Chapter 12 Suppositories

Suppositories

Derived from the Latin term supponere, meaning to place

under.

SUB under ; PONERE to place

Are solid dosage forms intended for insertion into body orifices
where they melt, soften, or dissolved and exert localized or
systemic effects.
Suppositories

Shape

Dimensions

1.Rectal
Suppository

Long, cylindrical and have

one or both ends tapered.

Infant: 1 gram
Adult: 2 grams

2.Vaginal
Suppository
Pessaries

Globular, oviform, or conical

shaped.

About 3 to 5
grams

3. Urethral
Suppositories
Bougies

Slender, pencil-shaped
suppositories.

For males: 4 g,
100-150 mm long.
Females: 2 g, 60
to 70 mm.

Types of Suppositories
1. Rectally
2. Occasionally Urethrally
3. Nasal Insertion
4. Vaginally
5. Rarely aurally

Characteristics based on Administration

1. They have various weights and shapes, the shapes and size of a
suppository must be such that it is capable of being easily inserted
without causing any distension and once inserted must be
retained for the appropriate period of time.
2. Rectal Suppository are usually 32 mm (1 1/2 inches) in length, are
cylindrical, have one or both ends tapered.
3. The USP and NF states that the adult Rectal suppositories weigh
about 2 grams when cocoa butter (theobroma oil), as vehicle, is
employed as based.
Nasal Suppositories - Burginarium
with a glycerinated gelatin base.
Aural Suppositories (Ear Cones)
pencil-shaped suppositories similar in shape to urethral
suppositories but shorter in length, generally about 32 mm
long.
have been prepared with cocoa butter base
Advantages:
1. When a drug cannot be tolerated, cause to vomit orally
2. When a drugs cannot be swallowed - causing choking
3. When a drug may be decomposed or inactivated by the pH or
enzymes in the GIT
4. Rectal suppositories administered for its systemic effects but
containing drugs destroyed in the liver are better than oral
administration since rectal administration, liver is by passed.
Disadvantage - Inconvenient absorption is irregular and difficult to predict

Local Actions:
Once inserted, the suppository base melts, softens or dissolves, distributing
the medicaments it carries to the tissues of the region.
Rectal Suppositories: relieves constipation or pain irritation, itching and
inflammation associated with hemorrhoids or other anorectal conditions
(pinworms, dermatitis)
Vaginal suppositories: as antiseptic in feminine hygiene and as specific agents
to combat an invading pathogen. (vaginitis - by Trichomonas vaginalis and
Candida albicans)
Urethral Suppositories: as antibacterial and as a local anesthetic preparatory
to urethral examination
Systemic Actions:
For system effects, the mucous membranes of the rectum and vagina
permits absorption of many soluble drugs.
Rectal suppositories:
Aminophylline & Theophylline - relief of asthma
Prochlorperazine & Chlorpromazine - nausea & vomiting, & as
tranquilizer
Chloral hydrate -sedative and hypnotic
Oxymorphine HCl - narcotic analgesic
Belladonna & Opium - analgesia and antispasmodic effect
Ergotamine tartrate - migraine syndrome
Aspirin - analgesic and antipyretic
Factors Affecting Drug Absorption of Suppositories
Physiological Factors:
1. Colonic content - When systemic effects are desired from the
administration of a medicated suppository, greater absorption
may be expected from a rectum that is empty than one that is
distended w/ fecal matter because of more absorbing surface.
So when deemed desirable, an evacuate enema will be used first.
Other conditions: diarrhea, colonic obstruction due to tumors,
tissue dehydration can influence the rate and degree of
absorption
2. Circulation Route - drugs absorbed rectally, unlike those absorbed
orally, by pass the portal circulation during their first pass into the
general circulation, thereby enabling drugs otherwise destroyed
in the liver to exert systemic effect.
The lower hemorrhoidal veins surrounding the colon receive the
absorbed drug and initiate its circulation throughout the body, by
passing the liver.
3. pH and Lack of Buffering Capacity of the Rectal Glands
The rectal fluids are essentially neutral in pH and have no
effective buffer capacity so no chemical change will occur in this
area.
The suppository base has a marked influence in the release of
active constituents incorporated into it.
Cocoa butter melts rapidly at body temperature but immiscible
with body fluids and therefore fails to readily release fat-soluble
drugs.
For systemic drug action, it is preferable to incorporate the
ionized rather than the unionized form of a drug to maximize
bioavailability
4. Physiochemical Factors:
a.
Drug
i.
Relative solubility of the drug in lipid & in water
ii.
Particle size of a dispersed drug
1) Lipid-water solubility - a lipophilic drug that
is distributed in a fatty suppository base in

