Ointments

By
Qusro Bin Hassan
B.Pharm, M.Pharm
Learning outcomes:
 Define ointment and classify different types of ointment bases.
 Explain different types of ointment bases.
 Properties of ointment bases.
 Characteristics of ointment bases.
 Selection of the appropriate base.
 Evaluation of ointments
 Requirement for ointments.
 Precutaneous Absorption.
 Factors influencing absorption through skin.
 Describe the different methods of preparation of ointments.
 Explain briefly about storage and containers of ointments.
 Labeling and advice for ointments during dispensing.
 Test requirements for ointments
 Official examples of ointments.
 Application of ointments.
Definition
 An ointment is a viscous, homogeneous, semisolid
preparation intended for externally as well as topically on a
variety of body surfaces. These include the skin and the
mucous membranes of the eye (an eye ointment), vagina, anus,
and nose. An ointment may or may not be medicated, and they
are easily spread.
 Ointments intended for application to large open wounds
should be sterile.
 They are used as emollients or for the application of active
ingredients to the skin for protective, therapeutic, or
prophylactic purposes.
 Types Of Ointments
1. Medicated - those with medicaments for
treatments of cutaneous (skin diseases).
 Examples: Sulfur Ointment, Zinc Oxide
Ointment and Compound Resorcinol

2. Non-medicated - also referred to as “ointment

bases” and use as such for their emollient or
lubricating effect or use as vehicles in medicated
ointments.
 Example: White Ointment
Classification of ointment bases
 The vehicle of an ointment is known as ointment base.
According to the USP, Ointment bases can be classified
according to composition and general characteristics. there are
different classes of ointment bases:
 Hydrocarbon Bases: e.g. soft paraffin, hard paraffin, and
liquid paraffin.
 Absorption bases: they fall into two classes:
 Non-emulsified Bases: e.g. Beeswax, Cholesterol, Wool Fat
 W/O emulsions Bases: e.g. Hydrous Wool Fat, cold cream
 O/W emulsions Bases: e.g. Polysorbate 80, Tween 80
 Water-soluble bases e.g. macrogols 200, 300, 400
 Water-miscible bases e.g. emulsifying wax, cetrimide
 Vegetable oils e.g. olive oil, arachis oil, coconut oil.
 Ointment bases
 Hydrocarbon (Oleaginous) Bases: This group
represents the most inert of chemical compounds.
Lipophilic vehicles easily spread on skin but reduces the
viscosity of ointments; sticky, not absorbed by skin,
immiscible with water, difficult to wash off the skin and
used as occlusive effect. E.g. paraffin ointment B.P.C
 Absorption Bases: Absorption bases which have the
property of absorbing several times their weight of water
but lesser amounts of alcoholic solutions, easily spread on
skin, absorbed by skin, less occlusive and good emollient
effect. However, absorption bases still possess the
undesirable property of greasiness, but they are more
readily removable from the skin than are oleaginous bases.
E.g. Wool alcohol ointment B.P.
Ointment bases
 Water-miscible Bases: They are hydrophilic in
nature, accept water or water-miscible liquids in their
external phase but thin out to a fluid lotion with the
addition of extra amount of water. E.g. Emulsifying
ointment B.P.
 Water-soluble Bases: They are soluble in water
as well as alcohol, accept a very limited amount of
water or alcohol without loss of viscosity of
ointments. This base have been developed from the
macrogels [poly ethylene glycols (PEG)]. They are
good absorption by skin; high water solubility so very
easily removed from the skin, and has good solvent
properties. E.g. Macrogol ointment B.P.C.
Vegetable oils
 These oils are used in ointments chiefly to
lower the melting point or soften bases of a
higher consistency and, also as an adjunct to
hydrocarbon bases to increase their emollient
effects and decrease their drying effects. These
oils can be used as ointment bases in them
when a high percentage of powder is
incorporated in a small amount of oil so that the
resulting consistency is quite viscous. Thus,
zinc oxide in castor oil is prepared occasionally.
Characteristics of ointment bases
 Affinity for skin, i.e. it should be miscible with both
aqueous and oily secretions of the skin and pH of the
skin.
 Stability.
 Smoothness.
 Non-irritating and non-sensitizing.
 Ability to absorb water and solutions of chemicals.
 Ability to release easily the incorporated
medicaments.
Selection of the appropriate base
 Desired release rate of drug substance.
 Desirability for topical or percutaneous
absorption.
 Stability of drug in ointment.
 Effect of drug on ointment base.
 Desire for easy removable.
 Properties which affect choice of
an ointment base are:

