PSC 4215 - Exam 1 - Suppositories

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27 Terms

1

Sub

Under

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2

Ponere

To place

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3

3 Regions of the body are suppositories intended for

Rectal, Vaginal, Urethral

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4

Which suppository can have systemic effects? Why?

  • Rectal

  • Middle hemorrhoidal veins can absorb the drug

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3 Hemorrhoidal veins

  1. Superior

  2. Middle

  3. Inferior

<ol><li><p>Superior </p></li><li><p>Middle </p></li><li><p>Inferior </p></li></ol><p></p>
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<p>Swollen, painful rectal veins; often a result of constipation</p>

Swollen, painful rectal veins; often a result of constipation

Hemorrhoids

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Characteristic of an ideal suppository base

Oleaginous or water soluble base that can melt at 37C or 98.6F and not leak out

(Others: Firm enough to insert at room temperature, Stable during manufacture & storage, Chemically compatible with drug, Non irritating)

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8
  1. Rectal suppository have _____ bases

  2. Vaginal/urethral have _____ bases

  • Rectal → Oleaginous such as cocoa butter

    (residues passes w stool)

  • Vaginal/urethral → Water soluble

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Theobroma oil

Coca butter

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Cocoa butter composition (Hint: POLLS)

POLLS

  • Palmitin

  • Olein

  • Laurin

  • Linolein

  • Stearin

and other long chain fatty acid glycerides

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How to extract theobroma oil

Dissolve it in ether or chloroform and extract using separation

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3 Limitations of cocoa butter in suppositories

  • Hydrophobic (unsuitable for vaginal/urethral)

  • Polymorphic (forms multiple crystals)

  • The melting point decreases after adding the drug

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2 Examples of cocoa butter substitutes (synthetics)

Witepsol and Wecobee

(long chain fatty acids that are synthesized)

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3 Types of water soluble bases used in suppositories

PEG, Glycerinated gelatin, Surfactant

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T/F: Water-soluble bases, such as polyethylene glycol (PEG)-based suppositories, tend to soften more slowly compared to fatty or oleaginous bases (like cocoa butter). This results in a slower drug release

T

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PEG 4000 (2)

  • Water soluble suppository base

  • Takes long to soften so slower release

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3 Methods to prepare suppositories

1. Hand rolling

2. Compression

3. Fusion (Molding)

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Compression method for suppository formation

Mixes cocoa butter or peg with heat sensitive or insoluble drugs

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Fusion/molding method for suppository formation

Melts cocoa butter, PEG, or glycerinated gelatin with drugs that ARE NOT heat sensitive. Insoluble powders must be finely dispersed

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Factors to consider when choosing suppository bases

SCAR

1. Solubility of drug in bases

2. Compatibility of drug in base

3. Application site (no cocoa butter for vaginal/urethra)

4. Rate of drug release/ absorption

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21

Rank rectal, vaginal, and urethral suppositories from smallest to largest

Urethral (Smallest) < Rectal < Vaginal (Largest)

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Compressed tablets, soft gelatin capsules, and urethral inserts may be used as suppositories but may cause

Irritation and inflammation

(not recommended unless theres a need)

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What could cause a fail in treatment of a urethral insert or rectal insert

Urinating or defecating less than 1 hour after insertion (not enough time to release/will not be in therapeutic range)

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2 Advantages of suppositories

1. Avoids oral/ parenteral route (ex: oral surgeries)

2. Localized site of action (ex: hemorrhoids, infection)

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4 disadvantages of suppositories

1. Inconvenience (ex: melt, deep)

2. Unpredictable absorption (ex: did it dissolve/ reach circulation? covered by mucus/ feces?)

3. Mucosal irritation

4. High cost

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How deep should a rectal suppository be inserted?

Past the anal sphincter

<p>Past the anal sphincter</p>
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8 Common Medications in Suppositories

  1. Analgesics

  2. Local Anesthetics

  3. Antipyretics

  4. Antiemetics

  5. Cathartics

  6. Sedatives/Hypnotics

  7. Antibiotics

  8. Antifungals

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