hardness as MW increases
  62. What is the melting point for most PEGs?
    50 degrees C
  63. If PEG bases melt at 50 degrees C, how is the drug released at body temperature?
    • Dissolve
    • DOESNT MELT
  64. You can blend different MW PEGs together to alter what characteristics?
    • Melting point
    • Physical Characteristics
    • Dissolution rate
  65. What is the iodine value?
    The grams of iodine that react with 100 grams of Fat or unsaturated material
  66. Why is the iodine value important?
    • Correlates with:
    • Decomposition by moisture, acids and oxygen
  67. What is the solidification value for a suppository base?
    The time it takes to solidify once cooled
  68. What is the Melting range for a suppository base?
    Initiation and endpoint of melting
  69. What are the possible type of suppository base orgin?
    Natural or synthetic
  70. What is the acid value of a suppository base?
    The mg of potassium hydroxide needed to neutralize the free acid in 1 gram of base
  71. What relative Acid Value is good for suppositories?
    Low
  72. Why is a low Acid Value good for suppository bases?
    • Complicate formulation work
    • React with ingredients
    • Cause irritation
  73. What is the water number for a suppository base?
    The grams of water that can be incorporated into 100 grams of Fatty base
  74. How can you increase the Water number of a fatty suppository base?
    Addition of surfactants
  75. What are the four methods of suppository manufacture?
    • Hand Molding
    • Compression molding
    • Pour molding
    • Automatic molding
  76. What is the oldest and simplest method for making suppositories?
    Hand molding
  77. Describe Hand molding:
    • Trituration of drug and base
    • Rolled into a cylinder with steel blade spatula
    • Divided
  78. What type of prescription could you use hand Molding for?
    • Few suppositories needed
    • Cocoa butter base
  79. What is the process of Compression Method of suppository molding?
    • Make a paste of the base and ingredients
    • Compress in a die
  80. What do you need to determine prior to compression molding?
    The compressibility of the base in the dies
  81. What is the most commonly used method for suppository production?
    Pour molding
  82. Describe the technique of pour molding:
    • Base is melted
    • Ingredients are added
    • Suppositories are cooled
  83. What is the output of a rotary automatic molding machine?
    3,500-6,000 suppositories per hour
  84. What type of suppositories need to be refrigerated?
    Cocoa butter and glycerinated gelatin
  85. What type of suppositories can be stored at room temperature?
    PEG
  86. What type of molds can suppositories be stored in?
    Metal or Plastic
  87. What are the advantages of disposable plastic suppository molds?
    • Cheap to change mold shape
    • No need to expensive molds or wrappings
    • Eliminate the wrapping process
  88. What are the five tests that should be performed on Suppositories?
    • Melting range test
    • Liquefaction test for rectal suppositories
    • Disintegration test in-vitro
    • Stability testing
    • Breaking test

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