Ointments

Definition:

These are semisolid preparations of drugs, either dispersed or dissolved

in a suitable base, meant for application to the skin or mucous
membranes.

ADVANTAGES
 Handling of ointments is easier than bulky liquid dosage forms.
 They are chemically more stable than liquid dosage forms.
 They facilitate application of the directly to the effected body part and
avoid exposure of other parts to the drug.
 They are suitable for patients who find it difficult to take the drugs by
parenteral and oral routes.
 They prolong the contact time between the drug and effected area.
 The bioavailability of drugs administered as ointments is more since it
prevents passage through liver.

DISADVANTAGES
 They are bulkier than solid dosage forms.
 When applications of an exact quantity of ointment to the affected area
is required, it is difficult to ascertain the same.
 They are less stable than solid dosage forms.

The various types of ointments are

I. Medicated ointments
II. Unmedicated ointments

MEDICATED OINTMENTS
These ointments contain drugs which show local or systemic effects.
These are of several sub-types
 Dermatologic ointments
 Opthalmic ointments
 Rectal ointments
 Vaginal ointments
 Nasal ointments

DERMATOLOGIC OINTMENTS
These ointments are applied topically on the external skin. The ointment
is applied to the affected area as a thin layer and spread evenly using
gentle pressure with the fingertips.
These are of three types

(1) Epidermic ointments: The drugs present in these type of ointments

exert their action on the epidermis of the skin.
Example: Ketoconazole ointment.

(2) Endodermic ointments: The drugs present in these types of

ointments exert their action on the deeper layers of cutaneous tissue.
Example: Demodex ointment.

(3) Diadermic ointments: The drugs present in these types of ointments

enter into the deeper layers of skin and finally in the systemic circulation
and exert systemic effects.
Example: Nitroglycerine ointment.

OPTHALMIC OINTMENTS
These are sterile preparations which are applied inside the lower eye lid.
Only anhydrous bases are used in their preparation. The ointment is
applied as a narrow band of approximately 0.25 - 0.5 inch.
Example: Sulfacetamide sodium ointment.

RECTAL OINTMENTS
These are the ointments to be applied to the perianal or within the anal
canal. The bases used are combinations of PEG 300 and PEG 3350, cetyl
alcohol and cetyl esters, wax, liquid paraffin and white paraffin.
Example: Benzocaine ointment.

VAGINAL OINTMENTS
These ointments are applied to the vulvovaginal area or inside the
vagina. As vagina is more susceptible to infections, the ointment should
be free from micro-organisms, moulds and yeasts.
Example: Candicidin ointment.

NASAL OINTMENTS
These are used in the topical treatment of nasal mucosa. Drugs get
absorbed into the general circulation through the rich blood supply of
the nasal lining.
Example: Ipratropium bromide ointment.

UNMEDICATED OINTMENTS
 These ointments donot contain any drugs. They are useful as emollients,
protectants or lubricants.
Example: Petroleum jelly.

CLASSIFICATION OF OINTMENT BASES

Four different classes of bases are available
 Hydrocarbon or oleaginous bases
 Absorbent bases
 Emulsion bases / Water washable bases
 Water-soluble bases

HYDROCARBON BASES: These are semisolid hydrocarbons

obtained from petroleum.
Examples: Hard paraffin, yellow soft paraffin, white soft petroleum and
gelled oleaginous vehicle.

ABSORBENT BASES: These are hydrophilic mixtures

of hydrocarbons and substances with polar groups. Substances like
cholesterol, lanolin, lanosterol etc., may be used in the formation of
absorption bases.
Examples: Hydrophilic petrolatum, hydrous wool fat and oily cream.

