SUPPOSITORIES
Presented by
Miss. SURITA GHOSH
Assistant professor in pharmaceutics
SETGOI
What Is a Suppository?
Solid or semi-solid dosage form
Intended for insertion into body orifices or
cavity ( Rectum, Vagina, Urethra )
They melt, soften or dissolve in the body
orifices or cavity with the help of body
tempareture and exert local or systemic effect.
2
Oral route
not useful.
ADVANTAGES Patient – GIT
problems,
Nauseous or
post
operative.
Drugs with
Very young ,
an
very old, or
unacceptable Advantages the mentally
taste can be
disturbed.
administered.
Drug - first Drug have GI
pass
metabolism. Drug - not side effects.
stable at GI
pH or
susceptible to 6
enzymatic
attack in the
GI tract
Need t o DISADVANTAGES
store at
low
temp
Embarrass-
ment to Leakage
patients
. Disadvantages
Large scale
Sometimes
production
incomplete
difficult
absorption.
and costly
I r r i tant d r u g cant 7
administered.
Ideal Properties
Should be completely non-toxic & non-irritant.
Should be compatible with a broad variety of drugs.
Should be non-sensitizing.
Should have wetting & emulsifying properties.
Should be stable on the storage i.e. does not
change color, odor or drug release pattern.
5
Types of suppositories
1. Rectal suppositories.
2. Vaginal suppositories.
3. Urethral suppositories.
4. Nasal suppositories.
5. Ear cones.
Rectal Suppository Urethral Suppository Vaginal Suppository
SHAPE OF SUPPOSITORIES
8
FORMULATION OF SUPPOSITORIES
A) Bases
B) Antioxidants
C) Emulsifying agents
D) Hardening agents
E) Preservatives
F) Thickening agents
G) Plasticizer
9
SUPPOSITORY bASE
Suppository bases plays important role in
maintaining their shape, solidity & also play
important role when inserted into the body
cavity.
Melt at body temp.
Should not adhere Dissolve or disperse
to the mould in body fluids
Release any
Easily mouldable medicament readily
Properties of an ideal suppository base
Stable above its Retain its shape
melting point when handled
Compatible with all Non-toxic & non-
medicaments irritant to mucous
membrane
34
Stable on storage
TYPES OF SUPPOSITORY BASES
1. Oleaginous bases or fatty base
1. Cocoa butter.
2. Emulsified cocoa butter.
3. Hydrogenated oils.
2. Hydrophilic bases
1. Glycero-gelatin base.
2. Soap-glycerin base.
3. Polyethylene glycol.
3. Emulsifying/Synthetic bases
1. Witepsol
2. Massa estarinum
35
3. Massuppol.
COCOA BUTTER (Theobroma oil)
Cocoa butter is fat obtained from the roasted seed of Theobroma cocoa
It is natural triglyceride.
Among all fatty acid about 40% are unsaturated fatty acid .
It can exist in more than one crystalline form or exhibits polymorphism.
At room temperature ,it is yellowish- white with a paints,chocolate like
odour.
It consists of a mixture of ester of oleic acid,palmatic acid,stearic acid and
other fatty acid with glycerol
ADVANTAGES
Melting range 30-36 0c,easily melts in the body
Readily melted on warming,rapid settling on cooling.
Miscible with many other ingredients.
Non-irritating.
DISADVANTAGES
Exhibits marked polymorphism.
Rancidity.
Stick to mould.
Leakage from body cavity.
Costly.
Immiscibility with body fluid.
Chloral hydrate or lactic acid liquefy it.
Hydrophilic bases
Glycero gelatin base
It is a mixture of glycerin and water which is made stiff by the addition of
gelatin
Properties:
It is colourless, transparent, translucent in nature.
It is soft to touch.
It melts at 30 - 350C
Type of gelatin bases: to avoidincompatibility
Type A or Pharmagel A: acidic in nature and used for acidic drugs.
Type B or Pharmagel B: alkaline in nature and used for basic drugs.
Used for vaginal suppositories
Glycero- Gelatin Base
Advantages
It melt at body temperature. It mix with
body fluid.
Not rancid.
It can be used to prepare suppositories using boric acid, chloral hydrate
bromides, iodides, iodoform opium etc.
