SUPPOSITORIES &

PESSARIES
 SUPPOSITORIES & PESSARIES
Define suppositories and pessaries.
Differentiate between suppositories
and pessaries.
Classify suppositories
Advantages & disadvantages of suppositories.
Discuss different suppository bases used.
Discuss the different method of preparation
Q. C. of Suppositories
 SUPPOSITORIES & PESSARIES
Suppositories are solid dosage forms intended for
insertion into body orifices where they melt, soften,
or dissolve and exert localized or systemic effects.

SUPPOSITORIES:
British Pharmacopoeia (BP) definition:
“Suppositories are solid, single-dose
preparations. The shape, volume and
consistency of suppositories are suitable for
rectal administration.”
 SUPPOSITORIES & PESSARIES
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.
 SUPPOSITORIES & PESSARIES
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 meant for

introduction in to nasal cavity.
They are prepared with glycerogelatin base.
They weigh about 1 gm and length 9-10 cm.
 SUPPOSITORIES & PESSARIES
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.
 SUPPOSITORIES & PESSARIES
ADVANTAGES:
_ Can be used for systemic absorption of drugs and avoid
first-pass metabolism.
_ Can exert local effect on rectal mucosa.
_ Used to promote evacuation of bowel.
_ Avoid any gastrointestinal irritation.
_ Can be used in unconscious patients
_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.
 SUPPOSITORIES & PESSARIES
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.
 Therapeutic uses
Suppository can be used for local or systemic effect.

The action depends on nature of drug , concentration

and rate of absorption

Rectal suppository are intended for treatment of

constipation and hemorrhoids.

Suppositories are also administered for systemic

action (analgesics, antispasmodics, sedatives &
tranquilizers).
 SUPPOSITORIES & PESSARIES
Pessaries are a type of suppository intended for vaginal use.
(Vaginal suppositories)
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.
 SUPPOSITORIES & PESSARIES
British Pharmacopoeia (BP) definition:
“ Pessaries are solid, single-dose preparations. They have
various shapes, usually ovoid, with a volume and consistency
suitable for insertion into the vagina. They contain one or
more active substances dispersed or dissolved in a suitable
bases that may be soluble or dispersible in water or may melt
at body temperature. Excipients such as diluents, adsorbents,
surface-active agents, lubricants, antimicrobial preservatives
and colouring matter, authorised by the competent authority,
may be added, if necessary.”
 SUPPOSITORIES & PESSARIES
TYPE 1- Fatty Bases / Oleagenous 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.
 SUPPOSITORIES & PESSARIES
Theobroma oil (Cocoa butter)
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.
 SUPPOSITORIES & PESSARIES
Disadvantages of Theobroma oil (Cocoa butter)
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 15-18°C or alpha crystals melting at 20-24°C.
Cocoa butter must be slowly melted over a warm water bath to
avoid the formation of the unstable crystalline form.
 SUPPOSITORIES & PESSARIES
b- Adherence to the mould: no contraction-needs
lubrication of mold.
c- Softening point too low for hot climates.
d- Melting point reduced by soluble ingredients: Phenol,
vol oil 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:Oxidatn of unsat glycerides
f- Poor water-absorbing ability: Improved by the addition of
emulsifying agents tweens
g- Leakage from the body
h- Expensive
SUPPOSITORIES & PESSARIES
Type II- Water-soluble and water-miscible bases:
A. 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%.
Glycerin partially substituted by PEG/PG for consistancy
Liable to mold growth- addn of preservatives
 SUPPOSITORIES & PESSARIES
DISADVANTAGES OF GLYCEROGELATIN BASES:
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. also have dehydrating effects on the rectal and
vaginal mucosa leading to irritation.
c- Unpredictable solution time.
d- Hygroscopic: So, they should be packaged in tight containers
e- Microbial contamination likely.
f- Long preparation time.
g- Lubrication of the mould is essential.
 SUPPOSITORIES & PESSARIES
2- Macrogols (polyethylene glycols):(CARBOWAXES)
- Polyethylene glycols are polymers of ethylene oxide and
water, prepared to various chain lengths, molecular weights,
and physical states.
- The numerical designations- average MOL WT
- Polyethylene glycols (PEGs) having avg mol.wts of 300, 400,
and 600 : clear, colorless liquids, while mol.wts of 600-1000,
semisolids.
- Those having average molecular weights of greater than 1000
ie1540,4000,6000 are wax-like, white solids with the hardness
increasing with an increase in the molecular weight.
 SUPPOSITORIES & PESSARIES
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.
Less brittle products which release the drug more readily
can be prepared by mixing high polymers with medium
and low polymers.
 SUPPOSITORIES & PESSARIES
III.SYNTHETIC HARD FAT/ EMULSIFYING BASES:
- For example: Suppocire, witepsol, Massupol
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.
 SUPPOSITORIES & PESSARIES
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.
 SUPPOSITORIES & PESSARIES
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.