Suppository Flashcards

(76 cards)

1
Q

What are Suppositories?

A
  1. Solid dosage forms
  2. administration via any of several body orifices
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2
Q

What happens to suppositories when they enter the body cavity?

3

A

melt, soften, or dissolve in the body.

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3
Q

What are the advantages of Suppositories? (8)

A
  1. infants/small children, or ppl who cannot take medications orally
  2. Severely debilitated patients
  3. Post operative people who cannot be administered oral medication.
  4. Suffering from severe nausea or vomiting.
  5. parenteral route unsuitable.
  6. Large dose drugs easier
  7. Mask unpleasant taste/smell of drug.
  8. Preferred for drugs that irritate oral/gastric mucosa when taken orally.
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4
Q

What are the advantages of Suppositories for Systemic Action?

2

A
  1. Drugs destroyed or inactivated by pH or enzymatic activity of the stomach are ideal candidates.
  2. Partially avoid first pass metabolism (50-70%).
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5
Q

What is a physical factor of drug absorption from rectal suppositories?

A

Human rectum.

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6
Q

Delete

A

Delete.

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7
Q

What are the 3 Physiologic Factors of Drug Absorption from Rectal Suppositories?

A
  1. pH (neutral) and lack of buffering capacity of the rectal fluids.
  2. Circulation Route.
  3. Colonic Content.
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8
Q

What does Colonic Content do?

A

interferes with the interaction of the drug and the absorbing surface.

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9
Q

How does the Circulation Route do?

A
  1. Drugs bypass the portal circulation into general circulation
  2. Lymphatic circulation assists rectal absorption.
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10
Q

How does the pH (neutral) and lack of buffering capacity of the rectal fluid play role?

A

Drugs will not change chemically.

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11
Q

What are the 3 Physicochemical Factors of Drug Absorption from Rectal Suppositories?

A
  1. Particle Size.
  2. Lipid-Water Solubility.
  3. Nature of the Suppository Base.
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12
Q

What does the Nature of the Suppository Base determine?

2

A
  1. Ability to melt, soften or dissolve at body temperature.
  2. Ability to spread
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13
Q

How does the Lipid-Water Solubility play a role?

A

important consideration in the selection of suppository base

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14
Q

Will a lipophilic drug distributed in a fatty base in low concentration escape to aqueous surroundings as well as a hydrophilic drug?

A

No, it will not.

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15
Q

What is the relationship between the size of particle, surface area, dissolution of the particle, & absorption?

A

The smaller the particle → the greater the surface area → the more readily the dissolution of the particle → the greater the chance for rapid absorption.

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16
Q

What are the 2 Classification of Suppository Bases?

A
  1. Water-Soluble and Water Miscible Bases.
  2. Fatty or Oleaginous.
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17
Q

What are some Fatty or Oleaginous types of Suppository Bases?

A

Cocoa Butter/Fatty Base

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18
Q

What are some Water-Soluble and Water Miscible types of Suppository Bases?

A

Glycerinated Gelatin
Polyethylene Glycol Polymers (PEG)

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19
Q

At what temperature does Cocoa Butter, NF (Theobroma Oil) soften?

A

Softens at 30°.

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20
Q

At what temperature does Cocoa Butter, NF (Theobroma Oil) melt rapidly?

A

Between 30-36 °C.

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21
Q

Why is cocoa butter base favored?

A

EMOLLIENT IN NATURE, SOOTHES ORGANS

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22
Q

What does Cocoa Butter exhibit and why?

A

Polymorphism - due to the triglyceride content with rapid heating/cooling.

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23
Q

At what temperature does Cocoa Butter reach Gamma form?

A

18° C.

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24
Q

At what temperature does Cocoa Butter reach alpha form?

A

22° C.

