SUPPOSITORIES

Dr.M.M.Gupta
B.Pharm., M.Pharm., MBA, Ph.D., FICS, FIAPST, FABSc, Pg CUTL
Senior Lecturer ( Pharmaceutics)
School of Pharmacy, Faculty of Medical Sciences
The University of the West Indies, Trinidad, WI

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 CONTENTS

Definition
Merits and Demerits
Limitations
Types
Suppository bases
Preparation
Calibration and Displacement value
Packaging
Evaluation

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Definition:
Solid or stiffened semi-solid dosage form for insertion into
body cavities other than mouth

Types
1. Rectal
2. Vaginal (Pessaries)
3. Urethral bougies
4. Ear (ear cones)
5. Nasal bougies

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MERITS:

Local effects

Systemic effects

By pass first pass metabolism

Alternative route for unconscious, elderly patients

Unpleasant drugs

Avoids gastric irritation & GI instability

Prolonged drug release

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DEMERITS

The problem of patient acceptability or Aesthetic objection

Suppositories are not suitable for patients suffering from

diarrhoea

Incomplete/ unpredictable absorption may be obtained

because suppository usually promotes evacuation of the
bowel

Leakage

Mucosal damage

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 TYPES OF SUPPOSITORIES
RECTAL SUPPOSITORIES:
Introduction into the rectum for their systemic and local
effect
Generally made from theobroma oil
Usually available in weight about 1-2 g

VAGINAL SUPPOSITORIES (PESSARIES)

Introduction into vagina
Larger than rectal suppositories
Conical, rod shaped
Available in 4-8 g
Mainly used for local action

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TYPES OF SUPPOSITORIES: Cont
NASAL SUPPOSITORIES ( Nasal Bougies)
Introduction into the nasal cavity
Thin and cylindrical
Prepared by glycero-gelatin base
These are about 9-10 cm long and weight about 1g

URETHRAL SUPPOSITORIES (Urethral Bougies)

Introduction into urethra
Thin, long and cylindrical
Weight 2-4 g

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TYPES OF SUPPOSITORIES: Cont
EAR CONES
Introduction into ear
Also known as Aurinaria
These are thin, long and cylindrical in shape
Weight about 1 g
Usually prepared with Theobroma oil

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FORMULATION OF SUPPOSITORIES
Drug ( API)

Base
Other additives – Surfactants, Soothing agents,
Antioxidants, Preservatives, Anti-settling agents
(blend of higher M.P waxes & fatty acids )

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 SUPPOSITORY BASE
IDEAL SUPPOSITORY BASE:

Melts at body temperature or dissolves in body fluids.

Non-toxic and non-irritant.
Compatible with any medicament.
Releases medicament readily.
Easily mouldable and removed from the mould.
Stable to heating above the melting point.
Easy to handle.
Stable on storage.

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 CLASSIFICATION OF SUPPOSITORY BASE

Oleaginous (Fatty) bases

a) Natural - Theobroma oils (cocoa butter) or their substitutes
b) Synthetic (Emulsified) - Witepsol, Massuppol, Massa
estarinum

Hydrophilic (water soluble/miscible) bases

a) Natural - Glycero- gelatin, soap-glycerin
b) Synthetic - Macrogols

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 NATURAL - COCOA BUTTER
Also know as Theobroma oil
It is a yellowish-white solid with an odour of chocolate and is a
mixture of glyceryl esters of different unsaturated fatty acids.

ADVANTAGES:
A melting range of 30 - 35°C (solid at room temperature but
melts in the body).
Readily melted on warming, rapid setting on cooling.
Miscible with many ingredients.
Non-irritating.

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COCOA BUTTER: Disadvantages
POLYMORPHISM:
When melted and cooled it solidifies in different crystalline
forms
If melted at not more than 36°C and slowly cooled it forms
stable beta crystals with normal melting point.
If over-heated then cooled it, produces unstable gamma
crystals which melt at about 15°C or alpha crystals melting
at 20°C.

ADHERENCE TO THE MOULD: Tendency to stick to the sides

of the mould when solidified

RANCIDITY ON STORAGE

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COCOA BUTTER: Disadvantages
Melting point reduced by soluble ingredients
Phenol and chloral hydrate have a tendency to lower the
melting point of cocoa butter.- So, solidifying agents like
beeswax (4%) may be incorporated to compensate for the
softening effect of the added substance.

