CHAPTER 10

OINTMENTS, CREAMS, AND GELS

Bungcasan
Kadile
Montecalvo
Salve
 W H AT A R E
Ointments, Creams, and Gels
Semisolid dosage forms intended for topical application.

Therapeutically, they may be applied to the skin, placed on the surface of the eye, or
used nasally, vaginally, or rectally.

The unmedicated ones are as protectants or lubricants.

Used for both local and systemic effects.

 W H AT A R E
Ointments, Creams, and Gels
IMPORTANT DISTINCTION

Topical dermatological product

• Deliver drug into the skin in treating dermal disorders, with the skin as the target organ.

Transdermal product
• Deliver drugs through the skin (percutaneous absorption) to the general circulation for
systemic effects, with the skin not being the target organ.
OINTMENTS
 May be medicated or
OINTMENTS
not. Semisolid
preparations
 Ointment bases may intended for external
be used for their application to the
physical effects or as skin or mucous
vehicles for medicated membranes.
ointments.
 Ointments
Ointment Bases

OLEAGINOUS ABSORPTION WATER- WATER-

BASES BASES REMOVABLE SOLUBLE
BASES BASES
 Ointments
Ointment Bases

OLEAGINOUS ABSORPTION WATER- WATER-

BASES BASES REMOVABLE SOLUBLE
BASES BASES
 Ointments
Ointment Bases

Also termed as hydrocarbon bases.

Have an emollient effect, protect against the escape of moisture,

OLEAGINOUS are effective as occlusive dressings, can remain on the skin for
BASES long periods without drying out, and because of their immiscibility
with water, are difficult to wash off.

Petrolatum, white petrolatum, white ointment, and yellow ointment

are examples of hydrocarbon ointment bases.

Liquid petrolatum (mineral oil)

• May be used as levigating agent when powdered substances
are incorporated in hydrocarbon bases.
 Ointments
Ointment Bases

PETROLATUM, USP Purified mixture of semisolid hydrocarbons obtained

from petroleum.

OLEAGINOUS Yellowish to light amber.

BASES
AKA yellow petrolatum and petroleum jelly (e.g.
Vaseline).

WHITE Purified mixture from petroleum that has been wholly

PETROLATUM, USP
or nearly decolorized.

Same purpose with petrolatum but more

aesthetically pleasing.

AKA white petroleum jelly (e.g. White Vaseline).

 Ointments
Ointment Bases
YELLOW
OINTMENT, USP
Contains 50 g of yellow wax and 950 g of petrolatum.

Yellow wax is the purified wax obtained from the

OLEAGINOUS honeycomb of the bee Apis mellifera.
BASES
AKA simple ointment, it has a slightly greater
viscosity than plain petrolatum.

WHITE OINTMENT,
USP

Differs from yellow ointment by substitution of white

wax (bleached and purified yellow wax) and white
petrolatum in the formula.
 Ointments
Ointment Bases

OLEAGINOUS ABSORPTION WATER- WATER-

BASES BASES REMOVABLE SOLUBLE
BASES BASES
 Ointments
Ointment Bases

Two types of Absorption Bases:

(a) Permit the incorporation of aqueous solutions resulting in the
formation of water-in-oil (W/O) emulsions (e.g., hydrophilic
petrolatum)
ABSORPTION
(b) W/O emulsions (syn: emulsion bases) that permit the
BASES
incorporation of additional quantities of aqueous solutions
(e.g., lanolin).

Used as emollients, but do not provide the degree of occlusion

afforded by the oleaginous bases.

Incorporate small volumes of aqueous solutions into hydrocarbon

bases by incorporating the aqueous solution into the absorption
base and then incorporating this mixture into the hydrocarbon
base.
 Ointments
Ointment Bases
HYDROPHILIC
PETROLATUM, USP

1000 g of this contains 30g cholesterol, 30g stearyl

ABSORPTION alcohol, 80g white wax & 860 g white petrolatum.
BASES

LANOLIN, USP AKA (Anhydrous lanolin), it is obtained from the wool

of sheep (Ovis aries).

A purified waxlike substance that has been cleaned,

deodorized, and decolorized

Contains not more than 0.25% water.

 Ointments
Ointment Bases

MODIFIED
LANOLIN, USP
ABSORPTION
BASES
Lanolin processed to reduce the contents of free
lanolin alcohols and any detergent and pesticide
residues.
 Ointments
Ointment Bases

OLEAGINOUS ABSORPTION WATER- WATER-

BASES BASES REMOVABLE SOLUBLE
BASES BASES
 Ointments
Ointment Bases

Oil-in-water emulsions commonly

WATER-
REMOVABLE called creams.
BASES

External phase is aqueous, so are

easily washed from skin and are
often called water-washable bases.
 Ointments
Ointment Bases

HYDROPHILIC
OINTMENT, USP
WATER-
REMOVABLE
BASES

Sodium lauryl sulfate → Emulsifying agent

Stearyl Alcohol and White Petrolatum → Constitutes
the oleaginous phase
Methylparaben and Propylparaben → Antimicrobial
preservatives.
 Ointments
Ointment Bases

OLEAGINOUS ABSORPTION WATER- WATER-

BASES BASES REMOVABLE SOLUBLE
BASES BASES
 Ointments
Ointment Bases

Do not contain oleaginous

components.
WATER-
SOLUBLE
BASES
Completely water washable and
often referred to as greaseless.

