SUPPOSITORIES AND ITS TYPES, BASES, INCOMPATIBILITY

SUPPOSITORIES
SUDHANNSHU SAGAR
Assistant professor
BHARTIYA PHARMACY COLLEGE, GAJRAULA

DEFINITION
These are solid or semisolid dosage forms, which are meant for insertion into the body
cavity such as the rectum, vagina, etc.
When these suppositories inserted, they melt disintegrate and dissolve at body temp. and
give their effect either local or systemic distribution. e.g. Pessaries, rectal suppositories
etc.
ADVANTAGES of SUPPOSITORIES
1. It avoids first-pass metabolism.
2. It can be used for unconscious patients.
3. It can be used for delivering higher amounts of doses.
4. It can be used for those patients who have swallowing difficulty (i.e.. children & old
aged)
5. Useful for local and rapid and rapid effects.

1. Patient acceptance and not comfortable.
2. It is more expensive than tablets.
3. Irritant drugs can’t be administered.
4. We need to store it at a low temperature.
Types of SUPPOSITORIES
Based on their use, they can be classified into five types:-
1. Rectal suppositories
2. Vaginal suppositories
3. Urethral suppositories
4. Nasal suppositories
5. Ear cones (arenarias)
Disadvantages of SUPPOSITORIES

1. RECTAL SUPPOSITORIES
 These are those suppositories that are meant for insertion into the rectum.
 For adults, it is about 2gm; for infants, it is one-half.
 It contains Theobroma oil or cocoa butter as a suppository base.
 e.g. Sedatives, Analgesics, etc.
Shape
tapped at one end or both ends.
2. VAGINAL SUPPOSITORIES
Also known as pessaries
 These are those suppositories that are meant for insertion into the vagina.
 These are globular/ oviform shaped, weighing about 5gm,
and containing a PEG base.
 These are mainly used for vaginal infection or as contraceptive drugs

These are those suppositories that are meant for insertion into the urethra.
It is also known as Bougies
It is made up of cocoa butter and about 2 gm for females and, 4gm for males weight.
These are in the shape of micro pellets (1.4mm diameter, 6mm long] and inserted 3cm) deep
into the urethra.
Alprostadil for treating erectile dysfunction.
4. NASAL SUPPOSITORIES (BOUGIES)
These are those suppositories that are in the nasal cavity meant for insertion
These are prepared from a gelato glycerine base.
These are thinner, 8cm in size, about 1 gm in weight.
3. URETHRAL SUPPOSITORIES

5. Ear cones (aurnarias)
These are those suppositories which are meant for insertion into the far cavity.
Also known as Aurinarias.
SUPPOSITORIES BASES
 These are those excipients that are used in the manufacturing of suppositories.
 These are the major parts of suppositories and play a major important role in –
 Maintaining the shape and solidity of suppositories
 In the release of medicaments.
 After being inserted into the body cavity, suppository bases get melted and release
medicament which provides effects.
 Ex:- Theobroma oil (cocoa butter), PEG (polyethylene glycol). Etc.

Bases based on their composition and physical properties, are classified as:-
 Oleaginous (fatty) bases,
 Aqueous bases (or water-soluble/miscible)
 Emulsifying bases.
PROPERTIES OF IDEAL SUPPOSITORIES BASES
 It should be melt of body temperature to release the drug.
 It should be non-toxic, non-irritant & non-sensitive.
 It should be compatible with most of the drugs.
 It should be easily mouldable and not adhere to moulds.
 It should be and stable on stable above its melting point storage
 It should retain its shape when handled
TYPES OF SUPPOSITORIES

1. OLEAGINOUS BASES
These are fatty bases and it is of two types →
i. Theobroma oil (cocoa butter)
ii. Triglycerides
 It is also known as Cocoa butter.
 It is the most commonly used suppository base and an ideal base.
 It is yellowish-white in color and like butter.
 It exists as a hard, amorphous solid at 15-20°C and melts at 30-35°C [body temp].
 It is obtained from the roasted seed of (Theobroma cocoa.)
THEOBROMA OIL

