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PHRM 1300 - Final > Section 7: Suppositories > Flashcards

Section 7: Suppositories Flashcards

1
Q

What are suppositories?

A

Solid dose forms for insertion into body orifices where they melt, soften, or dissolve releasing drug for local or systemic effect

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2
Q

What are suppositories commonly used for?

A

Rectal or vaginal insertion

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3
Q

What is special about the size and shape of suppositories?

A

Easy to insert and remain in place after insertion

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4
Q

What is usually the shape of a rectal suppository for adults?

A

Bullet-shaped

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5
Q

What is usually the weight of a rectal suppository for adults?

A

2 g

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6
Q

What is usually the shape of a rectal suppository for children?

A

Small and more cylindrical

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7
Q

What is usually the shape of a vaginal suppository?

A

Ovoid/egg shape

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8
Q

What is usually the weight of a vaginal suppository?

A

5 g

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9
Q

What happens to a suppository after it is inserted?

A

It melts, softens, or dissolves and medication is released to surrounding tissues

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10
Q

What are rectal suppositories for local effect used to treat?

A

Pain, inflammation, and itchiness associated with hemorrhoids or other anal-rectal conditions

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11
Q

What do rectal suppositories for local effect usually contain?

A

Local anesthetics, vasoconstrictors, astringents, analgesics, emollients, and protective agents

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12
Q

Why are emollients often found in rectal suppositories?

A

Make things softer

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13
Q

What is found in rectal suppositories that treat constipation and why?

A

Glycerin because it has a local irritating effect and lubricates

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14
Q

True or false: some suppositories contain laxative agents

A

True

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15
Q

What are vaginal suppositories usually used for?

A

Local effect, often for an infection

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16
Q

What are less common use of vaginal suppositories?

A

Contraceptive effects, antiseptics for hygiene, or local delivery of agent to treat infection due to yeast

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17
Q

What are some common systemic conditions that can be treated with suppositories?

A
  • Nausea and vomiting
  • Migraines
  • Analgesics
  • Tranquilizers
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18
Q

What are 3 advantages for suppository systemic use?

A

1) Bypasses GI tract and first-pass metabolism
2) Drugs irritating to stomach can be given this way
3) Used for patients unable to use oral route

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19
Q

What is a disadvantage to suppository use?

A

Absorption is erratic with inter-patient variability

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20
Q

What are 2 factors that affect drug absorption for suppositories?

A

1) Physiological

2) Physicochemical

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21
Q

How long is the adult rectum and what does it contain?

A
  • 20 cm long

- Contains 2-3 mL of inert mucous fluid

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22
Q

Why is absorption efficient in the rectum?

A

Large surface area and extensive blood and lymphatic vascularization

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23
Q

What conditions can affect absorption in the rectum?

A

Inflammation, diarrhea, tissue dehydration, and presence of tumours or polyps

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24
Q

What picks up drugs that have been absorbed by the rectum?

A

Blood and lymphatic vessels

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25
Q

What is the pH of an empty colon?

A

Neutral, with little buffer capacity

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26
Q

True or false: the ionic form of the drug will be affected when it is administered via a suppository

A

False, the ionic form will not be affected

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27
Q

What physicochemical properties affect absorption of suppositories?

A
  • Solubility
  • Partition coefficient
  • Particle size
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28
Q

What properties of the base of a suppository affect absorption?

A
  • If it melts or dissolves

- If it is hydrophilic/hydrophobic

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29
Q

What MUST a suppository base to?

A

Must remain solid at room temperature but soften, melt, or dissolve at body temperature

30
Q

What is the best suppository base for fat-soluble drugs and why?

A

Cocoa butter because it melts readily at body temperature but is immiscible with colonic fluid

31
Q

What is the best suppository base for lipid-soluble drugs?

A

Water soluble polyethylene glycol

32
Q

What are the 2 types of suppository bases?

A

1) Oleaginous and water soluble

2) Miscible

33
Q

What is generally used in oleaginous bases?

A

Cocoa butter

34
Q

At what temperature range does triglyceride melt?

A

30-36 C

35
Q

What happens when cocoa butter is heated?

A

It forms polymorphs

36
Q

What happens when cocoa butter is heated beyond its melting point?

A

It forms alpha polymorphs, which is liquid at room temperature

37
Q

What material can be added to cocoa butter to lower its melting point?

