Merits and demerits, types, bases, preparation, packing and use

1. SUPPOSITORIES &
PESSARIES
Parag Jain
Assistant Professor
Chhattrapati Shivaji Institute
of Pharmacy
Durg, Chhattisgarh
Presented by

2. Definition
• Semi-solid dosage forms intended for insertion into the body
orifices where it; melt , soften dissolve and exert localized or
systemic effects
• A suppository is a medicated solid dosage form generally
intended for use in the rectum, vagina and to a lesser extent, the
urethra.
• After insertion they melt or soften at body temperature, whereas
vaginal suppositories sometimes called as pessaries, are also
made as compressed tablets that disintegrate in body fluids.

3. Shape and size of suppositories

4. Advantages
Oral route not
useful.
Patient – GIT
problems,
Nauseous or
post
operative.
Very young ,
very old, or
the mentally
disturbed.
Drug have GI
side effects.
Drug - not
stable at GI
pH or
susceptible to
enzymatic
attack in the
GI tract
Drug - first
pass
metabolism.
Drugs with an
unacceptable
taste can be
administered.
Drug that
may be
abused as in
suicide.

5. Disadvantages
Mucosal
irritation
Traditional
Issues-
feeling of
aversion
Leakage
Sometimes
incomplete
absorption.
Inter and
intra
subject
variation.
Proctitis.
Large scale
production
difficult
and costly
Shelf life
(stringent
storage
conditions)
.
GI state
affects
absorption

6. TYPES OF SUPPOSITORIES
• Cone or torpedo shaped weighing 1 – 2 gRectal
• Globular, oviform, cone or wedge shaped weighing
2 – 8 g
• Made from glycero-gelatin or macrogol base
Vaginal
(pessaries)
• Thin pencil shaped pointed at one end
• Male bougies – 4 g and 100-150 mm
• Female bougies – 2 g and 60 – 75 mm
Urethral bougies
• Thin pencil shaped with pointed ends
• 1.2 g and 9 – 10 mm long
Nasal bougies
•Pencil shapedEar cones

8. Melt at body temp.
Dissolve or disperse
in body fluids
Release any
medicament readily
Retain its shape
when handled
Non-toxic & non-
irritant to mucous
membrane
Stable on storage
Compatible with all
medicaments
Stable above its
melting point
Easily mouldable
Should not adhere
to the mould
Properties of an ideal suppository base

9. TYPES OF SUPPOSITORIESBASES
Suppository
bases
Fatty bases
Cocoa Butter
Synthetic fats
Proprietary
synthetic
bases
Water soluble
or water
miscible bases
Glycero-
gelatin
Macrogols

10. Fatty bases

11. Properties It is the most widely used suppository base. And it is used
in the prescriptions when no base is specified.
It is naturally occuring triglyceride with oleopalmitostearin
and oleodistearin glyceride chain and contains 40% of the
unsaturated fatty acid.
It is yellowish white, solid, brittle fat, which smells and
tastes like chocolate.
Its melting point lies between 30-35oC (86-95oF) its iodine
value is between 34 - 38 and its acid value is no higher than
4.
It satisfies the requirements for an ideal base – non-reactive,
and melts at body temp.

12. Disadvantages
Polymorphism
Adherence to
mould
Low softening
point
Melting point
reduction
Deterioration
during storage
Poor water
absorbing
capacity
Leakage from
the body

13. POLYMORPHISM
Polymorphism in cocoa butter is observed due to
high proportion of unsaturated triglycerides.
The formation of various forms of cocoa butter
depends on the degree of heating, on the cooling
process and on the conditions during this process.
Each form of cocoa butter has different melting
point and drug release rates.

14. Cocoa butter exits in four crystalline state
α form
• melts at 24oC
• Obtained by
suddenly
cooling
melted cocoa
butter to 0oC.
ß form
• Crystallizes
out of the
liquefied
cocoa butter
with stirring at
18 to 23oC.
• Its melting
point lies
between 28
and 31oC.
ß` form
• changes
slowly into
the stable ß
form.
• Melts between
34 and 35oC.
• Change is
accompanied
by volume
contraction.
γ form
• melts at 18oC
• Obtained by
pouring a cool
cocoa butter,
before it
solidifies, into
a container
which is
cooled at deep
freeze temp.