EMULSION BASES: These are miscible with water and contain oil-in-
water emulgents. They can be easily removed from the skin. They
contain surfactants which serve the purpose of emulgents.
Based on the nature of surfactant present, emulsion bases are of three
types.
(a) Anionic emulsion bases: contains anionic surfactants like sodium
lauryl sulphate.
Examples: Hydrophilic ointment and emulsifying ointment.
(b) Cationic emulsion bases: contains cationic surfactants like cetrimide.
Example: Cetrimide emulsifying ointment.
(c) Non-ionic emulsion bases: contains nonionic surfactants like
cetomacrogols.
Examples: Cetomacrogol emulsifying wax.

WATER - SOLUBLE BASES: They donot contain oily ingredients and

are called greaseless bases. They are completely soluble in water.
Examples: Polyethylene glycols (PEGs), polyoxyl 40 stearate, and
polysorbates.

Common types of topical formulations:

1. Cream

 emulsion of water and oil

 classified as oil in water (o/w) or water in oil (w/o) emulsions
 o/w creams (e.g. vanishing creams) spread easily and do not
leave the skin greasy and sticky
 w/o creams (e.g. cold cream) are more greasy and more
emollient
 creams contain emulsifiers and preservatives which may cause
contact allergy

2. Ointment

 semi-solid preparations of hydrocarbons (petrolatum, mineral

oil, paraffins, synthetic hydrocarbons)
 strong emollient effect makes it useful in dry skin conditions
 occlusive effect enhances penetration of active drug and
improves efficacy (especially in thickened, lichenified skin)
 provides a protective film on the skin (e.g., useful in
housewife’s hands, irritant dermatitis)
 greasy, sticky, retains sweat (therefore, not suitable in wet
weepy dermatitis, hairy areas, skin prone to folliculitis, or hot
weather conditions)
 contains no water and does not require a preservative

3. Paste

 mixture of powder and ointment (e.g., zinc oxide 20% paste)

 addition of powder improves porosity (breathability). For
example, when treating diaper rash, a protective ointment base
which also allows breathability of the skin is desired.
 addition of powder to change an ointment into a paste also
increases the consistency of the preparation so that it is more
difficult to rub off. This property is useful when one does not
want an irritating preparation to get onto the normal skin (e.g.,
anthralin paste for treating psoriasis).

4. Lotion

 a loosely used term that nowadays includes any liquid

preparation in which inert or active medications are suspended
or dissolved
 an o/w emulsion with a high water content to give the
preparation a liquid consistency can be considered a lotion
  most lotions are aqueous or hydroalcoholic systems; small
amounts of alcohol are added to aid solubilization of the active
ingredient(s) and to hasten evaporation of the solvent from the
skin surface
 most acne lotions are hydroalcoholic which evaporate fast; they
are non-sticky and drying
 emulsion type lotions are usually not drying, depending on the
water content (higher water and/or less oil is more drying)
 lotions are easy to apply to large areas
 lotions are suitable for hairy areas, skin prone to
folliculitis/acne, intertriginous areas

5. Gel

 transparent preparations containing cellulose ethers or

carbromer in water or a water-alcohol mixture
 gels liquify on contact with the skin, dry and leave a thin film of
active medication
 gels tend to be drying
 they are useful in hairy areas
 they are cosmetically acceptable

Factors to consider when choosing a topical preparation:

1. Always consider the effect of the vehicle. An occlusive vehicle

enhances penetration of the active ingredient and improves
efficacy. The vehicle itself may have a cooling, drying,
emollient, or protective action. It can also cause side effects by
being excessively drying or occlusive.
2. Match the type of preparation with the type of lesions. For
example, avoid greasy ointments for acute weepy dermatitis.
3. Match the type of preparation with the site (e.g., gel or lotion for
hairy areas).
4. Consider irritation or sensitization potential. Generally,
ointments and w/o creams are less irritating, while gels are
irritating. Ointments do not contain preservatives or emulsifiers
if allergy to these agents is a concern.