 These are made up of Hydrogenated vegetable oils.
 These are synthetic triglycerides.
 These are sometimes used as substitutes of Theobroma oil.
 These are more expensive than Theobroma oil.
e.g. Palm oil, coconut oil, etc.
2. TRIGLYCERIDES
3. AQUEOUS BASES
These are water-soluble bases and it is further two types –
1. Glycerinated Gelatin:-
 It is a mixture of glycerine and water which further makes a stiff jelly type by adding
gelatin (Prolong release).
 This base is mostly used for vaginal suppositories.

 These bases are polymers in nature and are used for prolonging the release of drugs.
 Nowadays, these bases are used for their properties like being chemically stable, nor-
irritant, and miscible with water.
3. Emulsifying bases
 These are also fatty bases and contain higher molecular weight.
 Massa esterinum – comprises of monoditriglycerides of F.A
 Witepsol comprises hydrogenated triglycerides of lauric acid with added monoglycerides.
2. Polyethylene Glycols
 These suppositories should be stored in a cool place (10-15°C) and also require
preservatives.
 It is hygroscope in nature.

It can be prepared by three methods:-
 Hand Rolling Method
 Compression method
 Hot fusion Method
 Hand Rolling Method:-
 It is the simplest and most traditional method.
 It is used for a small scale or a few no. of suppositories by using cocoa butter with hands.
PROCESS
 First, cocoa butter, drug, and all other ingredients are mixed properly by using a pestle mortar
 The prepared mass is shaped into a ball by using a palm, then into a cylindrical form by using a
spatula, then cut a small portion and form a conical shape by using hands.
 It is prepared by slciful workers.
METHOD OF PREPARATION

 It is also known as cold compression molding.
 In this, suppositories are prepared by compressing.
PROCESS
• First mix all ingredients with a suppository base and make fine powder.
↓
• Now, fill this mass in the cylinder and apply lubricants in the moulds.
↓
• On compression, suppositories mass filled into moulds and get shaped, then taken out &
packed.
 Compression Method:-•

In this method, heat is used. It is not suitable for heat-sensitive substances.
PROCESS
 Firstly, the suppository base is melted, and the drug; and other excipients are dissolved in it.
 The mixture is removed from the heat and poured into suppository moulds.
 After solidifies, suppositories are removed from moulds.
SUPPOSITORY MOULDS –
 On the small scale, it has 6-12 cavities of different shapes and sizes,
 On a large scale, it has around 500 moulds cavities,
 Hot fusion method

DIFFERENT TYPES OF SUPPOSITORY
MOULDS THAT IS USED TO
FORMULATE THE SUPPOSITORIES

It is defined as the amount of drug displacing one part of the suppository base.
It is necessary to calculate this because suppositories of the same size can vary in
weight due to the nature of drugs
It can be calculated based on Theobroma oil as a suppository base
DISPLACEMENT VALUE
Displacement = (d/a-c)
Value (DV)
where, D a DV = Displacement value
d = amount of medicament present in Suppositories.
a = weight of base in suppositories [no medicine]
c = weight of medicament
a-c = amount of base displaced by medicament

Suppositories should be evaluated to check whether they fulfill the standard requirements or not.
The following tests should be performed examination
 Visual Examination / Appearance Test
 Mechanical Strength / Crushing Test
 Uniformity of Weight / Drug Content
 Melting Range Test
 Dissolution / Disintegration
 Softening of Liquefication Test
EVALUATION OF SUPPOSITORIES

Uniformity of weight:
Visual examination:
 In this, we check the appearance of suppositories visually.
 It is performed by examination of shape, surface, color, and odour
manually.
Mechanical strength / crushing test:
In this, we have to check the brittleness and elasticity of suppositories.
 For this, the suppository fits in the machine, and external
weight/force on it
 An ideal suppository can tolerate/face about 1.8.2kg pressure.
 mainly used to check transportation conditions
 In this, we have to check the weight of suppositories is equal and
that they contain an equal amount of drugs. For this, weigh 20
suppositories and calculate their average weight.

