3. Stability of the drug in the ointment base.
4. Effect of the drug on the consistency of the ointment base.
5. The desire for a base that is easily removed by washing with water.
6. Characteristics of the skin surface to which it is applied.
Preparation of ointments
Ointments are prepared by two general methods:
1. Incorporation
2. Fusion
The method used depends primarily on the nature of the ingredients.
Incorporation
By the incorporation method, the components are mixed until a uniform
preparation is attained, on a small scale the pharmacist may mix the
components using a mortar and pestle or a spatula and slab (a glass or
porcelain plate).
Incorporation of solids
When preparing an ointment by spatulation, the pharmacist works the
ointment with a stainless steel spatula having a long, broad blade. If the
components of an ointment are reactive with the metal of the spatula (e.g.
as in the case of phenol), hard rubber spatula may be used.
The ointment base is placed on one side and the powdered components
previously reduced to fine powders on the other side. A small portion of the
powder is mixed with a portion of the base until uniform mixture is
obtained. The process is continued until all portions of the powder and the
base are combined and thoroughly and uniformly blended.
It is often desirable to reduce the particle size of a powder or crystalline
material before incorporation into the ointment base, so that the final
product will not be gritty. This may be done by levigation process (i.e. mixing
the solid material in a vehicle to make a smooth dispersion).
The levigating agent used should be physically and chemically compatible
with the drug and base.
The levigating agent for example is mineral oil for oleaginous bases or the
bases where oils are the external phase and glycerine for bases where water
is the external phase.
The amount of levigating agent used should be about equal in volume to the
solid material. A mortar and pestle is used for levigation, this allows both
reduction of particle size and the dispersion of the substance in the vehicle.
After levigation, the dispersion is incorporated into the ointment base by
spatulation or with the mortar and pestle until the product is uniform.
Incorporation of liquids
Liquid substances or solutions of drugs are added to an ointment according
to ointment base’s capacity to accept the volume required. For example,
only very small amounts of an aqueous solution may be incorporated into an
oleaginous ointment, whereas hydrophilic ointment bases readily accept
aqueous solutions.
When it is necessary to add an aqueous preparation to a hydrophobic base,
the solution first may be incorporated into a minimum amount of a
hydrophilic base and then that mixture added to the hydrophobic base.
However, all bases even if hydrophilic have their limit to retain liquids
beyond which they become too soft or semiliquid. Alcoholic solutions of
small volume may be added well to oleaginous vehicles or emulsion bases.
- On large scale, roller mills force ointments through stainless steel rollers to
produce ointments that are uniform in composition and smooth in texture.
Fusion
By the fusion method, all or some of the components of an ointment are
combined by being melted together and cooled with constant stirring until
congealed. Components not melted are added to the congealing mixture as
it is being cooled and stirred.
Naturally, heat-labile substances and any volatile components are added last
when the temperature of the mixture is low enough not to cause
decomposition or volatilization of the components.
Substances may be added to the congealing mixture as solutions or as
insoluble powders levigated with a portion of the base. On a small scale, the
fusion process may be conducted in a porcelain dish or glass container.
Medicated ointments and ointment bases containing components as bees
wax, paraffin, stearyl alcohol and high molecular weight PEG which do not
lend themselves well to mixture by incorporation are prepared by fusion.
In the preparation of ointments having an emulsion base, the method of
manufacture involves both a melting and an emulsification process.
The water-immiscible components such as the oil and waxes are melted
together in a steam bath to about 70-75 °C, and an aqueous solution of the
heat-stable water soluble components is prepared and heated to the same
temperature as the oleaginous components, then the aqueous solution is
slowly added with mechanical stirring to the melted oleaginous mixture. The
temperature is maintained for 5-10 minutes and the mixture is slowly cooled
with the stirring continued until congealed.
If the aqueous solution were not the same temperature as the oleaginous
melt, there would be solidification of some of the waxes upon the addition
of the colder aqueous solution to the melted mixture.
