IPPP-II (Supp)
IPPP-II (Supp)
IPPP-II (Supp)
Dereje K (PhD)
Pharmaceutics course team
School of Pharmacy, Jimma University,
Jimma, Ethiopia
Suppositories are solid dosage forms intended for insertion into body
orifices other than mouth where they
melt, soften, or
dissolve and liberate the therapeutic agent to produce local or
systemic effects.
Purpose of Pessaries??
is about 15 to 20 cm long.
Blood from the upper haemorrhoidal vein enters the portal vein,
which flows into the liver, where drug metabolism occurs.
1. lipid-water solubility
The more drug the base contains, the more drug will be available for
absorption.
2. Particle size
Effect on dissolution of the particles
The rate of dissolution of the drug is inversely proportional to the
particle size of the dispersed active agent.
Notes
If the base interacts with the drug to inhibit its release, drug
absorption will be impaired or even prevented.
At room temperature, it is a
yellowish-white solid,
chocolate-like odour.
Chemically, it is a triglyceride
Excellent emollient
Rancidity on storage
Due to the oxidation of unsaturated glycerides
triglycerides from palm, palm kernel, and coconut oils with self-
emulsifying glyceryl monostearate and polyoxyl stearate)
Advantages
hydroxyl number
A high number
the base is less hydrophobic
its power to absorb water is high, leads to hydrolysis
affect drug release and subsequent absorption
Melting point
the selected base should melt to facilitate drug release and hence
absorption
If the active agent is soluble in the base, this will lead to a reduction
in the melting point of the base
The dispersion of solid drug particles into the molten base will
dramatically affect the viscosity of the product
2. Polyethylene glycols.
The ratio of glycerol, gelatin and water can affect the dispersion
time and thus the duration of action.
A higher proportion of gelatin in the mixture makes it more rigid and longer
acting.
Limitation of Glycerol–gelatin
Notes
Advantage of PEG
No laxative effect
Less microbial contamination
The base contract on cooling and easily removed
Melting point above body temperature (Cool storage is not so critical,
Suitable for hot climates)
The base dissolve in the body and disperse the medication slowly
Produce high-viscosity solutions, so leakage is less likely.
Good solvent properties
Suppositories and Pessaries
Polyethylene glycols (PEGs)..
Limitations
Hygroscopic
Thus may cause irritation to the mucosa
.The good solvent properties may result in retention of the drug
Incompatibilities:
with several drugs and packaging materials, e.g. benzocaine,
penicillin and plastic
Brittleness: if cooled too quickly and also on storage
Examples:
E.g. beeswax (white or yellow wax), cetyl esters wax, stearic acid
Emulsifying agents
Increase the water absorbing capacity of fatty bases.
Preservatives
used in suppository contains water soluble bases.
Thickening agents
prevent sedimentation of suspended in solid bases
Plasticizers
Improve flexibility of suppository and decrease brittle (macrogol)
E.g castor oil, Glycerine, glycol
Molds in common use today are made from stainless steel, aluminum,
brass, or plastic.
For example, for glycerogelatin base, liquid paraffin or arachis oil may
be used as the lubricant.
Similarly, any added medicinal agent alters the density of the base,
and the weight of the resulting suppository differs from that of those
prepared with base material alone.
2. After removal from the mold, the suppositories are weighed and the
total weight and average weight of each suppository are recorded
4. The volume of the melt is determined for the total number as well as
for the average of one suppository
Three methods are used to calculate the quantities of base that the
active medication will occupy and the quantities of ingredients
required.
100(𝑊−𝐴)
𝑓= +1
(𝐴)(𝑌)
Where
f is the dosage replacement factor
W is the weight of the pure base suppositories
A is the weight of suppositories with Y% of the active ingredient
Example 1
1. Determine the average blank weight, A, per mold, using the suppository
base of interest.
4. Melt the suppository base, incorporate the medication, mix, pour into mold,
cool, trim, and remove from the mold.
7. Take the weight of the medication required for each supppository and divide
it by the density factor of the medication to find the replacement value of the
suppository base.
10. Multiply the weight of drug per suppository by the number of suppositories
required to obtain the quantity of active drug required for the prescription.
DENSITY FACTOR METHOD
Example
1. Determine the average weight per mold (blank) using the suppository
base of interest.
3. Divide the density of the active drug by the density of the suppository
base to obtain a ratio.
4. Divide the total weight of active drug required for the total number of
suppositories by the ratio obtained in step 3 (this will give the amount
of suppository base displaced by the active drug).
5.
Suppositories and Pessaries
OCCUPIED VOLUME METHOD
5. Subtract the amount obtained in step 4 from the total weight of the
prescription (number of suppositories multiplied by the weight of the
blanks) to obtain the weight of suppository base required.
Example
The required weight of the base is 19.4 g, and the weight of the active drug is 2 g.
(a) Below 0°C (b) Between 5 and 10°C (c) Room temperature