15. Cocoa butter does not contract sufficiently on
cooling to loosen the suppositories in the mould.
Sticking may be overcome by adequate
lubrication.
Softening
point too
low for hot
climates
To raise the softening point, white bees wax may be
added to theobroma oil suppositories intended for use
in tropical and subtropical countries.
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.
Adherence to the
mould

16. Rancidity
on storage:
Due to the oxidation of unsaturated glycerides.
Poor
water-
absorbing
ability:
Improved by the addition of emulsifying
agents.
Leakage
from the
body:
Sometimes the melted base escapes from the
rectum or vagina, so, it is rarely used as a
pessary base.
Expensive Relatively high cost

17. SYNTHETIC FATS
To overcome the disadvantages of theobroma oil synthetic
substitutes were searched.
Obtained from hydrogenation and heat treatment to
vegetable oils such as palm kernel and arachis.
Hydrogenation saturates unsaturated glycerides and heat
treatment splits some of the triglycerides into fatty acid
and partial esters (mono and di glycerides).
Most synthetic fat bases are made by first hydrolysing the
vegetable oil, then hydrogenating the resulting fatty acids
and finally esterifying the acids by heating with glycerol.

18. Their solidifying points are unaffected by over heating.
They have good resistance to oxidation because their
unsaturated fatty acids have been reduced.
The difference between melting and setting points is small;
generally only 1.5 to 2oC and seldom over 3oC. Hence,
they set quickly, the risk of sedimentation is low and they
are easier to administer.
The melting point depression caused by fat soluble drugs
can be counteracted by choosing a high melting point
grade, while the hardness and brittleness that sometimes
results from a high content of insoluble powder can be
prevented by using a low melting point grade.
Advantages

19. High softening point grades are advantageous for
tropical and sub tropical formulations.
They usually contain a proportion of partial glycerides
some of which e.g. glyceryl monostearate, are w/o
emulsifying agents and therefore their emulsifying and
water absorbing capacities are good.
No mould lubricant is needed because they contract
significantly on cooling.
They produce suppositories that are white and almost
odourless and have very attractive, clean and polished
appearance.
Advantages

20. Disadvantages
They are more fluid than theobroma oil
when melted and at this stage sedimentation
is greater. Thickeners such as magnesium
stearate, bentonite reduce this problem.
The release and absorption of drugs in the
body may differ for theobroma oil and
synthetic bases.
They should not be cooled in a refrigerator or
ice because they become brittle if cooled
quickly.Additives such as polysorbate 80
correct this fault.

21. PROPRIETARY SYNTHETICBASES
Whitepsol (formerly
called Imhausen)
• It consists of
triglycerides of
saturated vegetable
acids (C12 to C18) with
varying proportions of
partial esters.
• The W45 grade is
used for general
dispensing.
Massa Estarinum
• It consists of mixture of
tri, di and
monoglycerides of
saturated fatty acids
with chain lengths of
C11 to C17. Grade B is
recommended for
general dispensing.
• This differs from the
previous materials in
being single general
purpose base with only
one modification, for
cold moulding.
• It consists of glyceryl
esters, mainly of lauric
acid to which a small
amount of glyceryl
monostearate has been
added to improve its
water absorbing
capacity.
• The B.P.C allows the
use of hydrogenated
vegetable oils provided
the melting point of the
suppositories is not
above 37oC.
Massuppol

22. WATER SOLUBLE OR
WATER MISCIBLE BASES

23. GLYCERO-GELATIN
This is a mixture of glycerol and water into a stiff jelly by adding
gelatin.
It is used for making jellies, suppositories and pessaries and its
proportion is changed according to its intended purpose.
Glycero-gelatin dissolves in body secretions and therefore is
preferable to a fatty base for administering antiseptics.
Since, solution is slow, drug release is more prolonged than from
fatty base.
At present the B.P allows a maximum disintegration time of 1 hr. for
Glycerol Suppositories B.P made with gelatin of B.P standard.

