Suppositories + Inserts Flashcards
What is a suppository?
Solid dosage form inserted into body orifices where they melt, soften, or dissolve at body temperature
Supossitories delivery is ______ dependent
formulation
Rectal suppositories are generally used for ______ delivery
systemic
Rectal suppositores are generally used to treat _____ anorectal diseases
local
What are the disadvantages of rectal suppositories?
- Violates patient’s dignity
- Local irritation
- Available in limited strengths
What are the advantages of rectal administration over oral?
- Administration is simple
- Avoids hepatic first pass elimination
- Drugs stability (avoids degradation in GI)
- Avoids unpleasant taste
- Kids + ppl unable to use PO meds can get it
What are some limitations of rectal administration?
- Pt acceptablity/compliance is poor especially for chronic therapy
- Limited commercial doses available
- Variable effectiveness
- Suppository may be rejected/ascend post insertion
Weight of rectal suppositories dependent upon ____ of the drug + base (mainly)
density
Vaginal suppositories are also known as….?
Pessaries
What are the advantages of vaginal administration of RX?
- Local + systemic delivery
- Large surface area
- Avoids hepatic first pass + GI degradation
- Self administration/removal is often an option
What are some limitations of vaginal administration?
- Route is gender specific
- Menstrual cycle/hormonal variations
- Physiological pH may enhance or affect dissolution and absorption of drugs
Urethral suppositories are also known as…?
Bougies
Systemic absorption is more commonly seen with _____ rather than vagina delivery
rectal
What are some formulation variables?
- Form of active
- Solubility
- Viscosity
- Brittleness
- Volume contraction
Generally, drug form will (be/not be) altered by rectal environment
not be
Rectal fluid is generally in pH range of 7.2-7.4 w/ _______ buffer capacity
negligible
Greater absorption is expected with a/an _____ colon
empty
What is brittleness caused by?
- High solid concentration
2. Shock cooling
Lipophilic drugs in fatty base have a (higher/lower) tendency to be released to the surround aqueous fluids than a ______ drug in a fatty base
lower + hydrophilic
Suppository base should remain ____ at room temperature
solid
What is the most commonly used fatty (oleaginous) base?
Cocoa butter
What is the most important characteristic of fatty (oleaginous) base?
Melts quickly at body temperature
How is cocoa butter harvested?
Seed of Theobroma cacao
What are some advantages of fatty (oleaginous) bases?
- Softens at 30 degrees C
- Generally non-irritating
- Acts as an emollient
What are some disadvantages of fatty (oleaginous) bases?
- Poor/eratic release of some drugs
- Exhibits polymorphism (in cocoa butter)
- May leak
Water-soluble bases ______ and mixes w/ aqueous body fluids
dissolves
Water-soluble bases may cause some _____ due to uptake of water and cause a slight ______ of the mucosa
irritation + dehyrdation
What is the most popular water-soluble base?
PEGS
What is an advantage of PEG?
- Mix and match MW bases to attain specific MP
What is a disadvantage of PEG?
- Drug incompatibilities
2. Cause irritation
Glycerinated gelatin suppositories (are/are not) recommended for rectal use but is more useful as a/an _____ insert
are not + vaginal
What is wrong with using glycerinated gelatin suppositories?
- Osmotic effect
2. Defecation reflex
Glycerinated gelatin bases provides (faster/slower) release and has a tendency to (absorb/repel) mositure
slower + absorb
What should you protect glycerinated gelatin bases from?
Atmospheric mositure
PEG suppositories (do/do not) melt at body temperature
do not
PEG suppositories contribute to ______ release of drugs
prolonged
PEG mixes w/ mucous upon dissolving and as a result it has ____ leakage compared to fatty bases
less
Slow release; poor escaping tendency
A. Oil-soluble drug + base
B. Water-soluble drug + fatty base
C. Oil-soluble drug + water base
D. Water-soluble drug + base
A. Oil-soluble drug + base
Moderate release
A. Oil-soluble drug + base
B. Water-soluble drug + fatty base
C. Oil-soluble drug + water base
D. Water-soluble drug + base
C. Oil-soluble drug + water base
Moderate release; based upon diffusion; all water soluble
A. Oil-soluble drug + base
B. Water-soluble drug + fatty base
C. Oil-soluble drug + water base
D. Water-soluble drug + base
D. Water-soluble drug + base
Rapid release
A. Oil-soluble drug + base
B. Water-soluble drug + fatty base
C. Oil-soluble drug + water base
D. Water-soluble drug + base
B. Water-soluble drug + fatty base
What are the methods of suppository prep?
- Molding from a melt (most common)
2. Hand rolling/shaping
Suppository drug must be released within _____
6 hours
To ensure max drug release, apply principle of _____ ______
opposite characteristics
Release of drug and onset of drug action depends upon three factors…what are they?
- Liquefaction of base
- Dissolution of active
- Drug diffusion thru tissues