Ointments

• Ointments are semisolid dosage forms intended for

external application to the skin or mucous membranes
• Medicated ointments are used for the effect of the
therapeutic agents they contain
• Un-medicated ones are used for their physical effects as
protectants, lubricants and emollients
• Ointment bases may be used for their physical effects or
as vehicles for medicated ointments
 According to the penetrability ointments are
classified as:

1) Epidermic ointments:
- Having very slight power of penetration into the skin
- Indicated specially when therapeutic action is required
on the diseased epithelium
- Bases used in this group are petrolatum, waxes and
their combinations

- Example: Ketoconazole ointment

2) Endodermic ointments:
- possess some power of penetration into the deeper
layers of the skin
- this group contains softer bases that liquefy at body
temperature like, vegetable oils, lard, lanolin,
anhydrous lanolin or combination of these
- Example: Demodex ointment

3) Diadermic ointments:
- these penetrate the skin and offer a better opportunity
for absorption of the medicament
- ointments of emulsion type and the water soluble
bases belong to this group
- Example: Nitroglycerine ointment
 Ointment bases

According to the USP ointment bases are classified into

four general groups:

a) Oleaginous bases
b) Absorption bases
c) Water-removable bases
d) Water-soluble bases
 Oleaginous bases

Properties:
- These are hydrocarbon bases
- On application to the skin give emollient effect, protect
against the escape of moisture
- Effective as occlusive dressings
- Can remain on the skin for long time without drying out
- Because of their immiscibility with water, difficult to wash
off
- Water and aqueous preparations may be incorporated in
small amount and with some difficulty
 Examples of Oleaginous bases

Petrolatum:
- a purified mixture of semisolid hydrocarbons obtained
from petroleum
- color varies from yellowish to light amber
- may be used alone or in combination of with other agents
as an ointment base
- also known as yellow petroleum and petroleum jelly
- a commercial product is Vaseline
White petrolatum:

- a purified mixture of semisolid hydrocarbons obtained

from petroleum that has been wholly or nearly
decolorized
- because of its lighter color, considered more esthetically
pleasing by some pharmacists and patients
- also known as white petroleum jelly
- a commercial product is White Vaseline
Yellow ointment:
- a combination of yellow wax and petrolatum
- also called simple ointment
- It has a slightly greater viscosity than plain petrolatum

White ointment:
- a combination of white wax ( bleached and purified yellow
wax) and petrolatum
 Absorption bases

Properties:
- these bases may be used as emollients
- not easily removed from the skin with water washing,
since the external phase of the emulsion is oleaginous
- useful as pharmaceutical adjuncts to incorporate small
volumes of aqueous solutions into hydrocarbon bases
- this is done by incorporating the aqueous solution into
the absorption base and then incorporating this mixture
into the hydrocarbon base
 Absorption bases

Absorption bases are of two types:

a) Those that permit the incorporation of aqueous
solutions resulting in the formation of w/o emulsions
( e.g., hydrophilic petrolatum)
b) Those that are w/o emulsions ( emulsion bases) that
permit the incorporation of additional quantities of
aqueous solutions (e.g.,lanolin)
Hydrophilic petrolatum
Formula for the preparation of 1000g Hydrophilic
petrolatum, USP is-
Cholesterol-30g
Stearyl alcohol- 30g
White wax- 80g
White petrolatum- 869g
Lanolin
- obtained from the wool of sheep, a purified waxlike
substance that has been cleaned, deodorized and
decolorized
- water content not more than 0.25%
 Water-removable bases

Properties:
- these are o/w emulsions resembling creams
- as the external phase is aqueous, easily washed from
skin
- they may be diluted with water or aqueous solutions
- they can absorb serous discharges
- an example of this type of base is Hydrophilic ointment
 Formulation of Hydrophilic ointment