24. Disadvantages
of glycero-
gelatin base
They are more difficult to prepare and handle.
Their solution time depends on the content and quality and
gelatin and the age of the base.
They are hygroscopic. So a careful storage is required. It
also leads to dehydration of the rectal mucosa with
consequent irritation; this is an advantage where a laxative
effect is required.
Gelatin is incompatible with protein precipitants such as
tannic acid.
They have a physiological action (used as laxative)

25. MACROGOLS (PEG)
Properties long chain polymers of ethylene oxide with general
formula HOCH2(CH2OCH2)8CH2OH
Exist as liquid if their average molecular range from
200 to 600 and they exist as wax like solid it is above
1000.
Their water solubility, hygroscopicity and vapour
pressure with increase in average molecular weight.
They do not hydrolyse or deteriorate and are
physiologically inert and do not support mold
growth.
The PEG suppositories can be prepared by both
moulding and cold compression methods.

26. 1.The mixtures have melting point above 42oC. Hence, cool
storage is not required, they are satisfactory for use in hot
climates, and administration is easy because they are not
slippery to handle.
2.Because of this high melting point they do not melt in the
body but gradually dissolve and disperse, freeing their
medication slowly and providing longer action than fatty
bases.
3.Their physical properties can be varied by suitable admixture
of high and low polymers. High polymers give hard products
that disintegrate and release their drug slowly.
ADVANTAGES OF MACROGOLS

27. ADVANTAGES OF MACROGOLS4.They do not stick to the mould since they contract on
cooling.
5.Because of their high molecular weight solution of
high viscosity are produced when they disperse in the
body.
6.They absorb water well and have excellent solvent
properties.
7. Products have clean smooth appearance.
ADVANTAGES OF MACROGOLS

28. 1.They are hygroscopic so careful storage is required. Irritancy can
be reduced by incorporating about 20% of water in the mass or by
instructing the patient to dip the preparation in water just before
insertion. This type of base is suitable for systemically active drugs.
2.Its good solvent properties can result in retention of the drug in the
liquefied base in the body with consequent reduction in therapeutic
activity.
3.Products sometimes fracture on storage, particularly if they
contain. High solubility of macrogols which can lead to a super
saturated solution in the water and subsequent crystallisation and
this the mass granular and brittle.
DISADVANTAGES OFMACROGOLS

29. 4.Crystal growth of certain medicaments may occur
particularly if they are partly in solution and partly in
suspension in the base. This makes the product brittle
and crystals may be irritating because they are large
and takes longer time to dissolve.
5.They are incompatible with bismuth salts, tannins
and phenol. They lower the activity of some
antibacterial agents and dissolve certain plastics
necessitating care in choosing containers.
DISADVANTAGES OFMACROGOLS

30. PREPARATION OF
SUPPOSITORIES AND
PESSARIES

31. 1. Moulding
2. Hand rolling
3. Compression
METHODS OF PREPARATION

32. PREPARATION OF SUPPOSITORIES-
MOULDS

33. PREPARATION BY MOLDING
• The steps in molding include
(a) melting the base,
(b) incorporating any required medicaments,
(c) pouring the melt into molds,
(d) allowing the melt to cool and congeal into suppositories,
(e) removing the formed suppositories from the mold.
• Cocoa butter, glycerinated gelatin, polyethylene glycol,
and most other bases are suitable for preparation by
molding.

34. Suppository Molds
• Molds in common use today are made from stainless
steel, aluminum, brass, or plastic.
• reusable and disposable Commercially available molds
available for preparation of rectal, vaginal, and urethral
suppositories, can produce individual or large numbers of
suppositories of various shapes and sizes.

35. Lubrication of the Mold
• Depending on the formulation, suppository molds may
require lubrication before the melt is poured to facilitate
clean and easy removal of the molded suppositories.
• Lubrication is seldom necessary when the base is cocoa
butter or polyethylene glycol.
• Lubrication is usually necessary with glycerinated gelatin.
• A thin coating of mineral oil applied with the finger to the
molding surfaces usually suffices.