Immiscible with body fluids

Leakage from the body cavities on melting

Expensive

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 COCOA BUTTER SUBSTITUTES
EMULSIFIED THEOBROMA OIL
Used, when large quantity of aqueous solutions are to be
incorporated
The use of 5% glyceryl monostearate, 10% lenette wax, 2-
3% cetyl alcohol, 4% beeswax and 12% spermaceti
prepare emulsified theobroma oil

HYDROGENATED OILS
Obtained by hydrogenation of vegetable oils

ADVANTAGES
Resistant to oxidation
Lubrication of mould is not required
Overheating does not affect the solidifying point
Good water absorbing capacity
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 Oleaginous bases: synthetic
WITEPSOL
Triglycerides of saturated vegetable acids
Small amount of beeswax added for use in hot climate
Prepared suppositories should not be cooled rapidly otherwise
chances of brittleness and fracture

Massa estarinum
Mixture of mono, di and triglycerides of saturated fatty acids
Also known as “ adeps solidus” and having M.P. 33.5 to 35.50 C

MASSUPOL
Glyceryl esters, mainly of lauric acid
Small amount of glyceryl monostearate added to improve
water absorbing capacity

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Oleaginous bases (synthetic): Advantages
Solidifying points are unaffected by overheating

Good resistance to oxidation

Difference between melting and setting points is small so set

quickly, the risk of sedimentation of suspended ingredients is
low.

They are marketed in a series of grades with different melting

point ranges, which can be chosen to suit particular products
and climatic condition.

They contain a proportion of w/o emulsifying agents, and

therefore, their water-absorbing capacities are good.

No mould lubricant is necessary because they contract

significantly on cooling.
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Oleaginous bases (synthetic): Disdvantages

Brittle if cooled rapidly, avoid refrigeration during preparation.

The melted fats are less viscous than theobroma oil. As a

result greater risk of drug particles to sediment during
preparation, lack of uniform drug distribution give localized
irritancy.

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 Water-soluble and water-miscible bases:
Glycero-gelatin base

The commonest is Glycerol Suppositories Base B.P., which

has 14% w/w gelatin, and 70% w/w glycerol & water Q.S. to
100%.
The glycerol-gelatin base U.S.P. consisted of 20% w/w gelatin,
and 70% w/w glycerol & water Q.S. to 100%.

Gelatin is used to provide stiffness

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Glycero-gelatin base …………..
Produces translucent suppositories which tend to dissolve or
disperse slowly in the body cavities

Preferred base over fatty base

Well suited for boric acid, chloral hydrate, bromide, iodides,

iodoform.
Particularly used for making pessaries

To avoid incompatible reactions two types of gelatin are used as

suppository base
Type A ( Phamagel A)- Acidic
Type B ( Phamagel B)- Alkaline

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Glycero-gelatin base: Disadvantages

The solution time depends on the contents and quality of

gelatin used.
Gelatin is incompatible with many drugs such as tannic acid,
ferric chloride, gallic acid etc
More chances of bacterial and mould growth so preservative
is required.
Hygroscopic so require special storage condition
Have a physiological action ( glycerol-suppository BP is used a
Laxative)

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 Soap-glycerin
In glycero-gelatin base, the gelatin is replaced with either curd
soap or sodium stearate which makes the base sufficiently
hard

Soap also helps in the evacuation action of glycerin.

The main disadvantage of this base is that they are very

hygroscopic

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 MACROGOLS (polyethylene glycols):
PEGs are polymers of ethylene oxide and water, prepared to
various chain lengths, molecular weights, and physical states.

Also known as carbowaxes or polyglycols

PEGs 300,400 & 600 are clear and colourless while those with
molecular weights of 800-1000 are semisolids and molecular
weights of greater than 1000 are wax-like, white solids with the
hardness increasing with an increase in the molecular weight.

These polyethylene glycols can be blended together to

produce suppository bases with varying: melting points,
dissolution rates and physical characteristics.

The melting point is often around 50°C.

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 ADVATAGES OF MACROGOLS

Chemically stable and non-irritant

Do not allow the bacterial or mould growth
Physiological inert
Physical properties changed according to the need by
combining the different proportion of high and low M.P.
polymers.
Provide prolong action because do not melt in the body cavity
but dissolve slowly for a long time.
Do not stick to the side of the mould.
Suppositories are clean and smooth in appearance

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 DISADVATAGES OF MACROGOLS

Hygroscopic

Incompatible with tannins, phenols etc.

High solubility of macrogols leads to supersaturation which

turn make crystals and fracture in the product on storage.

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 PREPARATION OF SUPPOSITORIES

METHODS ARE-

Hand Moulding or Rolling method

Cold Compression Method

Hot process or Fusion Method

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 HAND MOLDING

Ancient method of preparing suppositories

The drug is made into a fine powder.

It is incorporated into the suppository base by kneading

with it or by triturating in a mortar.

The kneaded mass is rolled between fingers into rod

shaped units.

The rods are cut into pieces and then one end is pointed.

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 COLD COMPRESSION METHOD
Useful for thermo-labile and insoluble drugs.
Cocoa butter is grated: The ingredients are mixed with an equal
amount of grated cocoa butter and added remaining amount
afterwards.
Compression of the prepared mass is done on hand or power
operated compression machine
ADVANTAGES:
It is a simple method.
It gives suppositories that are more elegant than hand moulded
suppositories.
Suitable for heat labile medicaments.
DISADVANTAGES:
Air entrapment may take place which may cause weight variation.
The drug and/or the base may be oxidized by this air.