Disadvantage
Difficult to prepare and handle.
Chance of bacterial growth.
Hygroscopic in nature. (become hard on drying and soft in cont with
moisture)
Laxative in action.
Incompatible with tannic acid, gallic acid, ferric chloride etc
Polyethylene Glycols/ Macrogols
These are available in solid, liquid or semi-solid state
depending on molecular weight.
Advantages:
They are chemically stable.
Inert, Non-irritant.
Do not allow bacterial growth.
Physical properties changes according to molecular weight.
Provide prolonged action.
Do not stick to mould.
Suppositories are clean and smooth in appearance.
Disadvantages
Hygroscopic in nature.
Incompatibility with some drugs tannins phenol etc.
Good solvent properties.
Supersaturation takes place
ANTI OXIDANTS
It protect the drugs and bases from getting degraded due to
oxidation.
These are commonly used in all types of suppositories.
EXAMPLES-
Ethyl or propyl gallate
Ascorbic acid
Butylated hydroxy anisole (BHA)
Butylated hydroxy toluene (BHT)
Hydroquinone
Tocopherol
19
EMULSIFYING AGENTS
These increase the water absorbing capacity of fatty bases.
EXAMPLES
Poly sorbates (TWEEN 61)
Wool alcohol
Wool fats
20
HARDENING AGENTS
These are involved in those formulation where the melting point
of the bases is decrease by the drugs.
These are the agents which are used to bring the melting point to
normal.
EXAMPLES
Beeswax
Macrogols at high molecular weight.
21
PRESERVATIVES
These are the agents which are used in prevent the growth of
microbial in suppository which contains water soluble bases.
EXAMPLES
Chorocresol
Methyl paraben
Propyl paraben
22
THICKENING AGENTS
These are the agents which are used to increases the viscosity of
molten bases and prevent sedimentation of suspended in solid
bases.
EXAMPLES
Aluminium monostearate
Colloidal silica
Magnisium stearate
Steary alcohol
23
PLASTICIZERS
These are the agent which are used to improved flexibility of
suppositories.
It is also used to make the less brittles to suppositories.
EXAMPLES
Castor oils
Glycerine
Glycol
Tween 80
Tween 85
24
METHOD OF PREPARATION
I. HAND ROLLING METHOD
II. FUSION METHOD
III. COLD COMPRESSION METHOD
25
HAND ROLLING METHOD
DRUG+ADDITIVES FINE POWDER
MIXED IN BASES
APPLY LUBRICANTS ON ROLLING TILE
ABOVE MASSES ARE ROOLED IN CYLINDRICAL SHAPE
CUT THE RODS
PACKED
STORED 66
MOLDS USED IN PREPARATION OF
SUPPOSITORIES-
Molds used in preparation of suppositories are the
metals devised with different shape.
It is consists of two or more parts which are joined
with a screw.
In side the molds the cavities are made up of
aluminium , brass, stainless steel , plastics.
Molds have different capacities like 1,2,4,8gm.
PREPARATION OF SUPPOSITORIES - MOULDS
30
FUSION METHOD
MELTING THE BASES DRUGS
FINE POWDER
TRITURATE
WITH WARM WATER
LIQUIDS
MIXED ½ PARTS OF LIQUIDS
MIXING PROPER
ADD REMAINS LIQUIDS
32
CONT……
APPLY THE LUBRICANTS IN MOLD
OVERFILLING OF MASSESIN MOLDS
REMOVE THE EXTRAMASSES
COOLING (10-15MIN)
OPEN MOLDS
PACKED
71
STORED
Automatic Molding Machine
PROCEDURE
DRUG+ADDITIVES FINE POWDER
MIXED WITH BASES
LUBRICANTS APPLY IN MOLDS
PLACED THE MASSES IN CYLINDER
APPLY PRESSURE
RELEASE SUPPOSITORY
COOLED PACKED STORED
35
DRUG+ADDITIVES FINE POWDER
MELT BASES + POWER
HOPPER
LUBRICATED THE MOLDS
FILL ABOVE MIXTURE INMOLD
COOLING SYSTEM
EJECTION SYSTEM
PACKED STORED
36
THANK YOU
