Suppositories & Pessaries
Introduction
Formulation(properties, classn of bases &
other excipients)
Preparation (calibration, displacement value)
Methods (fusion & compression)
Packaging, labelling & storage
Suppositories
Are special shaped solid dosage form of
medicament meant for insertion into body cavities
other than mouth(rectum, vagina& urethra).
They’ll melt /dissolve in the body cavity fluids to
release medicaments.
Its available various shapes, sizes &
weights(Generally 1-2 gms).
Base- cocoa butter / glycerogelatin
Pessaries
Special shaped (conical/rod/wedge) solid dosage
form of medicament meant for insertion into
vagina. Its larger than rectal supp.(3-6 gms).
Purposes/uses
To produce local action
To produce systemic action
To produce mechanical action on lower bowel
To facilitate evacuation in the treatment of
haemorrhoids, anal irritation, constipation, etc..
Advantages
Convenient mode of administration
Drugs which irritate the GIT, vomiting &
Destroyed by hepatic circulation/ by stomach
pH changes/ enzymes
Child/old persons/ unconcious / who cant
swallow
Rectal suppositories
It may be lubricating, soothing, antiseptic, local
anaesthetic action/ astringent effect.
Also meant for systemic effect contain analgesics,
antispasmodics, sedatives /tranquilizers.
Lower portion of rectum affords a large absorption
Surface area from which soluble subs. Can pass
quickly & reach the venous circulation directly
/rapid action of the drug.
…
However the rate & extent of absorption of drug
depends upon the nature of the base.
The maximum of therapeutic action is achieved by
drug incorporated in the finely divided
state/evenly distributed in the base
Types of suppositories
1.Rectal suppositories
2.Vaginal
3.Urethral
4.Nasal
5.Ear cones
Newer concepts of suppositories
1.Tablet
2.Layered
3.Coated
4.Capsule
5.Packing in disposable moulds
Suppository Bases
IDEAL PROPERTIES
1.Good in appearance
2.Melt at body temperature, dissolve/disperse in the body
cavity fluids
3.Retain its shape when handled
4.Stable on storage
5.Non-toxic&non-irritant
6.Easy release of incorporated medicament
7.Compatible with large number of drugs
8.Easy attain mould shape and non-stick
9.Easily mouldable by cold compression/pouring in mould
cavities
10.Not decompose if heated above its melting point
Types of suppository bases
Three types
1.Oily bases
2.Water soluble and water miscible bases
3.Emulsifying bases
1.Oily bases
(i) Theobroma oil
Known as coca butter
Crushed and roasted seeds of Theobroma cocoa
Yellowish white solid turns white on storage
Butter like consistency
Chocolate odour
Melting point 30-350C
Mixture of glyceryl esters of stearic,
palmitic,oleic and other fatty acids
Adv:
Widely used
melts at body temperature
release medicament into body cavity fluids
Rapid absorption
Good base for rectal suppositories
Not suitable for pessaries,urethral /nasal bougies
Disadvantages
Overheating changes physical characteristics
Sticky in nature
Polymorphism (different crystalline form) when
melted theobroma solidifies
Stable form obtained when melted mass allowed to
cool slowly &stand for a few days in a cool place
Rancid
Melts in warm weather
Sometimes immiscible with body fluids
(ii)Emulsified Theobroma oil
Used when large quantities of aqueous
solutions are incorporated
Agents used for emulsified theobroma oil 5%
glyceryl monostearate,10%lanette wax, 2-
3%cetyl alcohol,4%bees wax& spermaceti upto
12%
(iii)Hydrogenated oils
Substitute for theobroma oils
Eg.hydrogenated edible oil,coconut oil,palm kernel
oil,hydrogenated pea oil,stearin,mixture of stearic
&oleic acids
Advantages
1.Overhetating doesn’t affect solidifying point
2.Resistant to oxidation
3.Emulsifying & water absorbing capacities are good
4.Lubrication of mould not required
5.Produce colourless,odourless &elegant
suppositories
Disadvantages
Become brittle on rapid cooling in
refrigerator
More fluid when melted than theobroma oil
& result in sedimentation. Overcome by
adding thickening agent
2.Water soluble & water miscible
bases
(a) Glycero-gelatin
Its mixture of glycerin & Water.Made stiff by
adding gelatin
Stiffness depends on proportion of gelatin used
Hydrophilic nature,slowly dissolves in aqueous
solution&release medicaments
Used as vehicle in vaginal suppositories
Eg.belladonna extract, boric acid. Iodides
Gelatin used have two types
1. TYPE-A/PHARMAGEL-ACIDIC drugs
2. TYPE-B/PHARMGEL-ALKALINE DRUGS
Disadvantages
Less used
More difficult to prepare to handle
Hygroscopic must be stored in well closed
container
Gelatin is incompatible with many drugs
Support bacterial/mold growth
Solution time depends on content & quality of
gelatin used
(b) Soap glycerin suppositories
Curd soap/sodium stearate added with 95%
glycerin to harden suppositories.
