Suppository

Ms. Nisha Kalayil
Assistant Professor
Department of Pharmaceutics
SJIPR
MS. NISHA KALAYIL-Pharmaceutics I PCI
1

1. Definitions, Advantages & Disadvantages
2. Ideal properties & Types of suppositories
3. Types of Suppository bases
4. Method of preparation
5. Displacement value & its calculation
6. Evaluation of Suppositories (QC tests)
MS. NISHA KALAYIL-Pharmaceutics I PCI 2

1. Solid dosage forms of medicament for insertion into body cavities other than
mouth.
- The medicament is incorporated into the suppository base and the product is
formulated such as way that it melt/dissolve at body temperature in the body
cavity fluids to release the medicament.
- Emollients, astringents, antibacterial agents, hormones, steroids and local
anaesthetics are dispensed in suppository forms for treating local conditions of
vagina, rectum and urethra.
2. Advantages: Disadvantages:
- Can be easily administered - Irritant drugs cannot be administered
- Produces local effect - Causes embarrassment
- Promotes bowel evacuation - To be stored at low temperature
- Gives sustained action

IDEAL PROPERTIES:
Should melt at body temperature
Should release medicament readily
Should keep its shape
Should be non-toxic and non-irritant
Should stable on storage
Should be compatible with different formulation method
Should be stable if heated above its melting point
Should be easily moulded and should not adhere to the
mould

TYPES OF SUPPOSITORIES:
1. Rectal
2. Vaginal
3. Nasal Suppositories
4. Urethral
5. Earcones
NEW TRENDS:
1. Tablet suppositories
2. Layered suppositories
3. Capsule suppositories
4. Coated suppositories
5. Disposable moulds
2
5
3.Frankincense Oil Suppository
1
3
2

FACTORS AFFECTING THE RECTAL DRUG ABSORPTION:
1. Physiologic Factors
- Drugs absorbed by anorectal area and retain therapeutic action/values.
- Lower hemorrhoidal veins (50-70% drug absorption)
- Lymphatic circulation, pH.
2. Physiochemical characteristics of the drug
- Compatibility between drug and the excipients & suppository bases.
3. Physiochemical characteristics of the base & adjuvants
- Properties of suppository bases affect drug absorption.
4. Blood levels from different dosage forms.

FATTY
BASES
• Theobroma Oil
• Emulsified
Theobroma Oil
• Hydrogenated
Oils
WATER
SOLUBLE/
WATER
IMMISCIBLE
BASES
• Glycero- gelatin
• Soap glycerine
• Polyethylene
glycols
(macrogols)
EMULSIFYING
BASES
• Witepsol
• Massa Estarinum
• Massupol
Helps to retain its
shape and
firmness during
administration &
storage.

Theobroma oil
 A yellowish white solid
obtained from crushed
seeds of theobroma
cocoa.
 Also known as cocoa
butter.
 Mixture of glyceryl esters
of stearic, oleic, palmitic
and other fatty acids.
 Considered most suitable
for rectal suppositories.
 Disadvantage : shows
polymorphism, rancid and
melts in warm whether,
leaks from body cavity,
relatively costly.
Emulsified theobroma
oil
 The use of 5%
glyceryl
monostearate, 10%
lenette wax, 2-3%
cetyl alcohol, 4%
beeswax & 12%
spermaceti is
recomended for the
preparation of
emulsified
theobroma oil.
Hydrogentaed oils
 Obtained by
hydrogenation of
vegetable oils such as
arachis oil, cotton seed
oil, coconut etc.
 Substitute for theobroma
oil.
 Advantages: resistant to
oxidation, lubrication of
mould is not required,
colorless odorless and
elegant suppositories.
 Disadvantages: brittle on
rapid cooling, more fluid
compared to butter like
theobroma oil.