 Stability
 Penetrability
 Solvent property
 Irritant effects
 Ease of application and removal.
Evaluation of ointments
 Drug content
 Release of medicament from base
 Medicament penetration
 Consistency of the preparation
 Absorption of medicament into blood stream
 Irritant effect.
Requirement for ointments
 Microbial content: do not need to be sterile, but must
meet the FDA requirement of the test for absence of
bacteria such as S. areus and P. aeruginosa for
dermatological products.
 Minimum fill:
 Packaging, storage, labeling: (label should include the
type of base used)
 Additional standards: viscosity, in vitro release
 Percutaneous Absorption
 The skin offers greater
resistance to penetration by
drug substance than mucous
membrane because of high
amount of keratin in skin
than mucous membrane.
 Drugs may diffuse through
the skin by three different
routes:
Hair follicle region,
Sweat gland,
Stratum corneum.
Factors influencing absorption through skin

 Partition Co-efficient of drug: Drug with both water

and lipid solubility is favorable absorbed through the
skin.
 Moisture and temperature of skin: Humidity and
temperature shows influence on the absorption of
drug through skin. E.g. A ten times increase in
absorption of aspirin and glucosteroids, when the
environment temperature was raised from 10ºC to
37ºC and 50% humidity.
 Factors influencing absorption through skin

 Pathologic injury to skin: Injury to skin disrupt

stratum corneum, results in increased skin
permeability, increase blood vessels dilation may
result in increase in the absorption of drugs.
 Vehicle: Suitable vehicle can increase the drug
absorption through skin, drug that have a lower
solubility in vehicle are released more readily. The
pH of vehicle also can influence the rate of release of
drug. If drug is acidic, absorption is influenced when
the pH of vehicle is greater than Pka of drug and vice
versa.
Method of preparations
 Trituration method: This method is applicable
when the medicament is insoluble in the base or a
liquid present in small amount.
 This method used when one fatty base is soft or
medical agent are insoluble in fatty base. Use a
levigating agent to wet the powder and then
incorporate the wetted powder into ointment base.
 Levigating agents: Mineral oil for oily bases or
bases where oil are the external phase Glycerin for
bases where water is the external phase. Levigating
agent should be equal in volume to the solid material.
Method of preparations
 When liquid is added into an ointment, care must be
taken to consider the capacity of the ointment in
accepting the liquid. When it is necessary to add an
aqueous preparation to a hydrophobic base, the
solution should be added into minimal amount of the
hydrophilic base first. The mixture should be then
added into the hydrophobic base.
 Between 2 -4 g of ointment may be lost in
compounding process. The ointment is lost as it
adheres to beakers, slab, and spatula. Therefore make
an excess of ointment (add 10% excess to amount).
Method of preparations
 Trituration method: In this method, a finely-
subdivided insoluble medicaments (which is passed
through a 180µm sieve) are distributed by grinding
with a small amount of base or one of its ingredients,
followed by gradually increasing amounts of base.
 Trituration may be performed with either/:
a) Mortar and pestle made of porcelain with fairly
and smooth internal base and a flat head to the pestle.
b) An ointment tile/slabs/pads made of porcelain or
glass and stainless steel spatula, sometimes rubber or
plastic spatula are used.
Method of preparations
 Finely-Powders for incorporation by trituration are
placed in a mortar or on a ointment tile/slab and
gently mixed with base until the mixture is
homogenous and smooth.
 If, liquid ingredients present, before incorporate
liquid ingredients, a portion of base is placed on the
ointment tile/slab and a recess made to hold the
liquid.
 Finally, ointment is transfer to its container.
Trituration method
 Rx Sulphur Ointment B.P.C.
Send 50g sulphur ointment.
Master formula For 50g
Precipitated sulphur 100g 5g
Simple ointment 900g 45g
 Method of preparation: Sieve and weigh the precipitated
sulphur and place it on the slab. Weigh out the simple
ointment and place it on a different part of slab. Take a portion
of sulphur and portion of base of about three times the volume
of sulphur and mix them vigoursly until a homogenous and
smooth ointment is formed. Gradually add remaining sulphur
and base as same as before and collect the ointment together
on the slab using spatula and transfer to its container.
 Uses: used to treat acne and scabies.
Method of preparations
 Fusion Method: when an ointment base contains
several ingredients of melting points so melting the
base of highest melting point first and adding the
others in descending order of melting point.
 this method involves melting the ingredients together
and this process is carried out in an evaporating basin
on a water bath or hot plate (60-70ºC). Waxy solids
should be grated before weighing and should be
added first, so that melting will start. When all the
ingredients are melted, remove the basin from water
bath and gently stir until cold. Mixing, which should
be gentle to avoid air bubbles and lumps forming.
Method of preparations
 Any medicament may be added at different
stages of preparation depending on its
properties. If soluble and stable, it can be
added when the base is molten. If it is less
stable, or insoluble but easy to disperse, it can
be added during cooling.
Fusion Method
 Rx Simple Ointment B.P.C.
Send 50g simple ointment.
Master formula For 60g
Wool fat 50g 3g
Hard paraffin 50g 3g
Cetostearyl alcohol 50g 3g
Yellow/white soft paraffin 850g 51g
 Method of preparation: Grate the hard paraffin and
cetosterayl alcohol. Weigh 3g of each and place in an
evaporating basin on a water bath, weigh the wool fat, using a
piece of paper and add into basin, followed by the soft
paraffin, stir gently until fully melted. Remove from the heat
and continue to stir gently until cold and transfer to a suitable
container i.e. ointment jar or collapsible tube.
 Ointment mill
 If ointment is
preparing in large
quantity means, a
mixing device
(ointment mill) might
be used instead of
slab and spatula.
 Ointment mill
produce very smooth
and elegant
ointments.
 Electric Mortar and Pestle
 If ointment is preparing
in large quantity means,
a mixing device (electric
mortar and pestle) might
be used instead of slab
and spatula.
 This device allows the
formulation of ointment
and dispensing of
ointment in the same
container.
Storage and Containers for ointment
 Store in a cool place, but not allowed to freeze.
 Shelf life is 4 weeks
 Screw-capped amber glass
 Plastic pots (but…)
 Methyl salicylate incompatible with plastic
containers
 Collapsible metal tubes (but…)
 Tend to shed metal particles near their screw-
threads
Packaging
 Ointments are best packaged in suitable plastic
tubes or in syringes. The reason for this is that
there is minimal air space in the package and
the product is kept clean during the
administration process.
 Ointment jars, although widely used, expose
the preparation to air and microbial
contamination when opened
 Tubes May Be Filled By The
Following Steps
1.The prepared ointment is rolled into a cylinder shape of a piece of
parchment paper, the diameter is smaller than that of the tube.