A. Uy | Page 1 of 5

low concentration has loss of a tendency to

escape to the surrounding aqueous fluids
than would a hydrophilic substance present
in fatty base to an extent approaching the
saturation.
Ex.: polyethylene glycols - which dissolve in
the anorectal fluids, release for absorption
both water-soluble and oil-soluble drugs.
2) Particle size - For drugs present in the
suppository in the undissolved state, the
size of the particle will influence the
amount release and dissolved in absorption.
The smaller the particle size, the more
readily the dissolution of the particle and
the greater the chance for rapid absorption
b. Suppository base
i.
Ability to melt, soften or dissolve at body temperature
ii.
Ability to release the drug substance
iii.
It is hydrophilic or hydrophobic character
1) Nature of the base: must be capable of
melting, softening, or dissolving to release
its drug components for absorption.
2) Undesirable Characteristics Of A Base
a) That which interact with the
drug inhibiting its release such
that the drug absorption will be
prevented or delayed.
b) That which is irritating to the
mucous membranes of the
rectum thus initiating a colonic
response and prompt a bowel
movement, negating the
prospect of thorough drug
release and absorption.
Classification Of Suppository Bases
1. Fatty or Oleaginous bases
a.
When a base is not specified, Cocoa Butter is used
b. Other oleaginous materials:
i.
Hydrogenated fatty acids of vegetable oils - palm,
kernel oil, and cotton seed oil
ii.
Fat bases compounds - glycerin with the higher
molecular weight fatty acids: palmitic and stearic
acids
iii.
Example of Suppositories with Cocoa Butter as a
Base
1) Cotmar
2) Dehydag
3) Wecobee
4) Witepsol
5) Fattybase
2. Water-soluble or water-miscible bases
a.
The main members of this group are based of
i.
Glycerinated gelatin
USP Preparation Of Glycerinated Gelatin
1) Weigh medicinal substance
2) Add water to make 10 grams
3) Dissolved or mix 20 mL of glycerin and
20 g of granular gelatin.
4) Heat on a steam bath until all gelatin
dissolved

5)

3.

Pour the melted mixture into molds &

allow to congeal.
ii.
Bases of polyethylene glycols
Polyethylene Glycol
1) polymers of ethylene oxide and water,
prepared to various chain lengths,
molecular weights, and physical
states. They are available in a number
of molecular weights ranges 200, 400,
600, 1000, 1500, 1540, 3350, 4000,
6000 & 8000.
2) Polyethylene glycols with average MW
of 200, 400, and 600 are clear,
colorless liquids. Those greater than
1000 are wax like, white solids with
hardness increasing with an increase
in molecular weight.
Ex.: Polybase
***Glycerinated gelatin based suppositories have
tendencies to absorb moisture due to the hygroscopic
nature of glycerin causing the following effect:
Ex.: Jell-O
May lose their shape and consistency
May lose dehydrating effect and be irritating to the tissues upon
insertion
Miscellaneous bases, (combination of lipophilic and hydrophilic)
a.
Mixture of oleaginous and water-soluble materials
Ex.: Polyoxyl 40 stearate (mixture of monostearate &
distearate esters of mixed polyethylene diols & the
free glycols)
b. Mixtures of many fatty acids (including Cocoa Butter)
with emulsifying agents capable of forming W/O
emulsion. Also referred to as hydrophilic suppository
base.
c.
A soap as a base like glycerin suppositories which have
sodium stearate; a soap as the base are included.

Preparations Of Suppositories
1. Molding from a melt/Fusion (Pour Molding)
2. Cold Compression (No heat Application)
3. Hand molding/rolling and shaping (No Heat Application)
4. Compression in a tablet press
*** The method most commonly employed in both small scale and industrial
scale is molding.
Preparation By Molding
1. Melting of the base preferably in water or steam bath to avoid
local overheating.
2. Incorporating the required medicament - either emulsified or
suspend in it.
3. Pouring the melt into cooled metal molds, which are usually
chrome or nickel plate.
4. Allowing the melt to cool and congeal thoroughly using
refrigerator in a small scale or refrigerated air on a larger scale.
5. Removing the formed suppositories from the mold.
Note: Suppositories of cocoa butter, glycerinated gelatin, polyethylene
glycol and most other suppository bases are suitable for preparation by
molding.

