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Sub
Under
Ponere
To place
3 Regions of the body are suppositories intended for
Rectal, Vaginal, Urethral
Which suppository can have systemic effects? Why?
Rectal
Middle hemorrhoidal veins can absorb the drug
3 Hemorrhoidal veins
Superior
Middle
Inferior
Swollen, painful rectal veins; often a result of constipation
Hemorrhoids
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)
Rectal suppository have _____ bases
Vaginal/urethral have _____ bases
Rectal → Oleaginous such as cocoa butter
(residues passes w stool)
Vaginal/urethral → Water soluble
Theobroma oil
Coca butter
Cocoa butter composition (Hint: POLLS)
POLLS
Palmitin
Olein
Laurin
Linolein
Stearin
and other long chain fatty acid glycerides
How to extract theobroma oil
Dissolve it in ether or chloroform and extract using separation
3 Limitations of cocoa butter in suppositories
Hydrophobic (unsuitable for vaginal/urethral)
Polymorphic (forms multiple crystals)
The melting point decreases after adding the drug
2 Examples of cocoa butter substitutes (synthetics)
Witepsol and Wecobee
(long chain fatty acids that are synthesized)
3 Types of water soluble bases used in suppositories
PEG, Glycerinated gelatin, Surfactant
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
PEG 4000 (2)
Water soluble suppository base
Takes long to soften so slower release
3 Methods to prepare suppositories
1. Hand rolling
2. Compression
3. Fusion (Molding)
Compression method for suppository formation
Mixes cocoa butter or peg with heat sensitive or insoluble drugs
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
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
Rank rectal, vaginal, and urethral suppositories from smallest to largest
Urethral (Smallest) < Rectal < Vaginal (Largest)
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)
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)
2 Advantages of suppositories
1. Avoids oral/ parenteral route (ex: oral surgeries)
2. Localized site of action (ex: hemorrhoids, infection)
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
How deep should a rectal suppository be inserted?
Past the anal sphincter
8 Common Medications in Suppositories
Analgesics
Local Anesthetics
Antipyretics
Antiemetics
Cathartics
Sedatives/Hypnotics
Antibiotics
Antifungals