Glycero-gelatin base
 A mixture of glycerin
and water which is made
stiff by the addition of
gelatin.
 Making pessaries.
 Translucent
suppositories which
tends to dissolve or
disperse slowly in the
body cavity
 2 types: Pharmagel A
(Used for weakly acidic
drugs) & Pharmagel B
(Used for weakly
alkaline drugs)
 Disadvantages: glycerin
incompatible with many
drugs, microbial
contamination risk.
Soap-glycerin
suppositories
 The gelatin is
replaced with either
curd soap / sodium
stearate which
makes the base
sufficiently hard to
prepare good quality
suppositories.
 Disadvantages: very
hygroscopic
Polyethylene glycols
 Commonly known as
macrogols/polyglycol
s/carbowaxes.
 Advantages:
chemically stable,
non irritant, do not
allow baterial
growth.
 Disadvantages:
hygroscopic high
solubility leads to
supersaturation.

Witepsol
 Consists of
triglycerids of
saturated vegetable
acid with varying %
of partial esters.
 Suppositories
prepared should not
be cooled rapidly, in
order to prevent
them from
brittleness.
Massa estarinum
 Mixture of di &
trigylcerides of
saturated fatty
acids.
 also known as Adeps
solidus.
 White, brittle,
odorless and
tasteless.
 Garde B commonly
used in dispensing.
Massupol
 Consists of glyceryl
esters mainly of lauric
acid to which small
amount of glyceryl
monostearate has
been added to
improve water
absorbing capacity.
 Advantages: solidifies
rapidly, no irritant.
 disadvantages: not to
be colled rapidly, not
very viscous on
melting.

Improtant to determine
incompatibilities.
Indicates the
temperature at which it
melts
surface feel and the
hardness of the bases
time required for
solidifying the base when
chilled

FORMULATION OF
SUPPOSITORIES:
1. Rolling method/Hand
Moulding
2. Hot process/Fusion
method/Pour Moulding
3. Cold Compression
Moulding

 Simplest & oldest method
 Involves rolling well blended
suppository base into desired
shape.
 Practical & economic for small
number of suppositories.
 Disadvantages ??????
 Advantages???????

 Commonly used method on both
large scale and small scale.
 1st base is melted on water bath
and then the API is incorporated.
 The mass is finally poured into the
cooled metal moulds.
 Points to remember: pre-
lubricatoion, scraping off.

FORMULATION CCONSIDERATIONS:
1. Suppositories for local effect
2. Suppositories for systemic effect
3. Water in suppositories
4. Hygroscopicity
5. Incompatibilities
6. Viscosity
7. Brittleness
8. Density
9. Volume contraction
10. Lubricants or mould release agents
11. Dosage replacement factor
12. Weight and volume control
13. Rancidity and antioxidants

PACKAGING
 Suppositories must be packed so that
each suppositories are overwrapped
or placed in a container in such a
manner that they do not touch each
other.
 In Package Moulding: plastic /
aluminium foil
STORAGE &
TYPICAL STABILITY PROBLEMS
 Storage conditions and temperatures
 Stability problems include bloom fat
suppositories hardens, pinholes in
foil.

1. Melting Range Test
2. Softening Time
3. Breaking Test
4. Dissolution / Disintegration Time
Quality control (QC) is a procedure
or set of procedures intended to
ensure that a manufactured product or
performed service adheres to a
defined set of quality criteria or
meets the requirements of the client
or customer.

 Test is also called the macromelting range test.
 Measure of time it takes for the entire suppository to melt when immersed in a
constant temperature (37°C) water bath.
 In capillary tubes for the fat base only.

 Liquefaction/Softening Time
 Consists of a U-tube partially submersed in
constant temperature water bath. A constriction
on one side holds the suppository in place in the
tube.
 A glass rod is placed on top of he suppositories
and the time for the rod to pass through the
constriction is recorded as “softening time”.
 This can be carried out in 35.5 to 37°C.

 Method to measure the friability or brittleness of
the suppositories.
 The apparatus consists of double-wall chamber in
which the test suppositories are placed. Water at
37°C is pumped through the double walls. A rod 2
disc, on disc consists of suppository to be tested
and the other disc consists of weights to be add.
 The weight at which the suppository collapses is
the breaking point or the force that determines
the friability or brittlenesss.