A. Uy | Page 2 of 5

Suppository Molds
Molds in common use are made from stainless steel, aluminum,
plastic. The molds which separate into sections generally
longitudinally, are opened for cleaning before and after preparing
a batch of suppository, closed when the melt is poured and
opened again to removed the cold, molded suppository.
Scratches in the molds should be avoided especially the plastic.
Lubrication Of The Molds
Depending upon the formulation, suppository molds may require
lubrication before the melt is poured to facilitate the clean and
easy removal of the molded suppository.
Lubricant is a thin coating of mineral oil or expressed almond oil
applied with the finger to the molding surface is sufficient.

Density factor: 1.1

Dosage: 0.5000 gram/suppository
Suppository base: Cocoa butter

Blank weight of suppository: 2.000 grams

Calculations:
0.5000/1.1 = 0.4545 g weight of cocoa butter which should be
replaced by 0.5 g of the drug
2.000 g - 0.4545 = 1.5455 g weight of cocoa butter required by
the suppository
0.5000 + 1.5455 = 2.0455 g actual weight of suppository

2.

Calibration Of The Molds

It is important the pharmacist calibrate each of his
suppository molds for the suppository bases that
he generally employs to have proper quantity of
medicaments.
a.
The suppositories are weighed and the total weight &
average weight of each suppository are recorded.
b. To determine the volume of the mold, the
suppositories are carefully melted in a calibrated
beaker.
c.
The volume of the melt is determine for the total
number as well as the average of one suppository.
Suppository Molds and Packaging
1. Aluminum metal molds

come in a variety of cavity sizes and with a variety of

number of cavities per mold

Common sizes vary from 1 g to 2.5 g, and common number

of cavities range from 6 cavities up to 100 cavities

The two halves of the mold are held together with either
nuts or some molds have 1 centered screw.
2. Plastic suppository shells

come in long strips that can be torn into any number of

cavities

These disposable molds do not need any lubrication

regardless of the suppository mixture

available in 1 g to 5 g sizes, and many different colors.

Advantage: if the suppository should melt, it will not run out

of the mold. If the material can congeals again, it will retain
the suppository shape.
3. Flexible rubber molds

can be packaged with the suppository still in the mold.

Generally the mold is placed in a special box.
Determination Of The Amount Of Base Required
1. First Method
o
Subtract the volume of the drug substance from the
total volume needed.
For example: If 12 mL of Cocoa butter are required to
fill a suppository mold and if the medicaments in the
formula have a collection volume of 2.8 mL the 9.2 mL
of Cocoa butter will be required. By mutiplying 9.2 mL
times the density of cocoa butter, 0.86 g/mL the
weight result is 7.9 g will required
Another example: For Cocoa butter suppositories
Active ingredient: Aminophylline

3.
4.
5.

6.
7.

Second Method
o
Requires the following steps:
a.
Weigh the active ingredient for the preparation
of a single suppository
b. Dissolve or mix it with a portion of melted base
insufficient to fill one cavity of the mold.
c.
Place the mixture to the mold
d. Add additional melted base to the cavity to
completely fill the mold.
e. Remove the suppository from mold and weigh
f.
Then subtract the weight of the ingredient from
the total weight of the suppository to get the
amount of the base needed.
g.
Then multiplied by the number of suppository
made to get the total base needed.
Preparation of ingredient:
Glycerin
Stearic acid
Sodium carbonate
Water
Preparing the mold
Base preparation
Mxing and pouring
Opening a suppository mold

The suppository mixture is poured into the cavities of a

closed mold. When the suppository mixture has
congealed, the excess mass is removed from the top
surface of the mold & the mold is separated into the
two halves.

An efficient way to separate the mold is to remove the

wing nuts or loosen the centered screw and place the
mold so that the posts rest on the table top.

Then, apply a downward pressure only on the bottom

half of the mold.

A knife or spatula should not be used to pry the two

halves apart. This will damage the matching mold faces
which have been accurately machined to give a tight
seal.