The different methods of evaluation of ointments are

(1) Physical methods
 Test of rate of absorption
 Test of non-irritancy
 Test of rate of penetration
 Test of rate of drug release
 Test of rheological properties
 Test of content uniformity
(2) Microbiological methods
 Test of microbial content
 Test of preservative efficacy
PHYSICAL METHODS
TEST OF RATE OF ABSORPTION
Diadermic ointments are those from which the drug
moves into deeper skin tissues and finally into the systemic
circulation. Such ointments should be evaluated for the rate of
absorption of drugs. The ointment should be applied over a definite
area of the skin by rubbing. At regular intervals of time, serum and
urine samples should be analysed for the quantity of drug absorbed. The
rate of absorption i.e., the amount of drug absorbed per unit time
should be more.
TEST OF NON-IRRITANCY
The bases used in the formulation of ointments may
cause irritation or allergic reactions. Non-irritancy of the
preparation is evaluated by patch test. In this test 24 human
volunteers are selected. Definite quantity of ointment is applied under
occlusion daily on the back or volar forearm for 21 days. Daily the
type of pharmacological action observed is noted. No visible reaction
or erythema or intense erythema with edema and vesicular erosion should
occur. A good ointment base shows no visible reaction.
TEST OF RATE OF PENETRATION
The rate of penetration of a semisolid dosage form
is crucial in the onset and duration of action of the drug. Weighed
quantity of the preparation should be applied over selected area of the
skin for a definite period of time. Then the preparation left over is
collected and weighed. The difference between the initial and the final
weights of the preparation gives the amount of preparation penetrated
through the skin and this when divided by the area and time period of
application gives the rate of penetration of the preparation. The test
should be repeated twice or thrice. This procedure is tedious and not
followed anymore.
Using flow-through diffusion cell or microdialysis
method, the rate of penetration of the preparation can be estimated.
Animal or human skin of definite area should be collected and tied to
the holder present in a diffusion cell. The diffusion cell is placed in
a fluid bath. Measured quantity of the preparation is applied over the
skin and the amount of drug passed into the fluid is measured at
regular intervals by analyzing the aliquots of fluid using a
spectrophotometer.
TEST OF RATE OF DRUG RELEASE
A clean test tube is taken and the internal surface
is coated with the preparation as a thin layer. Saline or serum is
poured into the test tube. After a certain period of time, the saline
is analyzed for the quantity of the drug. The amount of drug when
divided by the time period gives the rate of drug release.
TEST OF RHEOLOGICAL PROPERTIES
The viscosity of the preparation should be such
that the product can be easily removed from the container and easily
applied to the skin. Using cone and plate viscometer the viscosity of
the preparation is determined.
TEST OF CONTENT UNIFORMITY
The net weight of contents of ten filled ointment
containers is determined. The results should match each other and with
the labelled quantity. This test is also called minimum fill test.
MICROBIOLOGICAL METHODS
TEST OF MICROBIAL CONTENT
Micro-organisms like pseudomonas aeruginosa and
staphylococcus aureus may contaminate the preparation and finally
infect the skin. So ointments should be tested for the absence of such
micro-organisms.
Solutions of different samples of the preparation
are made. Each sample is inoculated into separate volumes of 0.5 ml of
rabbit's plasma under aseptic conditions and incubated at 37 degrees C
for 1-4 hours. No formation of the clot in the incubated mass indicates
the absence of the micro-organisms.
TEST OF PRESERVATIVE EFFICACY
Using pour plate technique the number of
micro-organisms initially present in the preparation are determined.
Solutions of different samples of the preparation are made and mixed
with Tryptone Azolectin (TAT) broth separately. All cultures of the
micro-organisms are added into each mixture, under aseptic conditions.
All mixtures are incubated. The number of micro-organisms in each
sample are counted on 7th, 14th, 21st and 28th days of inoculation.
MICROBIAL LIMITS
On 14th day, the number of vegetative cells should not be more than 0.1% of initial
concentration.
On 28th day, the number of organisms should be below or equal to initial
concentration.