1. MOULD CALIBRATION: Necessary to find the actual mould capacity. Done by making suppositories
of plain base and then weighing the suppositories produced.
Calibration weight (y) = Total wt of suppositories
No. of suppositories
2. DISPLACEMENT VALUES AND INCORPORATION OF DRUG: Displacement value (DV) is defined as ‘the
number of parts by weight of drug which displaces 1 part by weight of base’
To calculate the quantity of base required, a simple equation is used:
Amount of base = (N * y) – N*D / DV
N – the number of suppositories made
y – the mould calibration
D – the weight of drug in one suppository
DV – Displacement Value

ΔProblems??????
1. A batch of six suppositories, of 1g nominal
weight, are produced and found to weigh
6.36g. What is the calibration weight?
Calibration weight (y) = Total wt of suppositories
No. of suppositories
6.36/6 = 1.06g
∆ Calculate the mould calibration
for a batch of plain suppositories.
a) 6 suppositories which weigh
5.88gm.
b) 8 suppositories which weigh
8.16gm
c) 6 suppositories which weigh
12.30gm
d) 6 suppositories which weigh
23.93gm
e) 12 suppositories which weigh
24.48gm

ΩProblems??????
1. Calculate the quantities of drug
required to prepare 6 suppositories
weighing 1gm each containing
250mg of Bismuth subgallate (DV =
2.7, mould calibration=0.94gm)
As excess of 2 is required, therefore
calculate for 8 suppositories
N = 8
y = 0.94gm
D = 250mg = 0.25gm
DV = 2.7
Using the equation
Amount of base = (N * y) – N*D / DV
= (8 x 0.94) - (8 x 0.25)/2.7
= 6.78gm
To complete the quantities for preparing the
suppositories,
Bismuth subgallate = 8 x 0.25gm = 2.00gm
Suppository base = 6.78gm

ΩProblems??????
Ω Calculate the quantity of base required to make the following batch of
suppositories:
a) 8 x 1gm suppostitories each containing 100mg of aspirin (DV = 1.1)
b) 6 x 1gm suppostitories each containing 100mg of aspirin (DV = 1.5)
c) 6 x 4gm suppostitories each containing 100mg of aspirin (DV = 1.3)
d) 6 x 2gm suppostitories each containing 100mg of aspirin (DV = 1.5)
e) 10 x 4gm suppostitories each containing 500mg of aspirin (DV = 1.3)

• The DV can be determined for any drug by comparing the weights of plain
suppositories with those conataining a known concentration of the drug.
• To calculate the DV for the drug it is neccesary to prepare two batches of
suppositories, one plain and the other containning a known percentage of the drug.

§Problems??????
1. A batch of 6 plain suppositories was
prepared and found to weigh 6.3gm.
Then a batch of 6 suppositories
containing 20% drug was prepared
and found weigh 7.5gm.
In a medicated suppositories, the weight
of the base is 80% of the total weight
wt. of base = 80 x 7.5 / 100 = 6.0gm
In a medicated suppositories, the weight
of the drug is 20% of the total weight
wt. of drug = 20 x 7.5 / 100 = 1.5gm
Therefore the weight of the base
displaced by the drug = 6.3 - 6.0 = 0.3gm
If 0.3gm of base is displaced by 1.5gm of
the base, then 1gm of drug will be
displaced by:
Amount of base displaced = 1.5/0.3 = 5
5 is the displacement value of the drug

§Problems??????
§ During the determination of the DV of a new drug the following informaation was
obrtained. what is the DV ?
a) A batch of 12 plain suppositories weigheed 12.6gm and a similar batch containing
10% drug weighed 13.1gm.
b) A batch of six 1gm plain suppositories weigheed 6.28gm and a similar batch
containing 15% drug weighed 6.42gm.
c) A batch of six 4gm plain suppositories weigheed 23.76gm and a similar batch
d) A batch of six 1g plain suppositories weigheed 5.94gm and a similar batch

1. TB of Pharmaceutics II by R.M Mehta
2. TB of Industrial Pharmacy by
Lacchman & Liebermann
3. Calculations for Pharmaceutical
Practice by Arthur Winfield.

Suppository

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