Suppository shells can be opened by peeling apart the

two tabs at the bottom of the shell.
Cooling and Finishing
Packaging

Suppository packaging
Strip ware

Strips (bars) with 10, 12, 20 or 24 individual cells

with or without punching

one side target printing

A. Uy | Page 3 of 5

white or transparency or one side white and one side

transparency foil
various opening methods like tear open slot, tear open strap, peel
off strap, short

Roll ware

with or without perforation between the cells

one or two side target printing

white or transparency or one side white and one side

transparency foil

various opening methods like tear open slot, tear open strap, peel
off strap "long", peel off strap "short"
Preparing and Pouring of the Melt
Using the least possible heat, the weighed suppository base material is
melted, generally over a water bath.
The medicinal substance are usually incorporated into portion of the melted
base by mixing on glass or porcelain tile with spatula, stir and allowed to cool
almost to its congealing point.
It is generally best to chill the mold in the refrigerator before pouring the
melt. Then, the melt is placed carefully and continuously in the filling of
each cavity in the mold.
The pouring must be continuous to prevent layering which may lead to a
product easily broken on handling.
When solidified the excess material is scraped off the top of the mold with
spatula. The mold is placed in the freezer to hasten hardening of the
suppository.
When suppositories are hard, the mold is removed from the freezer and
dislodged the suppositories from the mold.
Generally, little pressure is required to let fall the suppository of their mold.

2. Preparation By Compression
Suppositories may be prepared by forcing the mixed mass of the suppository
base and the medicament into special molds using suppository making
machines.
On a small scale, a mortar is heated in warm water before use and then
dried, the softening of the base and the mixing process are greatly facilitated
forming a paste-like consistency.
The compression process is especially suited for making suppositories which
contain substances that are heat labile and for suppositories containing a
great deal of substances insoluble in base.
The suppository mass is placed in the cylinder which is then closed, pressure
is applied from one end, by turning wheel and the mass is forced out of the
other end into the suppository mold or die. When the die is filled with the
mass, a movable end plate at the back of the die is removed and when
additional pressure is applied to the mass in the cylinder, the formed
suppositories are ejected.

Advantages of Compression:
1. The method is simple
2. The resulting suppository is more elegant than that of hand
molding
3. Avoid the possibilities of sedimentation of the insoluble solids in
the suppository base
Disadvantages:
1. Too slow for large scale operation
2. Air entrapment in molding fat type base suppositories. This
results in uncontrolled weight variation and favors the possible
oxidation of the base and active ingredients.
Preparation by hand rolling and shaping (no longer used today)
1. A plastic mass is formed from the base of grated Cocoa butter &
other ingredients.
2. Triturate in a mortar, then formed into a ball in the palms of the
hands, previously cooled in the ice water.

3.
4.

A broad bladed spatula or flat board is used to roll it into a

cylinder on a pile tile.
Cut with a spatula into sections and shaped as desired.

Compression In A Tablet Press

1. Carbon dioxide - releasing tablet - made up of dried sodium
biphosphate, sodium bicarbonate and starch. This compressed
rectal suppository is dipped or sprayed with a coating of water
soluble polyethylene glycol to add film for protection of the core
and for the aid in insertion into rectum.
2. Vaginal Compressed Tablet - in addition to the active ingredient, it
contains lactose and/or phosphoric acids for adjusting the acidity
of the vagina to an approximate pH 5.
Other Inserts (rectally, Vaginally, & Urethrally)
1. Tablets & capsules - Vaginal Tablets/Inserts
2. Ointments, Creams, & Aerosol Foams - ProtoFoam
3. Jellies & Gels
4. Contraceptive Sponge
5. Intrauterine Progesterone Drug Delivery System - Progestasert
6. Powders
7. Solutions - vaginal Douches
8. Enemas - Retention & Evacuation Enemas
9. Suspensions - Barium Sulfate Suspension
PACKAGING AND STORAGE
1. Glycerin Suppository tightly close glass container
2. Suppositories prepared with cocoa butter wrapped individually
3. Suppositories containing light sensitive individually wrapper
metallic foil
4. Commercially suppositories individually wrapped foil or plastic
5. Some packaged with continuous strips
6. Cocoa butter 300C
7. Glycerinated 200C to 250C
8. Polyethylene glycol room temperature
9. With humidity- absorbed moisture and tend to become spongy
10. With excessive dryness lose moisture and become brittle
ALPROSTADIL URETHRAL MICROSUPPOSITORY
MUSE
single use in male urethra
Medicated pellet measuring 1.4 mm in diameter by 3 mm or 6
mm long
Administered by inserting the applicator tip after urination
Available strength are 125, 250, 500, & 1000ug
For Erectile Dysfunction
Rectal Suppositories
Suppository
Bisacodyl
Chlorpromazine