2. With cap of the tube off to permit escape of air, the cylinder of
ointment with the paper is inserted into the open bottom of the tube

3. The piece of paper covering the ointments is grasped in one hand,

the other hand forces a heavy spatula down on the extreme end of
the tube, collapsing it and retaining the ointment while the paper is
slowly pulled from the tube. About one half (1/2) inch of the
bottom is then flattened with the spatula.

4. About 1/8 folds are made from the flattened end of the tube and
sealed by pliers or sealing clip on foot operated “crimper” machine.

Note: Ointments made by fusion may be poured directly into the tubes.
Stored at temperatures below 30oC to prevent softening.
labeling
 To be applied to the affected parts as directed.
 To be rubbed into the shoulder when required.
 To be rubbed into the affected area.
 To be rubbed gently into the affected area.
 To be applied to skin or mucous membrane as
instructed.
 TESTS REQUIREMENTS FOR
OINTMENTS
 Microbial Content
 Meet acceptable standard for microbial
 Must contain antimicrobial preservatives
 Preservatives: Methylparaben, propyl paraben,
phenols, benzoic acid, sorbic, quaternary
ammonium salts
 Example: Betamethasone Valerate Ointment –
must be absence of Staphylococcus aureus and
Pseudomonas aeriginosa
 TESTS REQUIREMENTS FOR
OINTMENTS
 Minimum Fill Test – net weight and volume
 Packaging, Storage, and Labeling – metal, plastic tubes, jar
 Well close containers, light sensitive, light resistant
 Labeling- type of base used (water soluble or insoluble)
 Additional Standards
 Examine the viscosity
 Vitro drug release to ensure within lot and lot-to-lot
uniformity
Official examples
 Salicylic Acid ointment B.P.
 Ichthammol ointment B.P.C.
 Calamine and Coal Tar ointment B.P.C.
 Zinc and Castor Oil ointment B.P.
 Methyl Salicylate ointment B.P.C.
Applications
 To protect skin or mucous membrane and to
permit rejuvenation of the tissue.
 To provide hydration of the skin or an
emollient effect.
 To provide a vehicle for applying a medication
either for local or systemic effect e.g. local-
topical antibiotic; systemic-nitroglycerin
ointment for angina.
 Sulphur ointment: To treat acne and scabies.
 Methyl salicylate ointment: As rubefacient.