• Hydrophilic ointments are prepared by combining the

following ingredients:
Methyl paraben
Propyl paraben
Sodium lauryl sulfate
Propylene glycol
Stearyl alcohol
White petrolatum
Purified water
 Water-soluble bases

Properties:
- do not contain oleaginous components
- completely water–washable and greaseless
- as they soften greatly with the addition of water,they are
mostly used for incorporation of solid substances
- example of this type is Polyethylene glycol ointment
 Polyethylene glycol ointment
Properties:
- a polymer of ethylene oxide
- PEGs having average molecular weight below 600 are
clear, colorless liquids
- those with MW above 1000 are waxlike white materials
- those with MW in between are semisolids
- the greater the MW, the greater the viscosity
- PEG ointment is prepared by combining PEG 3350 and
PEG 400 which results in a very pliable semisolid
ointment
 Selection of the appropriate base

Selection the base to use in the formulation of an ointment

depends on careful assessment of a number of factors,
including the following:

- Desired release rate of the drug substance from the ointment base
- Desirability of topical or percutaneous drug absorption
- Desirability of occlusion of moisture from the skin
- Stability of the drug in the ointment base
- Effect, if any, of the drug on the consistency or other features of the
ointment base
- Desire for a base that is easily removed by washing with water
- Characteristics of the surface to which it is applied
Ointments
 Preparation of ointments

• Since ointments are applied primarily to irritated areas, it

is an unbreakable rule that these preparations must not
contain granular or gritty particles which might cause
further irritation
• Regardless of the skin condition, ointments must be
smooth and free from granular or gritty particles
• In compounding ointments, the following rules should be
observed:
1) Insoluble substances to be incorporated in ointment
bases should always be in the impalpable powder form
 Preparation…

2) Insoluble substances are best incorporated when first

levigated with a small portion of the base to form a
smooth nucleus and then incorporated into the
remainder of the base
3) Water-soluble salts should be incorporated by
dissolving them in a small amount of water and
incorporating with the base, using anhydrous lanolin, if
necessary, to absorb the aqueous solution. This method
produces a smooth ointment with a minimum of
levigation
 Preparation..

When substances incorporated into ointment bases must

be reduced to a fine state of subdivision. Three methods
are generally available:
1) Use of an ointment slab and spatula
2) Use of the mortar and pestle
3) Use of an ointment mill
These methods may or may not involve fusion, depending
on the nature of the medicament to be incorporated into the
base and the base itself
 Use of an ointment slab…
• A stainless-steel spatula with a long, broad, flexible
blade is essential to the preparation of good ointments
• Two spatulas usually are used, one to levigate the
ointment, the other to remove accumulating ointment
from the levigating spatula
• Where danger of chemical reaction between the steel
spatula and active ingredients ( e.g. iodine, mercury
salts, salicylic acid) is a possibility, a hard rubber spatula
or wodden tongue depressor should be used
Use of an ointment
slab and spatula

• The usual technique consists of rubbing the powder with

a small amount of base until it is thoroughly distributed in
a finely subdivided state
• Then this concentrated ointment is incorporated into the
remainder of the base
• Mineral oil or a vegetable oil can be used as a levigating
agent if small quantities of medicaments are to be
incorporated in the base
• The use of large amounts of levigating agents may result
in undue softening of the finished ointment
Use of the mortar and pestle

• When large quantities of liquid are to be incorporated

into a base or when exceptionally large quantities of
ointment are to be made, then mortar and pestle should
be used
• 5 minutes of actual rubbing time was necessary to
produce homogeneity in products
• The use of mortar and pestle is considered not as
efficient as the spatula in reducing the size of the
particles incorporated in
• The particles have a tendency to ‘ride’ out from under the
pestle and the grinding effect is limited
 Use of an ointment mill