Product
Dulcolax
Thorazine

Effect
local
systemic

Ergomine tartrate

Cafergot

systemic

Hydrocortisone

Anusol-HC

local

Indomethacin

Indocin

systemic

Prochlorperazine
Promethazine HCl

Compazine
Phenergan

systemic
systemic

Category
Cathartic
Anti-emetic,
tranquilizer
Adrenergic
blocking agents
Pruritis, Inflamed
Hemmarhoids
Antiinflammatory,
analgesic
Anti-emetic
Anti-histaminic,
antiemetic,
sedative

A. Uy | Page 4 of 5

Vaginal Suppositories

g.

Product
AVC suppositories

Active Constituents
Sulfanilamide, 1.05gm

Betadine medicated

Povidone-iodine, 10%

Gyne-Lotrimin

Clotrimazole, 100 mg

Monistat 7

Miconazole nitrate, 200g

Semicid vaginal
contraceptive insert

nonoxynol-9,100 mg

Sultrin vaginal tablet

Sulfathiazole, sulfacetamide
sulfabenzamide, 500 mg
Terconazole, 80 mg

Terazol 3

Category
Candida albicans
infections
relief of vaginitis due
to Candida albicans,
Trichomonas, and
Gardnerella vaginalis
Vulvovaginal yeast
(candida) infections
Antifungal for
vulvovaginal
candidiasis
(moniliasis)
Non-systemic
reversible method of
birth control
Haemophilus
vaginalis vaginitis
Antifungal for
vulvovaginal
candidiasis
(moniliasis)

h.

i.
2.

e.

f.

Other examples:

Miconazole 7

Clotrin-V

Encare (for birth control)

g.
h.
JELLIES
-

Examples of supp.:

Vaginal
a.
b.
c.
d.

Gently but firmly push the suppository into the rectum

until it passes the sphincter (about 1/2 to 1 inch in
infants, and 1 inch in adults.
Close your legs and sit (or lay) still for about 15
minutes. Avoid emptying bowels for at least one hour
(unless the suppository is a laxative). Avoid excessive
movement or exercise for at least one hour.
Wash hands again with soap and warm water
immediately after inserting the suppository.
Wash your hands carefully with soap and warm water.
Remove any foil or plastic wrapping from suppository.
Place suppository in applicator.
Hold the applicator by the opposite end from where
the suppository is.
Either lay on your back with your knees bent, or stand
with your feet spread a few inches apart and your
knees bent.
Gently insert the applicator into the vagina as far as it
will go comfortably. Once you are ready, push the
inside of the applicator in and place the suppository as
far back in the vagina as possible.
Remove the applicator for the vagina.
Wash your hands again with soap and warm water.

class of gels in which the structural coherent matrix contains a

high portion of liquid usually water
usually formed by adding a thickening agent: tragacanth or CMC
usually clear and uniform semisolid consistency
Example of Jellies

Lidocaine HCl Jelly

Cyclomethycaine Sulfate Jelly

Promoxine HCl Jelly local anesthetic

Ephedrine Sulfate Jelly - symphatomimetic

Anucort HC 25mg
Hemril-HC 25mg
Cotecxin supp.
Hemmorhoidal-HC 25mg

Administration
1. Rectal
a.
b.
c.
d.

e.

f.

If possible, go to the toilet and empty bowels.

Wash hands carefully with soap and warm water.
Remove any foil or plastic wrapping from the
suppository.
Lubricate the tapered end of the suppository with a
small amount of K-Y Jelly. If the jelly is not available,
moisten the suppository with a small amount of water.
Either stand with one leg on a chair, or lay on one side
with one leg straight and the other leg bent toward
your stomach.
Separate buttocks to expose the rectal area.

A. Uy | Page 5 of 5