SUPPOSITORIES

2C PHARMACY
GROUP 5
HERRELLA, HANNAH
ILAGAN, ISABELLE
INUMERABLE, MYZHEL
JAIN, NATASHA
KOBAYASHI, TACTTO
ETYMOLOGICAL
ORIGIN Derived from the Latin word
supponere - to place under

SUB under; PONERE to place
SUPPOSITORIES
Solid dosage forms
Intended for insertion into body orifices where
they
Melt
Soften
Dissolve
Exert localized or systemic effects by distributing
the medicaments it carries to the tissues of the
region
SUPPOSITORIES
Have various weights and shapes.
o capable of being easily inserted without
causing any distension.
o Once inserted, it must be retained for the
appropriate period of time.
ADVANTA
GES
1. Drugs are not destroyed or
inactivated by the pH or enzymatic
activity of the GIT
2. GI irritation is avoided
3. Bypass the liver
4. Convenient for administration of
drugs to patients who are unable
to swallow oral medications.
5. Effective route in treatment of
patients with severe nausea and
vomiting.
6. Ideal for post operative people
who cannot be administered oral
medication.
DISADVAN
TAGES 1. Inconvenient
2. Absorption is irregular and is
difficult to predict
TYPES OF
SUPPOSITORIES
RECTAL
VAGINAL
URETHRAL
APPEARANCE DIMENSIONS LOCAL ACTIONS
Long
Cylindrical
one or both ends
tapered
Shapes: bullet,
torpedo or little finger
Infant: 1 gram
Adult: 2 grams

Length: about 32 mm ( in.)
Relieves constipation
Relieves pain irritation,
itching and inflammation
associated with anorectal
conditions (hemmorhoids,
pinworms, dermatitis)
RECTAL
SUPPOSITORIES
PRODUCT GENERIC NAME USE EFFECT
Dilaucid Hydropmorphone Analgesic systemic
Compazine Prochlorperazine anti-emetic systemic
Phenergan Promethazine HCl anti-histaminic, anti-
emetic, sedative
systemic
Indocin Indomethacin anti-inflammatory,
analgesic
systemic
Thorazine Chlorpromazine anti-emetic,tranquilizer systemic
Anusol-HCl Hydrocortisone pruritis, inflamed
hemmorhoids
local
Dulcolax Bisacodyl cathartic local
APPEARANCE DIMENSIONS LOCAL ACTIONS
Globular, oviform, or
conical shaped
About 5 grams contraceptives
Antiseptic in feminine
hygiene
Specific agents to
combat an invading
pathogen
(Trichomonas
vaginalis and
Candida albicans)
VAGINAL SUPPOSITORIES
/ PESSARIES
APPEARANCE DIMENSIONS LOCAL ACTIONS
Slender
pencil-shaped
Males:
4 g, 100-150 mm long
3-6 mm in diameter
Females:
2 g
about 70 mm long
Antibacterial
Local anesthetic
preparatory to urethral
examination
URETHRAL
SUPPOSITORIES /
BOUGIES
FACTORS AFFECTING DRUG
ABSORPTION
A. PHYSIOLOGICAL FACTORS
1. Colonic content
When systemic effects are desired, greater absorption may
be expected from an empty rectum as the drug will be in
good contact with the absorbing surface of the rectum.
2. Circulation route
The lower hemorrhoidal veins surrounding the colon receive
the absorbed drug and initiate its circulation throughout the
body, bypassing the liver. Lymphatic circulation also assists in
the absorption.
3. pH and lack of buffering capacity of the rectal glands
it is preferred to incorporate the ionized salt form of the
drug to maximize bioavailability
B. PHYSIOCHEMICAL FACTORS
1. Lipid-water solubility
When drugs are highly soluble in the vehicle, release rate
into rectal fluid will be low
a hydrophobic drug in a fatty base has greater to be
released into the body fluid than a lipophilic drug that is
distributed in a fatty base (at low concentration)
2. Particle size
the smaller the particle size, the greater the surface area,
the more readily the dissolution of the particle, the greater
chance for rapid absorption
3. Nature of the base
if the base interacts with the drug to inhibit its release, drug
absorption will be impaired or prevented
If the base irritates the mucous membranes of the rectum,
it may prompt bowel movement.

PROPERTIES OF AN IDEAL
SUPPOSITORY BASE
Melts at body temperature or dissolves in body fluids.
Non-toxic and non-irritant
Compatible with any medicament
Releases any medicament readily
Easily moulded and removed from the mould
Stable to heating above the melting point
Easy to handle
Stable on storage
CLASSIFICATION OF
SUPPOSITORY BASES
I. FATTY OR OLEAGINOUS BASES
II. WATER SOLUBLE AND WATER MISCIBLE
BASES
1. GLYCERINATED GELATIN
2. POLYETHYLENE GLYCOL
III. MISCELLANEOUS BASES

1. FATTY OR OLEAGINOUS
BASES
Most frequently employed
Examples:
Theobroma oil (Cocoa butter)
Hydrogenated fatty acids of vegetable oils
Fatty based compounds containing glyceryl
monostearate and glyceryl monopalmitate
Commercial products:
Fattibase
Wecobee bases
Witepsol bases



Cocoa butter as a
suppository base

ADVANTA
GES
DISADVAN
TAGES
1. bland and nonsensitizing to membrane
tissues

2. readily available; can be hand rolled

3. solidification temperature is 12-13 below
its melting point (easy to pour before
hardens)

4. available grated or in bricks

1. must be kept in refrigerator or controlled
room temperature (because of the low
melting point)

2. has several polymorphic forms that have
even lower melting points (18, 24, and 28-
31C)

3. poor and erratic release of some
medications

GLYCERINATED GELATIN
o Most frequently used in vaginal suppositories
o softens slowly, slow drug release
o Hygroscopic
dehydrating effect
irritant
2. WATER-SOLUBLE OR
WATER-MISCIBLE BASES
POLYETHYLENE GLYCOL
o Polymers of ethylene oxide and water
o Available in number of molecular weight ranges
o 300, 400, and 600 (clear, colorless liquids)
o average (waxlike whitesolids)
o Do not melt a body temperature, dissolve slowly in
body fluids
o Slow release of medications
o Convenient storage
o Slow insertion
o Do not leak from orifice
o Do not irritate mucous membranes

3. MISCELLANEOUS
BASES
combination of oleaginous and water-
miscible materials
Hold water or aqueous solutions and are
said to be hydrophilic
Example:
Polyoxyl 40 stearate
- Surfactant
- Mixture of monostearate and distearate
esters of mixed polyethylene diols and free
glycols
- White to light tan waxy solid, water soluble

PREPARATIONS OF
SUPPOSITORIES
1. Molding from a melt most frequently use in both small
scale and industrial scale
STEPS IN MOLDING
a. Melting the base
b. Incorporating required medication
c. Pouring the melt into the mold
d. Cool and congeal
e. Remove the formed suppositories gently
2. Compression
3. Hand rolling and shaping

PLAY VIDEO: Extemporaneous preparation of a suppository
PACKAGING AND
STORAGE
Tightly closed glass containers
Slide boxes or plastic boxes
Strips ware/Roll ware

With humidity deliquescent,
becomes spongy
With excessive dryness loose
moisture, becomes brittle

Play Video: How to use suppository
Glycerinated gelatin suppository
20-25C
Suppositories prepared with cocoa
butter
wrapped individually, 30C
Suppositories containing light
sensitive
individually wrapped in opaque
materials such as metallic foil
Commercial suppositories
individually wrapped in foil or
plastic
PEG suppositories
room temperature
FIN