For ideal suppositories, the deviation is not more than 5% b/w average and individual
weight.
Melting Range test:
 In this, we have to check the melting range/point of suppositories,
 For this, put suppositories in a water bath for 30 minutes at 37℃.
Disintegration/dissolution test:
To check the dissolution rate of suppositories.
Put suppositories in dissolution/disintegration apparatus, then filled with suitable
dispersion medium at temp 37°C
Then check their time of dissolution.

 In this, we have to measured time in which suppository get completely liquify,
Softening/Liquefaction:-
PACKAGING
Suppositories are individually wrapped and then
filled in plastic, tin, and aluminum containers.

SUPPOSITORIES AND ITS TYPES, BASES, INCOMPATIBILITY

DEFINITION
 Pharmaceutical incompatibility is a condition that occurs when two or more mixed
and form substances are undesirable products, which may affect the safety,
efficacy, and appearance of the pharmaceutical preparation.
 It may occur during compounding, dispensing, formulation, manufacturing,
packaging, and administration of drugs.

 When two or more non-compatible substances are mixed, a physical change
takes place and an unacceptable product is formed.
 It may change the color, odor, taste, viscosity, and appearance of the product.
Examples:-This incompatibility occurred due to
 Immiscibility
CLASSIFICATION / TYPES
• It is divided into three types:-
 Physical incompatibility.
 Chemical incompatibility.
 Therapeutic incompatibility.
PHYSICAL INCOMPATIBILITY

 Insolubility
 Precipitation
 Liquefication
Immiscibility:-
In this oils and water are immiscible with each other. They can be made miscible with water
by emulsification.
E.g.
Rx
Castor Oil – 15 ml
water up to - 60 ml
Make the emulsion
In this, Caster oil is immiscible with water. To overcome this, an emulsifying agent is used.

Insolubility:-
Material cannot dissolve in a particular solvent system.
E.g.
In this, phenacetin is insoluble so tragacanth is used as a suspending agent to make a
stable suspension.
Rx
phenacetin - 3g
Caffeine - 1 g
orange syrup – 12 ml
water up to - 90 ml
Make a mixture/suspension

Rx
Tincture benzoin compound – 15 ml
Glyceride - 60 ml
Rose water q.s - 100 ml
Precipitation:-
In this, a drug in solution may be precipitated, if the solvent is added in which the drug is
insoluble.
E.g.
 Tincture benzoin compound contains resins and this resin is insoluble in water so it
can form a precipitate.
 The addition of tincture with rapid stirring prevents this.

Liquefication:-
When two or more low melting point solids are mixed, they form a soft mass or liquid
known as a “Eutectic mixture”
e.g.
Rx
Methanol - 3g
Camphor - 1 g
Ammonium chloride – 12 ml
light magnesium sulfate – 60 g
Make an insufflation
 On mixing, methanol, camphor, and ammonium chloride get liquefied due to a lowering
of melting point below room temperature.
 To prevent this, mix light magnesium sulphate.

CORRECTION
Change the order of mixing of ingredients of the prescription.
Emulsification
Addition of suspending agents
Change in the form of ingredients.
CHEMICAL INCOMPATIBILITY
 When two or more non-compatible substances or ingredients of prescription are mixed
together, a chemical change takes place and an inactive or toxic product may be formed.
 It may change the structure as well as the pharmacological properties of drugs.
 These changes may be immediate or may be after some time i.e. delayed incompatibility

TYPES OF CHEMICAL INCOMPATIBILITY:-
Chemical incompatibility can occur due to
1. Oxidation
2. Hydrolysis based on chemical changes
3. Polymerization
4. Isomerization
1. Oxidation
 It is the condition of the gain of oxygen and loss of electrons.
 It can decompose the complete solution/drug.
e.g. phenolic compounds, antibiotics, volatile, oils, etc.
 It can be prevented by using antioxidants, protecting from light, using buffers to maximum
pH