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25
At what form is cocoa butter Metastable?
Alpha form.
26
At what temperature does Cocoa Butter reach Beta prime?
27° C.
27
At what temperature does Cocoa Butter reach Beta form?
30-35° C.
28
At what form is cocoa butter stable?
Beta form.
29
What is Glycerinated Gelatin Base used in?
Urethral & Vaginal Suppositories.
30
What is the formulation of Glycerinated Gelatin Base?
Glycerin 70 parts, Gelatin 20 parts, Water + Drug 10 parts.
31
For the creation of Glycerinated Gelatin Bases, what must happen?
Dissolve/suspend drug in water; mix with glycerin; add to gelatin slowly. Apply low heat to melt gelatin + gentle stirring. Pour on mold.
32
Are Glycerinated Gelatin Bases Hygroscopic or Deliquescent?
Hygroscopic.
33
How must Glycerinated Gelatin Bases be stored?
Store in airtight containers.
34
What is Polyethylene Glycol Suppository Bases varying in?
Varying molecular weights.
35
What varies because of the varying molecular weights of Polyethylene Glycol Suppository Bases?
Melting Point varies as function of MW.
36
What is the temperature range for PEG 300?
Tm = -15 to -18 °C.
37
What is the temperature range for PEG 1,000?
Tm = 37 - 40 °C.
38
What is the temperature range for PEG 8,000?
Tm = 60 - 62 °C.
39
How fast do Polyethylene Glycol Suppository Bases dissolve in body fluids?
Slowly.
40
What are the 5 Excipients for Suppositories?
1. Stiffening Agents. 2. Surfactants. 3. Suspending Agents. 4. Disintegrants. 5. Preservatives.
41
What are some examples of Stiffening Agents (Suppository Excipient)?
Cetyl alcohol, Stearyl alcohol, wax.
42
When are Preservatives needed as a Suppository Excipient?
Needed when suppositories are hygroscopic.
43
How are Suppositories Prepared?
Molding.
44
How is molding of Suppositories done?
Melt Base + Drug(s). If needed, lubricate mold with small amount of mineral oil or glycerin. Pour melted mix into mold, overfill. Allow melt to cool and congeal. Remove from mold, scrape off excess.
45
What is the length & weight of adult Rectal Suppositories?
~ 2 g & 1-1.5 inches long.
46
What is the length of infant Rectal Suppositories?
Half the adult size.
47
What are some Local and systemic effects of Rectal Suppositories?
Sedatives, tranquilizers and analgesics.
48
What is the Largest single use Rectal Suppository?
OTC hemorrhoidal remedies.
49
For Vaginal Suppositories, is first pass metabolism avoided for systemic drugs?
Yes.
50
For the vagina, what is a suppository preferred over?
Gels, foams.
51
Is the vagina acidic?
Yes.
52
What does the acidity of the vagina vary with?
Age, hormonal fluctuations, infection.
53
What is the avg weight of Vaginal Suppositories?
3 to 5 g.
54
What kind of Vaginal Suppository base is the most convenient?
Water-soluble bases.
55
What base of Vaginal Suppositories tend to 'leak'?
Oleaginous bases.
56
What do Progesterone compounded suppositories vary widely in?
Hormone replacement therapy.
57
Are Antifungal & antibacterial preparations of vaginal suppositories widely used?
Yes.
58
Are Vaginal Tablets or vaginal suppositories used more?
Vaginal tablets.
59
Why are vaginal tablets used more than vaginal suppositories?
Easier to manufacture, more stable, less messy to handle.
60
What are vaginal tablets intended to do?
Disintegrate within the vagina.
61
What is the Special Excipient of Vaginal Tablets?
Mucoadhesives.
62
How are suppositories Packaged?
May be wrapped or unwrapped, Glass or plastic containers.
63
How are suppositories stored?
Room temperature or under refrigeration, Moderate humidity.
64
How are Glycerinated gelatin suppositories packaged in?
Glass, tightly-closed containers.
65
How are Cocoa butter suppositories packaged?
Individually wrapped.
66
What are the Compendial Requirements of suppositories?
1. Disintegration test. 2. Dissolution test. 3. Content uniformity. 4. Melting Point Testing. 5. Loss on drying. 6. Weight uniformity.
67
How is weight uniformity of suppositories measured?
Weigh 20 suppositories. Not more than 2 deviate by > 5% from average weight. Not more than 10%.
68
What does Melting Point Testing of suppositories verify?
Suppositories melt at body temperature.
69
What does Loss on drying of suppositories for?
Packaging container integrity.
70
What must be measured to check Loss on drying of suppositories?
Measure weight gain or loss of suppositories after storage.
71
For Patient Counseling of the use of suppositories, if suppositories are stored at 4°C, what must happen?
Warm to room temperature before insertion.
72
For Patient Counseling of the use of suppositories, what must you do with cocoa butter suppositories?
Rub cocoa butter suppositories gently with fingers to melt surface - lubrication.
73
For Patient Counseling of the use of suppositories, what must you do with Glycerinated gelatin or PEG suppositories?
Should be moistened with water before insertion.
74
For the Nonsterile Compounding Beyond-Use Date (BUD) Flowchart, what is the first step?
Identify the Dosage Form / Type of Preparation.
75
For the Nonsterile Compounding Beyond-Use Date (BUD) Flowchart, if it’s a solid with an active ingredient from a manufactured product, what is the BUD?
BUD of 25% of time remaining until product’s expiration date or 6 months, whichever is earlier.
76
For the Nonsterile Compounding Beyond-Use Date (BUD) Flowchart, if it’s a solid without an active ingredient from a manufactured product, what is the BUD?
BUD of 6 months - if USP-NF substance used.