Disadvantages
1.Hygroscopic
(c) Polyethylene glycols
Widely used
Known as carbowaxes & polyglycols
Molecular weight of 200 to 1000-liquids,more
than 1000 are wax like solids
Stable, physiologically inert
3.Emulsifying bases
1.Massa Esterinum
2.Witepsol
3. Massuppol
1) Massa Esterinum
1.Known as adeps solidus.
2.Mixture of mono,di,triglycerides of saturated
fatty acids
3.white,brittle,odourless,tasteless solid
4. Melts at 33.5% to 35.50C
5.Several types available-grade B is recommended
2) Witepsol
Triglycerides of saturated vegetable acid with
varying proportion of partial esters
Brittle & fracture when cooled
Mould must not be lubricated
3) Massuppol
Consists of glyceryl esters of lauric acid
Small amount of glyceryl monostearate added to
improve water absorbing capacity
Advantages
Overheating donot alter physical properties
Do not stick to mould
Do not require previous lubrication
Solidify rapidly
Less possiblity to rancid
Can absorb large amount of water
Preparation of suppositories
1.Rolling Method
2.Hot process/fusion method(moulding)
3.Cold compression method
1. Rolling method: By Hand rolling
2. Hot process or fusion method
Dispensary suppository 6 to 12 cavities with desired
shape &size
Large scale preparation moulds used upto 500 cavities
Made up of stainless steel,nickel-copper
alloy,brass,aluminium/plastic
Cleaning-lubrication or removal of suppository
longitudinally by removing screw in centre of plates
Opened plates immersed in hot detergent water,washed
&dried
Lubrication of moulds
To obtain suppository smooth surface
Prevent sticky nature
Soft soap 10gm,glycerol 10gm&alcohol(90%)
50ml is most suitable for oily bases
Liquid paraffin/arachis oil for glycero gelatin
suppository
Emulsifying base/macrogol base-no lubricant
used
Lubricating mould –brush or gauze swab is used
Cotton wool not used
Calibration of the mould
Standard mould of 15 grain/1 gramme
capacity used
Calibration for individual base &medicament
is used
Preparaing set of individual base alone
Weighing the product
Average mean is considered the true capacity
of the mould
Values recorded
Displacement value (D.V)
The quantity of the drug which displaces one part
of the base is known as D.V.
Since the volume of a suppository from a particular
mould remains same but its weight varies due to
the variation in densities of drug & the base with
which mould was calibrated.
To get a product of uniform & accurate weight,
allowances must be made for the change in density
of the mass due to added drugs.
For this purpose the D.V of the drug is taken into
consideration
3.Cold compression method
Suitable for thermolabile and insoluble drugs
Not suitable for glycerogelatin base
Prepared by mix powdered drug with an equal amount
of grated cocoa butter
Prepared mass placed in cylinder of machine
Force it to cavities of mould through narrow opening by
applying pressure to piston
Further apply pressure
Stop plate removed
Suppository taken out
On large scale hydraulically operated cold compression
machine are used.
Packing and storage
Packed in shallow
Partitioned cardboard boxes
If plain boxes used suppository should be
wrapped in waxed paper/tin foil
Glycerogelatin suppository packed in well
closed glass/plastic container
Labelling
Labelled as “Store in a cool place “ & warning
“not to be taken orally” or “for rectal use only”