 It is the condition of the gain of oxygen and loss of electrons.
 It can decompose the complete solution/drug.
 It may be due to atmospheric oxygen light, temp, presence of pre-
oxidants, etc.
e.g. phenolic compounds, antibiotics, volatile oils, etc.
 It can be prevented using antioxidants protected from light and buffers to
maintain pH.
1. OXIDATION

 It is a condition or chemical reaction in which water reacts with a compound and
breaks its covalent bond and the breakdown of the compound, leads to its
decomposition.
e.g.
Codeine phosphate Codeine + Phosphate
 It may be due to the presence of water, (pH) and temperature increase.
 It can be prevented by
 protecting from moisture
 and water-absorbing substance
 Use appropriate solvent instead of water.
2. HYDROLYSIS

3. POLYMERISATION
 In this, a single unit of chemicals (monomers) bond together to form a long-chain
polymer.
e.g.
formaldehyde paraformaldehyde.
 It can be prevented by storing formaldehyde at a suitable temperature and adding 15%
methanol.
It can be caused due to temperature, light, solvent, impurities, etc.-
heat

4. ISOMERISATION
 In this, drugs convert into isomers. Isomers are identical in their formula but
different in their structure.
e.g.
l – adrenaline d-adrenaline due to change in temp or pH.
 It can be prevented by managing temp, pH, solvent, and impurities.
 It can further divide into two types:-
 Tolerated
 Adjusted

 In this, the chemical interaction can be minimized by changing the order of mixing or
mixing the solution in dilute form but no alteration is made in the formulation.
I . TOLERATED INCOMPATIBILITY:
 It may result from prescribing certain drugs to a patient to produce a specific degree of
pharmacological action. Still, the nature or intensity of the action produced is different
from that intended by the prescriber.
II. ADJUSTED INCOMPATIBILITY:
 In this, the chemical interaction can be prevented by addition or removal of the reacting
ingredients of a prescription.
THERAPEUTIC INCOMPATIBILITY:

This occurs due to the following reasons:-
1. Error in the dosage form
2. Wrong dosage form
3. Contraindicated drugs
4. Drug interactions etc…
1. Error in the dosage / overdose
It may result from an error in writing or interpreting the prescription order.
The most serious type of error is overdose, which can lead to poisoning.
Rx
Atropine Sulphate – 6mg
Phenobarbital - 360 mg
One capsule is to be taken three times in a day
 In this, the dose of Atropine sulphate and phenobarbital is 12 times daily.
 The prescription is referred back to the prescriber to correct the dose of drugs.

2. Wrong dosage form
Certain drugs have quite similar names. So, there is always a chance/ danger of dispensing the
wrong dose.
e.g. Digitoxin and Digoxin, Prednisone & Prednisonal.
 The prescription should be checked properly and it needs clarification then must clarify
from the prescriber.
3. Contra – indicated drugs
There are certain drugs that may be contraindicated in a particular disease or a particular
patient who is allergic to it.
e.g. Corticosteroids are contraindicated in peptic ulcer.
To prevent this must chek the patient history and allergic condition before prescribing drugs.

The effect of one drug is altered/changed by the simultaneous administration of another drug.
e.g.
4. Drug interactions
Rx
Tetracycline hydrochloride - 250 mg
take ten capsules
Direction – take with milk
 Tetracycline is inactivated by calcium, which is present in milk, so, it should not be taken
with milk.
 The prescription may be referred back to the physician to change the direction.
CORRECTION
 Dosing error/ overdose should be avoided.
 Drug provided in specific desired form.
 Avoid contraindicated drugs.
 Drugs with drug interaction should be avoided.

SUPPOSITORIES AND ITS TYPES, BASES, INCOMPATIBILITY

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