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 HOT OR FUSION METHOD

Using a suppository mould which is made of metal or plastic.

Traditional metal moulds are in two halves which are clamped
together with a screw.

STEPS:
The base is melted and precautions are taken not to overheat
it.
The drug is incorporated in it.
The molten liquid mass is poured into chilled (lubricated if
cocoa butter or glycrogelatin is the base)molds.
After solidification the cone shaped suppositories prepared

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 LUBRICANTION OF SUPPOSITORY MOULDS

Lubricating the cavities of the mould is helpful in producing

elegant suppositories and free from surface depression.

- The lubricant must be different in nature from the suppository

base, otherwise it will be absorbed and fail to provide a buffer
film between the mass & the metal.

- The water soluble lubricant is useful for fatty bases while the
oily lubricant is useful for water soluble bases.

- The lubricant should be applied on a gauze or with fairly stiff

brush.

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 LUBRICANTS FOR SUPPOSITORY
BASES

Name of base Lubricant used

Cocoa Butter Softsoap (10g)+ glycerin(10g)+ Alcohol (50ml)

Glycero-gelatin Liquid Paraffin or Arachis Oil

Synthetic No Lubricant is required

( Witepsol)

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 CALIBRATION OF THE MOULD
Generally a standard mould of one gram capacity is used.

The size of suppository from particular mould remains same

but the weight varies due to density of different bases and
medicaments are different as weight of moulds are based on
particular base.

So mould should be calibrated for individual base and

medicaments and this is done by preparing a set of
suppositories using the base, weighing the suppositories and
then find the average mean which will indicate the true
capacity of the mould

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 DISPLACEMENT VALUE
The volume of a suppository from a particular mould is uniform
but its weight will vary because the densities of the
medicaments usually differ from the density of the base with
which the mould was calibrated.

To prepare the suppositories of uniform and accurate weight

displacement should be calculated

So displacement value is defined as” The quantity of the drug

which displaces one part of the base”

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 Calculation of displacement value
Prepare and Weigh of 6 suppositories ( Containing CB or other base)
= A gm
Prepare and Weigh of 6 suppositories ( containing 40% medicament)
= B gm
Calculate the amount of CB present in Medicated Suppositories
= 60/100×B= C gm

Calculate the amount of medicament present in the medicated supp.

=40/100×B= D gm
Calculate the amount of CB displaced by D gm of medicament
= (A-C) gm

DISPLACEMENT VALUE = D /A-C

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Calculate the displacement value of Zinc Oxide in Cocoa Butter
suppositories containing 40% of Zinc Oxide and is prepared in a 1 gm
mould . The weight of 8 Suppositories is 11.74 gm
Weigh of 8 suppositories ( Containing CB ) = 1×8= 8 g (A)

Weigh of 8 suppositories ( containing 40% medicament) = 11.74 g (B)

Amount of CB present in 8 Suppositories = 60/100×11.74= 7.044 g ( C)

Amount of medicament present in the 8 supp. =40/100×11.74= 4.696 g (D)

Amount of CB displaced by D gm of medicament = (A-C) gm

So Displacement value = D /A-C = 4.696/ (8-7.044)= 4.912 = Appox 5

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 PACKAGING AND STORAGE

Suppositories are usually packed in Tin or Aluminium, paper or

plastic.

Poorly packed suppositories may give rise to staining,

breakage or deformation by melting.

Both cocoa butter and glycerinated gelatin suppositories

stored preferably in a refrigerator.

Polyethylene glycol suppositories stored at usual room

temperature without the requirement of refrigeration.

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 EVALUATION:

Weight variation Test

Breaking Test

Melting temperature Test

Dissolution test

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 WEIGHT VARIATION TEST
Weigh 20 suppositories individually. w1, w2, w3….w20
Weigh all the suppositories together = W.
Calculate the average weight = W/20.

LIMIT: not more than 2 suppositories differ from the average

weight by more than 5%, and no suppository differs from the
average weight by more than 10%.

Upper limit = average weight + (5×Avg Weight/100)

Lower limit = average weight - (5×Avg Weight/100)

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HARDNESS TEST(Breaking Test)

The suppository is placed in the instrument.

Add 600 g; leave it for one min. (use a stop

watch).

If not broken, add 200 g every one min. until

the suppository is broken.

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 MELTING RANGE TEST
This test is also called the Macromelting range test and is a
measure of the time for the entire suppository to melt when
immersed in a constant-temperature (37oC) water bath.

The apparatus commonly used for measuring the melting

range of the entire suppository is the USP Tablet
Disintegration Apparatus.

PROCEDURE:
The suppository is completely immersed in the constant
temperature water bath, and the time for the entire suppository
to melt or disperse in the surrounding water is measured.

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 DISSOLUTION TEST

Dissolution testing methods include the-

Paddle method

Basket method

Membrane diffusion method/dialysis method

Continuous flow/Bead method

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 SUPPOSITORIES

THANK
YOU
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