A

Phenol

38
Q

What is an advantage to using semi-synthetic oleaginous bases?

A

Do not form low temperature melting polymorphs

39
Q

What are 2 examples of semi-synthetic oleaginous bases and what are they made of?

A

1) Fattibase – triglycerides from palm and coconut oil

2) Witepsol – triglycerides of C12-C18 saturated fatty acids

40
Q

What type of oleaginous bases are good for rectal irritation and why?

A

Semi-synthetic because it had soothing emollient properties

41
Q

What are 2 examples of water soluble and miscible bases?

A

1) Polyethylene glycols

2) Glycerinated gelatin

42
Q

What is unique about polyethylene glycol?

A

Comes in a variety of molecular weights, ranging from 200-8000, with lower values being liquid

43
Q

What does a higher value PEG correspond with?

A

Higher melting point

44
Q

Normally, is one PEG used or is a combination used and why?

A

A combination is used so they can fuse and incorporate the medication

45
Q

How does a PEG mixture release medication?

A

Slowly dissolving

46
Q

PEG is hydroscopic. What does this mean?

A

It needs to be protected from moisture; but must be moistened just prior to use otherwise a stinging sensation will ocur

47
Q

What type of base is usually used for vaginal inserts?

A

Glycerinated gelatin

48
Q

What does glycerinated gelatin consist of?

A

20% gelatin, 70% glycerin, and 10% water

49
Q

How does glycerinated gelatin release medication?

A

Slow, and through softening and dissolution

50
Q

True or false: glycerinated gelatin is not miscible with vaginal secretions

A

False, the two are miscible

51
Q

What is glycerin base composed of?

A

85% glycerin, 9.5% sodium stearate, 5.5% water

52
Q

What are the 3 ways to prepare a suppository?

A

1) Molding
2) Compression
3) Hand rolling and shaping

53
Q

What is the most common method of suppository preparation?

A

Molding

54
Q

True or false: when preparing a suppository, the least possible amount of heat is used

A

True

55
Q

True or false: when preparing a suppository, it is best to melt the base right on the hot plate

A

False, it is best to melt in a water bath

56
Q

How are medicinal substances incorporated when preparing a suppository?

A
  • Mix with some molten base using spatulation

- Stir into molten base and remove from heat

57
Q

When making a suppository, what ingredients are the last to be added?

A

Labile or volatile ingredients

58
Q

What are 2 tips to use when pouring suppository mixture into molds?

A

1) Stir while pouring just above congealing temperature to prevent material from settling in tip
2) Pour small excess to allow for contraction

59
Q

_____ molds should be lubricated prior to use

A

Metal

60
Q

When should excess material be scraped away when preparing suppositories?

A

After completely cooled, but before opening the mold

61
Q

Why should excess mixture be prepared when making suppositories?

A

To allow for losses

62
Q

What are the 2 types of suppository molds?

A

1) Metal

2) Plastic

63
Q

How should suppositories containing glycerin be stored?

A
  • In glass or otherwise protected from moisture

- May need refrigeration

64
Q

How should suppositories containing PEG be stored?

A

Keep away from moisture

65
Q

How should suppositories containing cocoa butter be stored?

A

Individually wrapped to prevent adhesion

66
Q

What should the patient be counselled on when using suppositories (4 points)?

A

1) Ensure all wrapping is removed prior to use
2) Tip inserted first
3) If half suppository prescribed, cu length-wise
4) Dip PEG or glycerin based products in water prior to use to avoid burning sensation

67
Q

What are 3 common calculations that need to be done when preparing suppositories?

A

1) Calibrations
2) Base displaced by medication
3) Amount of base and medication needed

68
Q

What is an important note about base displaced by medication calculations?

A

Suppositories with a mass of 2 g and a drug load less than 100 mg, the mass of base being displaced is generally insignificant and doesn’t need to be considered

69
Q

Can tablets be used as the drug source for suppositories?

A

Yes, but must take into account the weight of excipients

70
Q

What is density factor usually for?

A

Cocoa butter

71
Q

What does density factor allow for?

A

Calculation of how much base will be displaced by drug

72
Q

What is the formula for density factor?

A

df = weight of drug / weight of base displaced

PHRM 1300 - Final (6 decks)

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