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Pharmaceutics IV Test 2 > Lecture 7 Suppositories > Flashcards

Lecture 7 Suppositories Flashcards

1
Q

What is a suppository?

A

A solid dosage form intended for insertion into a body orifice where it melts, softens and/or dissolves to exert local or systemic effects.

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2
Q

Describe the different types of suppositories?

A
  • Rectal: cylindrical or conical shaped. Approx. 2 g, about 1-1.5 inches long
  • Vaginal: may be ovoid, globular, other shape. 3 to 5 g
  • Urethral: vary depending upon male/female
  • -Male: 3 – 6 mm dia, 140 mm long, 4 g wt–
  • -Female: 3 mm dia, 70 mm long, 2 g wt–
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3
Q

What are the advantages of suppositories?

A
  • Alternative to oral route
  • By-passes the first-pass effect ->Potential for higher bioavailability
  • Safe, painless, and easy administration
  • Target delivery
  • Admin a larger dose than is possible orally
  • Pediatric, geriatrics, comatose populations
  • Avoids nausea and vomiting
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4
Q

What are the disadvantages of suppositories?

A
  • Unpopular route
  • Leakage
  • Unpredictable drug absorption
  • Potential for irritation
  • Induce a poop
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5
Q

What is the ideal suppository?

A
  • Base should be non-irritating and non toxic
  • Base should be compatible with a wide variety of active ingredients
  • Uniform distribution of active ingredient throughout the dosage form
  • Melt or dissolve in rectal fluids
  • Stable–>Physically intact—not brittle, crumbling, etc. and chemically stable
  • Pharmaceutically elegant
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6
Q

What physiologic factors affect rectal absorption?

A
  • Rectum is small, approx 15-20 com long w/ 2-3 mL of fluid
  • Better absorption when the colon has been ‘emptied’
  • Bypass first pass effect, direct absorption into the lower hemmorhodial veins
  • Neutral pH of 7.2-7.8 fluids, drug may not ionize
  • Lipid-water solubility; will is be able to cross the membrane?
  • Particle size, triturate down to as fine a powder as possible
  • Nature of the base, pH nature or the drug and compatibility with the drug
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7
Q

What are the classifications of suppository bases?

A
  • Fatty or oleaginous bases: cocoa butter and synthetic triglyceride mixtures
  • Water-soluble/Water-miscible bases: glycerinated gelatin, PEG polymers, Misc Bases
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8
Q

What are the disadvantages of oleaginous/fatty bases?

A
  • Designed to melt at body temperature, gamma form

- Very sensitive to temperature

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9
Q

What are the polymorphs of cocoa butter?

A

Gamma form 18° C
Alpha form 22° C
Beta prime form 27° C
Beta form 30-35° C

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10
Q

What are the advantages of a PEG suppository base?

A
  • Polymers of varying molecular weights
  • Water-soluble
  • Relatively low melting points
  • Stable
  • Dissolve in body fluids
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11
Q

What are specific considerations for bases?

A
  • Water
  • Hygroscopicity
  • Incompatibilities
  • Viscosity
  • Brittleness
  • Density
  • Volume contraction
  • Dosage replacement
  • Weight/volume control
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12
Q

Drug Release from different bases

A
  • Oil-soluble drug w/ oily base :: Slow release; poor escaping tendency
  • Water-soluble w/ oily base :: rapid release
  • Oil-soluble drug w/ water-miscible base :: Moderate release rate
  • Water-miscible drug w/ water-miscible base :: Moderate release; based on diffusion; all water soluble
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13
Q

What approach should you consider in formulations?

A
  • Local or systemic use
  • Rectal, vaginal, urethral
  • Quick, slow, prolonged effect
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14
Q

What are the methods of preparation?

A
  • Molding (fusion) : rectal rocket
  • Compression : industrial scale
  • Hand rolling : rarely done
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15
Q

What should you consider when preparing molded suppositories?

A
  • Method most often employed both small scale and industrially
  • Elegant appearance
  • Caution must be exercised w/ heat sensitive drugs
  • Wide variety of molds available
  • Most bases suitable for molding
  • Molds often require lubrication and calibration
  • Determine the amount of base required
  • Preparing and pouring the melt
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16
Q

What should you consider when preparing compressed (compression) suppositories?

A
  • Mass of base and API is forced into special molds
  • Useful for heat-labile substances
  • Eliminates the likelihood of insoluble components settling during manufacturing
  • Some limitation to the shapes of suppositories
  • Rarely used in extemporaneous compounding
17
Q

What should you consider when preparing hand rolled suppositories?

A
  • Historical art
  • Limited to cocoa butter suppositories
  • Requires experience and good technique, lack elegant appearance
  • Does not require special equipment or calculations
18
Q

What are compounding hints?

A
  • Prepare 10% overage to allow for loss
  • Mark disposable molds for fill level
  • Melt temperature is critical for plastic molds
  • Dampen bulky powders with liquid
  • Mix liquid ingredients w/ powders
19
Q

How do you determine the amount of base needed?

A
  • Dosage replacement factor method
  • Density factor
  • Occupied volume method

-If API < 100 mg then volume occupied is insignificant

20
Q

What is the equation for the dosage replacement method?

A

f=[[100(E-G)] / (G*X)] + 1

f = dosage replacement factor
E = weight of pure base suppository
G = weight of suppository w/ X% of the API
X% = percent of API in the suppository
1 = cocoa butter is arbitrarily assigned this value
21
Q

What is the equation of the density factor method?

A

DF = B / (A-C+B)

DF = density factor
A = avg weight of the blank
B = weight of API per suppository
C = avg weight of the medicated suppository
22
Q

Explain the occupied volume method.

A
  1. Determine the average weight per mold using the designated base
  2. Weigh out enough base for 10 suppositories
  3. Divide the density of the active drug by the density of the base to obtain a ratio
  4. Divide the total weight of the active drug required for the total number of suppositories by the ratio obtained in step 3
  5. Subtract the amount obtained in step 4 from the total weight of the prescription to obtain the weight of base required
  6. Multiply the weight of active drug per suppository times the number of suppositories to obtain the quantity of active drug required
23
Q

How should you package/label suppositories?

A

-Ointment Jars
-“Unwrap, moisten and insert…”
-“Moisten and insert…”
-“Insert…”
“Store in refrigerator”

24
Q

How do you store suppositories?

A
  • glass or plastic containers
  • wrapped or unwrapped
  • room temperature or under refrigeration
  • moderate humidity
25
Q

What is the stability of suppository?

A
  • 6 months if prepared from USP/NF ingredients
  • 25% of expiration period remaining if prepared from commercial products
  • Can be varied depending upon documentation
26
Q

What are important things about rectal suppositories?

A
  • Local and systemic effects
  • Many commercial examples
  • Patient counseling
  • Some suppositories can be divided into smaller doses.
27
Q

What are important things about urethral suppositories?

A
  • thinner and tapered ~5mm diameter and up to ~140 mm long
  • Local infections
  • Microsuppository for the treatment of ED
  • PEG vehicle will dissolve
28
Q

What are important things about urethral suppositories?

A
  • Local infections
  • Water-soluble bases most convenient
  • Oleaginous bases tend to “leak”
  • Progesterone compounded suppositories very widely used in hormone replacement therapy
  • Tablets

Pharmaceutics IV Test 2 (7 decks)

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