UNIVERSITI KEBANGSAAN MALAYSIA
TITLE :
|
THE EFFECT OF DIFFERENT AMOUNT OF PEG ON THE
PHYSICAL CHARACTERISTICS OF SUPPOSITORY
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NAME :
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1.
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MOHD YADZLAN BIN YAHYA
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A148257
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2.
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MUHAMMAD NUR HAKIM BIN ZULKIFLI
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A147672
|
|
3.
|
PHYLICIA GAN YING HUI
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A147533
|
|
4.
5. |
ONG YEE WEI
SURUTHI A/P MOHHAN |
A147638
A147962 |
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LECTURER’S NAME
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:
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Prof. Madya Dr. HALIZA BINTI KATAS
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SEMESTER II, SESSION 2015-2016
FACULTY OF PHARMACY
1.0 Introduction
Suppositories
are solid dosage forms of various sizes, appearance and weights. Suppositories
are one of the rectal preparations. Some other examples of rectal preparations
may include foams and enemas. Suppositories are intended for administration by
rectal route where they melt, soften or dissolve to exert their effect. They
are capable of being easily inserted into the intended orifice without causing
undue distention.
The
suppository is usually composed of a medicament or drug incorporated in a
suppository base. The suppositories may be made up of either oil-soluble or
water-soluble base. The medicament may be intended for retention within the
cavity for localized drug effect or to be absorbed for the exertion of systemic
effect. For example, rectal localized action such as relief of constipation,
pain, itching and inflammation associated with hemorrhoid conditions.
Suppositories are indicated for systemic action in pediatric patients and in
patients who cannot take or tolerate oral medication due to variety of reasons
e.g. to relief nausea, vomiting and pain.
The
drug must be spread in a suitable base of suppository. Ideal suppository bases
should be easily formed by compression or molding; release any medicament
readily; melt at body temperature or dissolve or disperse in body fluids; keep
its shape when handled; compatible with the drugs, non-irritant and non-toxic.
Polyethylene glycol is an example of base that possesses desirable properties
to formulate a suppository. This is because they are non-irritating, chemically
stable, miscible with both water and mucous secretions, do not melt at body
temperature and at the same time able to provide sustained release of drug.
2.0 Objectives
1.
To
calibrate suppository moulds with PEG before preparing medicated suppositories.
2. To determine the effect of different compositions of PEG base on the physical characteristics of suppositories.
2. To determine the effect of different compositions of PEG base on the physical characteristics of suppositories.
3.0 Material and
metodology
3.1 Apparatus
Analytical balance
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1 x Suppository mould set
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Water bath at 37oC
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1 x Spatula
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Hotplate
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4 x Weighing
boats
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4 x 50 mL beaker
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2 x Glass rod
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1 x 5 mL pipette and pipette
bulb
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1 x 5 mL measuring cylinder
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3.2 Materials
Polyethylene glycol (PEG) 1000
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Distilled water
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Polyethylene glycol (PEG) 6000
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Liquid paraffin
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Paracetamol
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3.3 Methodology:
3.3.1 Calibration of Suppository Molds with PEG
Base
For
this calibration exercise, 10 g of the following proportions of PEG 1000 and
PEG 6000 were used.
Ingredients
|
Percentage
|
Weight
Basis
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PEG 1000
|
60%
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6 g
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PEG 6000
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40%
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4 g
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To calibrate
the mold with PEG suppository base:
- A clean and dry mold was taken. The mold was not lubricated. PEG 1000 was melt on a steam bath or hot plate, then, the heat was reduced and was mixed in the other PEG.
- The mixture was removed from the heat and
allowed to cool before pouring into the mold.
- The cavities in the mold were overfilled and
was let to stand at room temperature until solid.
- The excess were carefully removed with a hot
spatula; then the suppositories were removed from the mold.
- The suppositories were weighed and the total
weight were recorded. The average suppository weight was calculated.
Mold #
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6
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Total weight for 6 suppositories =
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6.1825 g
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Average weight for one
suppository =
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1.0304 g
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3.3.2 Preparation of paracetamol
suppositories
1. Saturated
stock solution of paracetamol was prepared by adding 1 g of paracetamol in 5
mL distilled water.
2. The
following paracetamol suppository (10 g) using the formulation below were
prepared :
Suppository
|
PEG
1000
(g)
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PEG
6000
(g)
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Paracetamol
stock solution (mL)
|
Total
(g)
|
I
|
9
|
0
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1
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10
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II
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6
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3
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1
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10
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III
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0
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9
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1
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10
|
3. One
type of PEG was melt on a hot plate, then, the heat was reduced and mixed in
the other PEG.
4. The
mixture was removed from the heat and allowed to cool before pouring into the
mold.
5. The
cavities were overfilled in the mold and was let to stand at room temperature
until solid.
6.
Excess were removed carefully with a hot spatula; then the suppositories were
removed from the mold.
7. The
shape, texture and color of the suppositories were observed.
8. Each
of the suppositories were inserted into a separate beaker containing distilled
water (10 mL and pre-warmed at 37oC) and then, the beaker was kept
into a water bath (37oC).