• The ointment mill is convenient and ideal for making

ointments in lots of 5 lbs. or more, although small mills
are available for use in the community pharmacy
• Small mills are available with stainless steal rollers or the
more chemically resistant clay rollers
• The ointment is prepared in the usual manner and then
run through the mill until smooth and free from gritty
particles
 ointment mill…
• When making ointments on a larger scale, the powdered
medicaments are shifted into the softened or melted
base
• The mixture is stirred until it has congealed and then it is
run through an ointment mill until smooth
• In some instances, the powdered medicament is mixed
with a small portion of the base to make a concentrate
which is run through an ointment mill several times
• Then the concentrate is mixed with the remainder of the
base in a change can mixer
 Fusion

Fusion is necessary when-

- waxes, paraffins, fatty alcohols, fatty acids or any
hard waxlike materials are included in the formula
- a medicament is soluble in the melted base
- most emulsion and absorption bases are prepared by
fusion
 Fusion..
• In preparing ointments by fusion, the substance having
the highest melting point is placed in an evaporating dish
or beaker on a water bath and melted at the lowest
temperature possible
• Other substances are added in order of decreasing
melting points
• In this way, the entire base is not heated to the highest
temperature
• Medicaments soluble in the melted base should be
added to the base just before it congeals
 Packaging of ointments

Topical dermatologic products are packaged in either jars

or tubes
Ointment jars:
- made of clear or opaque glass or plastic. Some are
colored- green, amber or blue
- opaque jars are used for light sensitive products
- commercially available empty ointments jars vary in size
from about 0.5ounce to 1 pound
 Tubes in packaging ointments are gaining
popularity over jars

• They are light in weight

• Relatively inexpensive
• Convenient for use
• Compatible with most formulative components
• Provide greater protection against external
contamination and environmental conditions
 Ointment tubes:

• Made up of aluminum or plastic

• Ointment to be used for different purposes are packaged
with special applicator tips
• Tubes of aluminum generally are coated with an epoxy
resin, vinyl or lacquer to eliminate any interactions
between the contents and the tube
• Plastic tubes are made of high or low-density
polyethylene or a blend of each, polypropylene,
polyethylene terephthalate and various plastic, foil or
paper laminates, sometimes 10 layers thick
 Plastic tube offers special features and
advantages

• Low-density polyethylene is soft and resilient and

provides a good moisture barrier
• High-density polyethylene provides a superior moisture
barrier but it is less resilient
• Polypropylene has a high level of heat resistance
• Polyethylene terephthalate offers transparency and a
high degree of product chemical compatibility
 Filling ointment jars

• On a small scale, the ointments jars are filled carefully by

transferring the weighed amount of ointments with a spatula
• The ointment is packed on the bottom and along the sides of the jar,
avoiding entrapment of air
• The jar size should allow the ointment to reach near the top of the
jar but not so high as to touch the lid when closed
• Ointments prepared by fusion may be poured directly into the
ointment jar to congeal in it
• In large scale manufacture of ointments, pressure fillers force the
specified amount of ointment into the jars
• Electric mortars and pestles can be used to prepare an ointment in
the dispensing container
 Filling ointment tubes

• Tubes are filled from the open back end of

the tube, opposite from the cap end
• Ointments prepared by fusion may be poured while still
soft but viscous directly into the tubes with caution to
prevent stratification of the components
• The filled tubes are closed and sealed
• Manual filling of an ointment tube requires a number of
steps:
- the prepared ointment, placed on waxed or parchment
paper and rolled into a cylindrical shape, is inserted into
the open end of the tube and pushed forward as far as
allowed
 Filling ointment tubes…
- With a spatula pressing against the lower portion of the
tube and making a crease below the ointment fill, the
paper is slowly removed, leaving the ointment in the tube
- the bottom of the tube is flattened, folded and sealed
with a crimping tool or clip
Industrially , automatic filling, closing, crimping and
labeling machines are used for large scale tube
packaging of semisolid pharmaceuticals
- plastic and laminate tubes are closed and sealed by
heat and crimping
- metal tubes are sealed by folding and crimping with or
without a vinyl, latex or lacquer sealant