Suppositories are solid dosage forms

intended for insertion into body

orifices where they melt, soften, or
dissolve and exert localized or
systemic effects.
● Dosage form characteristics:
a. Rectal suppositories for adults weigh 2 gm and are
torpedo shape.
● Children's suppositories weigh about 1 gm.

b. Vaginal suppositories or Pessaries weigh about 3- 5gm and

are molded in globular or oviform shape or compressed on a
tablet press into conical shapes.
c. Urethral suppositories called bougies are pencil shape.
Those intended for males weigh 4 gm each and are
100-150 mm long.
● those for females are 2 gm each and 60-75 mm in
length.

d. Nasal suppositories: called nasal bougies or buginaria

meant for introduction in to nasal cavity.
● They are prepared with glycerogelatin base.
● They weigh about 1 gm and length 9-10 cm.
e. Ear cones:
● Aurinaria and meant for introduction into ear.
● Rarely used
● Theobroma oil is used as base.
● Prepared in urethral bougies mould and cut
according to size.
ADVANTAGES:
_ Can exert local effect on rectal mucosa.
_ Used to promote evacuation of bowel.
_ Avoid any gastrointestinal irritation.
_ Can be used in unconscious patients (e.g. during fitting).
_ Can be used for systemic absorption of drugs and avoid first-
pass metabolism.
– Babies or old people who cannot swallow oral
medication.
– Post operative people who cannot be administered oral
medication.
– People suffering from severe nausea or vomiting.
● DISADVANTAGES OF SUPPOSITORIES:
– The problem of patient acceptability.
– Suppositories are not suitable for patients suffering from
diarrhea.
– In some cases the total amount of the drug must be
given will be either too irritating or in greater amount than
reasonably can be placed into suppository.
– Incomplete absorption may be obtained because
suppository usually promotes evacuation of the bowel.
SUPPOSITORIES:
British Pharmacopoeia (BP) definition:
“Suppositories are solid, single-dose
preparations. The shape, volume and
consistency of suppositories are suitable
for rectal administration.”
 Pessaries

● Pessaries are a type of suppository intended for vaginal

use.
● The larger size moulds are usually used in the
preparation of pessaries such as 4 g and 8 g moulds.
● Pessaries are used almost exclusively for local
medication, the exception being prostaglandin pessaries
that do exert a systemic effect.
● Pessaries
● Common ingredients for inclusion in pessaries for
local action include:
● antiseptics
● contraceptive agents
● local anaesthetics
● various therapeutic agents to treat trichomonal,
bacterial and monilial infections.
IDEAL SUPPOSITORY BASE:
1. Melts at body temperature or dissolves in body fluids.
2. Non-toxic and non-irritant.
3. Compatible with any medicament.
4. Releases any medicament readily.
5. Easily moulded and removed from the mould.
6. Stable to heating above the melting point.
7. Easy to handle.
8. Stable on storage.
I FATTY BASES: designed to melt at body
temperature.
1- Theobroma oil (Cocoa butter)
● 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.A melting range of 30 - 36°C (solid at room
temperature but melts in the body).
b.Readily melted on warming, rapid setting on
cooling.
c. Miscible with many ingredients.
d. Non-irritating.
⚫ Disadvantages:
⚫ a- Polymorphism:
- When melted and cooled it solidifies in different crystalline
forms, depending on the temperature of melting, rate of
cooling and the size of the mass.
- 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 produce unstable gamma crystals
which melt at about 15°C or alpha crystals melting at 20°C.
⚫Cocoa butter must be slowly melted over a warm water bath to
avoid the formation of the unstable crystalline form.
b. Adherence to the mould:
c. Softening point too low for hot climates.
d.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.
e. Rancidity on storage:
f. Poor water-absorbing ability: Improved by the
addition of emulsifying agents.
g. Leakage from the body:
h. Expensive
SYNTHETIC HARD FAT:
- For example: Suppocire,
witepsol. Advantages:
a.Their solidifying points are unaffected by
overheating.
b.They have good resistance to oxidation because of
the lower content of unsaturated fatty acids.
c.The difference between melting and setting points
is small. Hence they set quickly, the risk of
sedimentation of suspended ingredients is low.
d- They are marketed in a series of grades with different
melting point ranges, which can be chosen to suit
particular products and climatic condition.

e-They contain a proportion of w/o emulsifying agents,

and therefore, their water-absorbing capacities are good.

f- No mould lubricant is necessary because they contract

significantly on cooling.
Disadvantages:
a.Brittle if cooled rapidly, avoid refrigeration
during preparation.
b.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.
 ● II Water-soluble and water-miscible bases:
● 1- Glycero-gelatin:

● 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%.
 DISADVANTAGES:
a.A physiological effect: osmosis occurs during dissolving
in the mucous secretions of the rectum, producing a
laxative effect.
b.Can cause rectal irritation due to small amount of liquid
present.
c. Unpredictable solution time.
d.Hygroscopic: So, they should be packaged in tight
containers and also have dehydrating effects on the rectal
and vaginal mucosa leading to irritation.
e. Microbial contamination likely.
f. Long preparation time.
g. Lubrication of the mould is essential.
2- Macrogols (polyethylene glycols):
- Polyethylene glycols are polymers of ethylene oxide and
water, prepared to various chain lengths, molecular weights,
and physical states.
- The numerical designations refer to the average
molecular weights of each of the polymers.
- Polyethylene glycols (PEGs) having average molecular
weights of 300, 400, and 600 are clear, colorless liquids,
while those with molecular weights of 600- 1000 are
semisolids.
- Those having average 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.
● Drug release depends on the base dissolving rather
than melting.
● The melting point is often around 50°C.
● Higher proportions of high molecular weight
polymers
● produce preparations which release the drug slowly and are
also brittle.
● Preparation of suppositories:
●Suppositories are prepared by four methods: I
Hand moulding:
-Hand molding is useful when we are preparing a
small number of suppositories:
1. The drug is made into a fine powder.
2.It is incorporated into the suppository base by
kneading with it or by trituration in a mortar.
3.The kneaded mass is rolled between fingers into rod
shaped units.
4. The rods are cut into pieces and then one end is
● II Compression molding:
● 1. The cold mass of the base containing the
drug is compressed into suppositories using a
hand operated machine.
⚫**Advantages:
1. It is a simple method.
2.It gives suppositories that are more elegant than hand
moulded suppositories.
3.In this method sedimentation of solids in the base is
prevented.
4. Suitable for heat labile medicaments.
⚫**Disadvantages:
1.Air entrapment may take place. 2.This air
may cause weight variation.
3.The drug and/or the base may be oxidized by this air.
● III Pour moulding:
- Using a supp. mould which is made of metal or plastic.
Traditional metal moulds are in two halves which are
clamped together with a screw.
● Steps:
1.The base is melted and precautions are taken not to overheat
it.
2. The drug is incorporated in it.
3.The molten liquid mass is poured into chilled(lubricated if
cocoa butter or glycrogelatin is the base)molds.
4. After solidification the cone shaped suppositories
 Lubricating the 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 become absorbed and
will 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 pledget of gauze
or with fairly stiff brush.
 No lubricant
Base Lubricant
required

• Theobroma oil • Soap spirit • Synthetic fats

• Glycerol- • liquid paraffin • Macrogols
gelatin base
● IV Automatic Moulding machine:
● All the operations in pour moulding are done by
automatic machines. Using this machine, up to
about 10,000 suppositories per hour can be
produced.
● 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.