9. The time for
the suppositories to melt was recorded.
4.0 DISCUSSION:
1. Describe the importance of calibrating
suppository mould before preparing mediated suppository.
Suppository
moulds should be calibrated before preparing medicated suppository to ensure
accurate dosing of the suppository produced. This is because error due to the
slight differences among same type of moulds and among the cavities within a
mold often occur. As each individual mold is capable to hold a specific volume
in every openings, therefore calibration process of every suppository mould for
the usual base is important to prepare medicated suppositories with accurate
quantity of medicaments.
2. Compare the physical
appearance of suppositories that are formed and discuss.
Suppository
|
PEG 1000 (g)
|
PEG 6000 (g)
|
Shape
|
Hardness
|
Greasiness
|
Color
|
I
|
9
|
0
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Bullet
|
+
|
+++
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Clear white
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II
|
6
|
3
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Bullet
|
++
|
++
|
Intense White
|
III
|
0
|
9
|
Bullet
|
+++
|
+
|
Intense White
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Indicator:
+ Low
++ Medium
+++ High
All the
suppositories are bullet-shaped because bullet-shaped mould is used to prepare
the suppositories in this experiment. Different quantities of PEG 1000 and PEG
6000 will affect the physical characteristics of the suppositories such as in
the form of hardness, colour and greasiness. In this experiment, the quantities
of PEG 1000 decreases from suppository I to III while in the other hand, the
quantitiy of PEG 6000 is increasing from suppository I to III. Formulation with
the highest quantities of PEG 1000 take the longest time to solidify and
therefore suppository I with the highest quantity of PEG 1000 take the longest
time to be solidified in this experiment.. From suppositories I to III, the
quantites of PEG 1000 is decreasing while the quantity of PEG 6000 is
increasing. The hardness of the suppositories increases from I to III due to
the reason that increasing quantity of PEG 6000 will increase the number of
hydrogen bonds between the molecules which increase the hardness and strength
of the suppositories formed. Besides, PEG 6000 affect the greasiness of the
suppositories formed where the suppository with highest quantity of PEG 6000
appeared to be dry and less greasy.
Low
molecular weight polyethylene glycol causes suppository formed to be more transparent
and clear which is shown by the suppository I with greatest amount of PEG 1000
appeared to be the clearest suppository compared to suppository II and III.
This is because low amount of PEG 6000 will causes the suppository to have less
color intensity.
In a
nutshell, PEG 1000 will increase the greasiness of the suppository. The higher
the quantity of PEG 1000 in a formulation, the greasier the suppository. In the
other hand, PEG 6000 will increase the hardness of the suppository. The greater
the quantity of PEG 6000 in a formulation, the harder the suppository. As for
suppository III, it has the highest quantity of PEG 6000 and the lowest
quantity of PEG 1000, therefore suppository III is the hardest and the least
greasy suppository among the suppositories produced in this experiment. The
suppositories produced are in white colour because the active ingredient which
is paracetamol used in this experiment is white in colour. The intensity of the
colour of suppository depends on the quantity of PEG 1000 found in the
formulation. The higher the quantity of PEG 1000, the more transparent it is.
Suppository I appeared to be in clear white because it has the highest quantity
of PEG 1000.
3. Plot a graph of time required
to melt the suppository against the amount of PEG 6000 in the formulation. Compare and explain
the result.
The time
required to melt the suppository against the amount of PEG 6000 in the formulation for the suppository I
was 44.36 minutes, Suppository II was 42.44 minutes while Suppository III is
35.14 minutes. Based on the result, the Suppository I with zero gram of PEG
6000 required longer time to melt while Suppository III with 9 grams of PEG
6000 has shortest time to melt down. This shows that the higher the amount of
PEG in the formulation of the suppository the shorter the time to melt down
compared to the one with non-added PEG 6000 formulation. This is because the
larger the molecular weight of the PEG, the harder the PEG is. That is why the
Molecular weight affecting the time required for the suppository to melt down.
4. Describe the function(s) of
each ingredient used in the suppository formulation.
Paracetamol
or Acetaminophen is one of drugs that have both antipyretic and analgesic
properties. Analgesic is defined as an agent that relieves or reduces the
sensation of pain by elevating the pain without disturbing consciousness. The
antipyretic can be used as a drug that is responsible for lowering temperature
of a feverish organism but has no effect on normal temperature states.
The Poly
Ethylene Glycol or PEG is used in mixture of PEG to give satisfactory hardness
and dissolution time of suppository and also act as an excipient which is
lubricant for the suppository formulation. It also acts as a base for some
cosmetic and suppository.
5.0 Conclusion
Calibration
of suppository moulds with PEG before preparing medicated suppository is
important in order to ensure accurate dosing of the suppository produced.
Besides that, the different amount of combination of PEG 1000 and PEG 6000 in
the suppository preparation affects the physical characteristics of
suppositories such as the hardness, greasiness texture, shape of the
suppository.
6.0 References