36. lubrication before the melt is poured to facilitate clean and
easy removal of the molded suppositories

37. Calibration of the Mold
• Each individual mold is capable of holding a specific
volume of material in each of its openings.
• Different bases prepared in the same mold will have
different weight Because of the difference in the densities
of the materials, Similarly, any added medicinal agent
alters the density of the base, and the weight of the
resulting suppository differs from that of those prepared
with base material alone.
• The pharmacist should calibrate each suppository mold
for the usual base (generally cocoa butter and a
polyethylene glycol base) so as to prepare medicated
suppositories each having the proper quantity of
medicaments.

38. Determination of the Amount
of Base Required
• Knowing the amount of drug substances provided in each
suppository subtracted from the total volume of the mold
will give the volume of base required.
• if considerable quantities of other substances are to be
used, The total volume of these materials is subtracted
from the volume of the mold, and the appropriate amount
of base is added.
• Because the bases are solid at room temperature, the
volume of base may be converted to weight from the
density of the material.

39. Preparing and Pouring the Melt
- Using the least possible heat over a water bath, the weighed
suppository base material is melted on porcelain casserole .
- Medicinal substances are incorporated into a portion of the
melted base by mixing on a glass or porcelain tile with a
spatula.
- After incorporation, this material is stirred into the
remaining base, which has been allowed to cool almost to its
congealing point.
- Any volatile materials or heat-labile substances should be
incorporated at this point with thorough stirring.

40. Preparing and Pouring the Melt
- The melt is poured carefully and continuously into each cavity
of the mold, which has been previously equilibrated to room
temperature.
- If any undissolved or suspended materials in the mixture are
denser than the base, so that they have a tendency to settle,
constant stirring, even during pouring, is required,
- The mold is usually placed in the refrigerator , after harding ,
the mold is removed from the refrigerator and allowed to come
to room temperature. Then the sections of the mold are
separated, and the suppositories are dislodged, with pressure
being exerted principally on their ends and only if needed on
the tips.
- Generally, little or no pressure is required, and the
suppositories simply fall out of the mold when it is opened.

42. II] HAND ROLLING
Hand molding is useful when we are preparing a small
number of suppositories
The drug is
made into fine
powder
Incorporated
into suppository
base
By trituration or
kneading
Mass is rolled
into rod shape
by fingers
Rods are cut
into pieces
Desired shape
is given by
hand

43. III] COMPRESSION MOLDING -LARGE SCALE
OPERATION
Prepared mass C is placed in a cylinder A
It is forced through narrow opening D by
means of piston B into a mould.
Threads of mass pass in the mould G
and are compressed until a homogenous
fused mass is formed in E.
On removal of retaining plate F the
suppositories are ejected by further
pressure.
The mass and compression cylinder of
the machine may be chilled to prevent
heat of compression from making the
mass too fluid.
Useful for moulding suppositories
containing insoluble solids (no risk of
s e d i m e n t a t i o n ) o r t h e r m o l a b i l e
medicaments.
Unsuitable for glycero-gelatin products

44. 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
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

45. PACKAGING AND LABELLING FOR
SUPPOSITORIES
Rigid paperboard
boxes
Flat box with a lid
Labelling :
1. Store in a cool place
2. For rectal use only or not to be taken orally
3. Moisten before use (for glycero-gelatin and
macrogol bases)

46. PACKAGING AND LABELLING FOR PESSARIES
Glass bottles Plastic bottles
Labelling :
1. Moisten the pessaries with water before insertion to
reduce stinging caused by osmotic withdrawl of water
to reduce the tissues during solution in vagina.
2. For vaginal use only or not to be taken orally.
3. Store in a cool place.

47. Website: www.probecell.com Email: probecellinfo@gmail.com
Ph: 7415211131
Office: Smriti Nagar, Bhilai, Chhattisgarh - 490020
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