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

UPPOSITORIES

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

For systemic effects, the mucous membrane of he

rectum and vagina permit the absorption of many
soluble drugs

SUPPOSITORIES

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. 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

PREPARATION OF SUPPOSITORIES
MOLDING
COMPRESSION

HAND

ROLLING

MOLDING

Steps:

1.

Melting the base

2.

Incorporating required medicaments

3.

Pouring into molds

4.

Allowing to cool and congeal

5.

Removing from mold

- Cocoa Butter, Glycerinated gelatin, Polyethylene Glycol

MOLDING

- Molds are commonly made out of Stainless steel, Aluminum, Brass or

Plastic

Lubrication of Mold

Seldom necessary for bases such as Coca butter and Polyethylene Glycol

For Glycerinated gelatin, thin layer of mineral oil is necessary

No material irritating to mucous membrane should be used as mold

lubricant

Calibration of the Mold

1.

Preparation of molded suppositories from base alone

2.

After removal from mold, weighed and the total weight

and average for each is recorded

For volume:
1.

Carefully melted in a calibrated beaker

2.

Volume of melt is determined for total number and

average for each suppository

Determination of the amount of base

required
Total volume of mold Volume of drug substance = Volume of base
required

Because bases are solid at room temperature, volume of base may be

converted to weight from the density of material

Determination of the amount of base

required
1.

Weigh the active ingredient for a single suppository

2.

Dissolve with a portion of melted base insufficient to fill one cavity

of mold

3.

Add additional melted base to the cavity to fill it completely

4.

Allow to congeal and harden

5.

Remove from mold and weigh

Weight of suppository Weight of active ingredients = Weight of base x

Number of suppository required

Determination of the amount of base

required
1.

Place all required medicaments for the total number of suppositories

(including one extra) in a calibrated beaker

2.

Add a portion of melted and incorporate drug substance

3.

Add sufficient melted base to reach the required volume of mixture

on the original calibration of the volume of mold

Preparing and pouring the mold

Water bath is used because it requires the least possible heat

Porcelain casserole is the best utensil because it permits convenient

pouring

Small amount of silica gel (25 mg) can be incorporated into the
formula to aid in keeping the active drug suspended

Continuous pouring to prevent layering which may lead to a product

easily broken on handling

Poured excessively over each opening

Preparation by compression

Base and other ingredients are combined by thorough mixing , friction

of the process softening the base into a paste-like consistency

On small scale, using a heated mortar (to facilitate softening of the

base and mixing) and pestle

On large scale, using mechanical kneading mixers and warm mixing

vessel

Preparation by compression

Suited for heat-labile medicinal substances or a great deal of

substances that are insoluble in the base

Permits no likelihood of insoluble matter settling during manufacture

DISADVANTAGE

Special suppository machine is required

Limited suppository shapes are produced

Preparation by Compression
1.

Suppository mass is placed in cylinder and closed

2.

Mechanical pressure application or by turning a wheel

3.

Mass is forced out of the other end into the mold

4.

When filled with mass, movable end plate at the back of the die is
removed

5.

And when additional pressure is applied to the mass in the cylinder,

formed suppositories are ejected

Suppositories with uniform circumference may be produced by

extrusion through a perforated plate and cutting the extruded mass to
the desired length

Preparation by Compression

Preparation by Hand Rolling and Shaping

Oldest and simplest method of preparation of suppository

Requires a considerable skill in hand rolling

Uses cocoa butter as base

Has the advantage of avoiding the necessity to heat the

cocoa butter

TYPES OF
SUPPOSITORIES
RECTAL
VAGINAL

URETHRAL

RECTAL
SUPPOSITORIES

APPEARANCE

DIMENSIONS

Long
Infant: 1 gram
Cylindrical
Adult: 2 grams
one or both ends
tapered
Length: about 32 mm ( in.)
Shapes: bullet,
torpedo or little finger

LOCAL ACTIONS

Relieves constipation
Relieves pain irritation,
itching and inflammation
associated with anorectal
conditions (hemmorhoids,
pinworms, dermatitis)

PRODUCT

GENERIC NAME

USE

EFFECT

Dilaucid

Hydropmorphone

Analgesic

systemic

Compazine

Prochlorperazine

anti-emetic

systemic

Phenergan

Promethazine HCl

anti-histaminic, antiemetic, 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

VAGINAL SUPPOSITORIES
/ PESSARIES
APPEARANCE

Globular, oviform, or
conical shaped

DIMENSIONS

About 5 grams

LOCAL ACTIONS

contraceptives
Antiseptic in feminine
hygiene

Specific agents to
combat an invading
pathogen
(Trichomonas
vaginalis and
Candida albicans)

URETHRAL
SUPPOSITORIES
/
APPEARANCE
DIMENSIONS
LOCAL ACTIONS
BOUGIES

Slender
pencil-shaped

Males:
4 g, 100-150 mm long
3-6 mm in diameter
Females:
2g
about 70 mm long

Antibacterial
Local anesthetic
preparatory to urethral
examination

FACTORS AFFECTING DRUG

ABSORPTION
A. PHYSIOLOGICAL FACTORS
1.

Colonic content

2.

Circulation route

3.

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.
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.

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
Melts at body temperatureBASE
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
FATTY OR OLEAGINOUS BASES
SUPPOSITORY
BASES
II. WATER SOLUBLE AND WATER MISCIBLE
I.

BASES

III.

1.

GLYCERINATED GELATIN

2.

POLYETHYLENE GLYCOL

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

Cocoa butter as a
suppository base

ADVANTA DISADVAN
TAGES
GES

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 2831C)
3. poor and erratic release of some
medications

2. WATER-SOLUBLE OR
GLYCERINATED GELATIN
WATER-MISCIBLE
BASES
o

Most frequently used in vaginal suppositories

softens slowly, slow drug release

Hygroscopic

dehydrating effect

irritant

POLYETHYLENE GLYCOL
o

Polymers of ethylene oxide and water

Available in number of molecular weight ranges

300, 400, and 600 (clear, colorless liquids)

average (waxlike whitesolids)

Do not melt a body temperature, dissolve slowly in

body fluids
o

Slow release of medications

Convenient storage

Slow insertion

Do not leak from orifice

Do not irritate mucous membranes

3. MISCELLANEOUS
BASES

combination of oleaginous and watermiscible 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

PACKAGING AND
STORAGE Tightly closed glass containers

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

Slide boxes or plastic boxes

Strips ware/Roll ware

With humidity deliquescent,

becomes spongy

With excessive dryness loose

moisture, becomes brittle

FIN