Suppositories
May Saab
Associate Professor
Pharmaceutical Technology Department
Faculty of Pharmacy, BAU
Suppositories
➢ Suppositories are solid dosage forms inserted rectally or
vaginally to melt or dissolve and exert a systemic or local
effect.
➢ Suppository bases include:
• Fatty bases (cocoa butter, suppocire, witepsol) release drug at room Temp
• Water soluble (PEG, Glycerogelatin) slowly release drog intravag
macrogol
➢ Suppository Adjuvants:
• Preservatives benzalconium chloride, sodium benzoate,parabens
• Antioxidants mainly for cocoa buter due to unsaturated FA ex:topoferol (vit E) butylated hydroxyanisol
Butylated Hydroxy toluene
• Viscosity imparting agents to prevent sedementation and uneven distibution
• Plasticizers to improve flex and avoid brittleness
• Surfactants inhance the dispersability of certain companent in fattybas and their dissolution/realse into
rectal fluids especially with a fatty base with low hydroxile number ex:cocoa butter
Specific Problems in Suppositories
➢ Hygroscopicity: can cause irretation to the rectum or vagaina so before insertion dip in water first
• PEG and glycerogelatin suppositories must be stored under controlled
hygroscopic during their inviromental humidity they will absorb water whic will affect their
humidity outer appearance
➢ Incompatibility:
• PEG incompatibility with certain drugs.
incompatible with plastic mold (PVC) ad aspirin
wgich will lead to transacetylation
➢ Viscosity:
• In the manufacture of suppositories made with low-viscosity bases,
extra care must be exercised to avoid the sedimentation of suspended
particles
• Use narrow melting range suppository bases, adding fatty acids or fatty
alcohols, or adding 2% aluminum monostearate of suppositories.
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Specific Problems in Suppositories
➢ Brittleness same thing for PEG
• Brittleness of Synthetic fats are often induced by rapid chilling. plastecizers
are needed
• The temperature differential between melted base and mold should be
as small as possible.
• Addition of a small amount of Tween 80, fatty acid monoglycerides,
castor oil, or propylene glycol imparts plasticity and renders it less
brittle. Glycerol
➢ Rancidity:
• Rancidity results from the autoxidation and subsequent decomposition
of unsaturated fats.
• Measures by the iodine number
• Add antioxidants
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Specific Problems in Suppositories
➢ Blooming: T: well storage + surfactants (to improve dispertion and stop migration)
• During storage, dullness on the surface. faty base with lower point + change in temp/humidity
->melt and migrate through suppository and crystalise
on the surface and affect drug and crystallise into white
➢ Hardening: poly morphism
spots
• During storage, fatty base suppositories become harder due to
crystallization, hence affecting melting of the suppositories and drug
absorption rate
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Suppository Manufacturing
for heat labide drug but has bad appearence and not accepted by patient due to astetic
➢ Compression molding obsolete depend on grading the sppos base and reduce size and mix
with semi solid ingredient plus drug into a low consistency mold
in fatty base suppo should be grated plus mixed with lanoline for consistency
➢ Pour molding: +drug->molded
PEG graded +water+glycerol+disperse drug into mixture->compression molde
• Stainless steel molds
• In-Package molding
it is more prefered where it is marketed withing its plastic liner so any fluctuation of TEMP/melting/resolidification
wont lead to change in their shape
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Mass Preparation
➢ Weighing the components
➢ Melting at 60° C in a stainless steel container with a
steam jacket
➢ Container equipped with an agitator (anchor, propeller,
for viscous for low to medium viscocity
or turbine)for improvement its homogenous dispertion of melted mass
and enven distibution of Temp within the mass
mass
➢ Drugs and additives are dispersed or solubilized in the
molten base.
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In Package Molding
made of poly vinyl chloride or aluminium
➢ Can make 12,000-20,000
suppositories per hour
➢ Previously thermoformed
plastic or aluminum strips or
immediately thermoformed
strips
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In Package Molding
➢ For in process thermoformed mold,
two vertical set rolls of aluminum
foil or plastic films are used.
➢ Both films are connected to form
bowl-like halves and heat sealed
➢ The tops of the molds are left open
for filling of the molten suppository
mass
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In Package Molding
➢ The filled molds are then
transferred in upright position
to a cooling tunnel
➢ Finally hermetically sealed and
cut for final packaging.
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Manufacturing
Quality Control Test
➢ Appearance
➢ Uniformity of mixing cut longitudinaly to see the distribution and mixing
➢ Uniformity of weight 20 suppo randomly chosed weight each and make average +/-5%
2 are exepcted outside the range but none should exeede the double
➢ Melting point using a chamber water jacketed at 37 C and behind it white and balck background Using a stopwa
required to melt the suppository
mass
➢ Breaking test
➢ Softening time penetrometer
➢ Disintegration test
➢ Dissolution test
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