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SUPPOSITORIES
Laboratory experiment
Fatty bases
Cocoabutter Advantages: It satisfies the requirements for an ideal base – innocuous, bland, and non-reactive, and melts at
(theobroma body temp
oil)
Disadvantages: Polymorphism, Adherence to mould, Low softening point, Melting point reduction,
Deterioration during storage, Poor water absorbing capacity and Leakage from the body.
Synthetic fats Advantages: Their solidifying points are unaffected by over heating. They have good resistance to oxidation
because their unsaturated fatty acids have been reduced. The difference between melting and setting points is
small; generally only 1.5 to 2C˚ and seldom over 3C˚. They set quickly, the risk of sedimentation is low and
they are easier to administer. The melting point depression caused by fat soluble drugs can be counteracted by
choosing a high melting point grade, while the hardness and brittleness that sometimes results from a high
content of insoluble powder can be prevented by using a low melting point grade. W/o emulsifying agents, No
mould lubricant is needed because they contract significantly on cooling, have very attractive, clean and
polished appearance.
Disadvantages: They should not be cooled in a refrigerator or ice because they become brittle if cooled
quickly. Additives such as polysorbate 80 correct this fault. They are more fluid than theobroma oil when
melted and at this stage sedimentation is greater. Thickeners such as magnesium stearate, bentonite reduce
this problem.
proprietary Whitepsol (formerly called Imhausen), Massa Estarinum and Massuppol.
synthetic
bases/ Advantages: No polymorphism, Tolerance of oxidation, Rapid Solidify, Do not need mould lubricant, Mix
Emulsifying with physiological fluid easily, non-irritant, withstand overheating and can absorbs large amount of aqueous
bases liquids.
Disadvantages: Should not be cooled in refrigerator or on ice, Become brittle if cooled quickly, They may
have dehydrating effect and problems with API sedimentation due to low viscosity on melting and more
expensive.
Water soluble or water miscible bases
glycero- Advantages: dissolves in body secretions and therefore is preferable to a fatty base for administering
gelatin antiseptics. Since, solution is slow; drug release is more prolonged than from fatty base. At present, the B.P
allows a maximum disintegration time of 1 hr. for Glycerol Suppositories B.P made with gelatine of B.P
standard.
Disadvantages: They have a physiological action (used as laxative) They are more difficult to prepare and
handle. Their solution time depends on the content and quality and gelatin and the age of the base. They are
hygroscopic. So a careful storage is required. It also leads to dehydration of the rectal mucosa with consequent
irritation; this is an advantage where a laxative effect is required. Gelatin is incompatible with protein
precipitants such as tannic acid.
macrogols Advantages: The mixtures have melting point above 42C˚, cool storage is not required, they are satisfactory
(PEG) for use in hot climates, and administration is easy because they are not slippery to handle. Do not melt in the
body but gradually dissolve and disperse, freeing their medication slowly and providing longer action than
fatty bases. Their physical properties can be varied by suitable admixture of high and low polymers. High
polymers give hard products that disintegrate and release their drug slowly. Softer, less brittle preparations
that disperse and liberate their drug more quickly are obtained by mixing high with either medium or medium
and low polymers or by adding plasticizers.
They do not stick to the mould since they contract on cooling. Because of their high molecular weight solution
of high viscosity are produced when they disperse in the body. They absorb water well and have excellent
solvent properties. Products have clean smooth appearance
Disadvantages: They are hygroscopic so careful storage is required. Irritancy can be reduced by
incorporating about 20% of water in the mass or by instructing the patient to dip the preparation in water just
before insertion. This type of base is suitable for systemically active drugs. Its good solvent properties can
result in retention of the drug in the liquefied base in the body with consequent reduction in therapeutic
activity. Products sometimes fracture on storage, particularly if they contain High solubility of macrogols
which can lead to a super saturated solution in the water and subsequent crystallisation and this the mass
granular and brittle. Crystal growth of certain medicaments may occur particularly if they are partly in
solution and partly in suspension in the base. This makes the product brittle and crystals may be irritating
because they are large and takes longer time to dissolve. They are incompatible with bismuth salts, tannins
and phenol. They lower the activity of some antibacterial agents and dissolve certain plastics necessitating
care in choosing containers.
PEGs
Theoretical weight =
20g-----------------------------------------------------------------------------------Weight of empty
beaker = 73.7 g. ------------------------------------------------------------------------Weight of one
SUPP base without API (1.7g.) ---------------------------------------------------------Weight of tow
SUPP base without API (3.70g)-------------------------------------------------------Determine the
amount of base required:-------------------------------------------------------------Weight of base
required = (theoretical weight – weight of base displaced)*base %
Questions
Q2- Describe the effect of different bases on the physical characteristic of the
suppositories?
Two important factors when preparing suppositories with cocoa butter base.
This base must not be heated above 35°C (95°F) because cocoa butter is a
polymorphic compound and if overheated will convert to a metastable structure that
melts in the 25° to 30°C (77° to 86°F) range. Thus, the finished suppositories would
melt at room temperature and not be usable.
The change in melting point caused by adding certain drugs to cocoa butter
suppositories. For example, chloral hydrate and phenol tend to lower the melting
point. It may be necessary to add spermaceti or beeswax to raise the melting point of
finished suppositories back to the desired range.
Suppositories I II III
PEG 6000 0 3 9
amount (g)
Shape
Bullet
Bullet Bullet
Translucent
Colour Off-White Clear white
white
Hardness + ++ +++
Table 3. A study of the effect of different amount of PEG6000 on the physical characteristics
of suppositories.