Mostly used for incorporation of

solid substances.
 Ointments
Ointment Bases

POLYETHYLENE
H(OCH2CH2)nOH
GLYCOL
OINTMENT, NF Polymer of ethylene oxide and water.
WATER-
SOLUBLE < 600 MW: Clear, colorless liquids
BASES > 1,000 MW: Waxlike white materials
MW in between 600 and 1000: Semisolids

The greater the molecular weight, the greater the

viscosity.

Viscosity of PEGs range from average molecular

weight of 200 to 8,000.
 Ointments
Ointment Bases
Selection of the Appropriate Base

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 easily removed by washing
with water
Characteristics of the surface to which it is
applied
 Ointments
Ointment Bases
Selection of the Appropriate Base

EXAMPLES:

Dry, scaly skin: Ointment

Weeping or oozing surfaces: Cream

Intertriginous areas or where friction

may occur (Between the thighs or
under the armpit): Lotion
 Ointments
Preparation of Ointments

INCORPORATION FUSION
 Ointments
Preparation of Ointments

INCORPORATION
 Ointments
Preparation of Ointments

INCORPORATION
Components are mixed until a Ointment mill
uniform preparation is attained.
Electronic mortar and pestle
On a small scale, as in
extemporaneous compounding, the “Unguator”
pharmacist may mix the components
using a mortar and pestle, or a
spatula may be used to rub the
ingredients together on an ointment
slab (a large glass or porcelain plate
or pill tile).
 Ointments
Preparation of Ointments

“Unguator”

A device which allows a

pharmacist to place the
ingredients in a plastic
ointment jar with a special
lid that allows for a mixing
blade to be used to mix
the ingredients in the
dispensing container.
 Ointments
Preparation of Ointments

INCORPORATION
Solids
It is desirable to reduce the particle size of a powder or crystalline material
before incorporation into the ointment base so the final product will not be gritty.

This may be done by levigating, or mixing the solid material in a vehicle in

which it is insoluble to make a smooth dispersion.

Levigating agents: (should be compatible with drug and base)

Mineral oil (for bases in which oils are the external phase)
Glycerin (for bases in which water is the external phase)
 Ointments
Preparation of Ointments

INCORPORATION
Liquids

Liquid substances or solutions of drugs are added to an ointment only after due
consideration of an ointment base's capacity to accept the volume required.

Only very small amounts of an aqueous solution may be incorporated into

an oleaginous ointment, whereas hydrophilic ointment bases readily accept
aqueous solutions.
 Ointments
Preparation of Ointments

Ointment or roller mills

Used to force coarsely
formed ointments through
stainless steel or ceramic
rollers to produce
ointments uniform in
composition and smooth in
texture.
 Ointments
Preparation of Ointments

FUSION
 Ointments
Preparation of Ointments

FUSION METHOD
All or some of the components of an Once congealed, the ointment may
ointment are combined by being be passed through an ointment mill
melted together and cooled with (in large-scale manufacture) or
constant stirring until congealed. rubbed with a spatula or in a mortar
to ensure a uniform texture.
On a small scale, fusion may be
conducted in a porcelain dish or
glass beaker.

On a large scale, it is carried out in

large steam-jacketed kettles.
 Ointments
Compendial Requirements

Microbial Content

Minimum Fill

Packaging, Storage, and Labeling

 Ointments
Compendial Requirements

MICROBIAL CONTENT
Topical applications are not required Antimicrobial Preservatives: inhibit
to be sterile (except ophthalmic microbial growth
preparations).
• Methylparaben
Preparations that contain water tend • Propylparaben
to support microbial growth to a • Phenols
greater extent than water-free • Benzoic acid
preparations. • Sorbic acid
• Quaternary ammonium salts
 Ointments
Compendial Requirements

MINIMUM FILL

Minimum fill test

→ Determination of the net weight or volume of the
contents of filled containers to ensure proper contents
compared with the labeled amount.
 Ointments
Compendial Requirements

PACKAGING, STORAGE, AND LABELING

Large-mouth ointment jars

Metal or plastic tubes

Opaque or light-resistant containers (for light-sensitive preparations)

Must be stored in well-closed containers to protect against contamination and in

a cool place to protect against product separation in heat.

USP directs the labeling for certain ointments and creams including proper
storage conditions, dosing and administration.
 Ointments
Compendial Requirements

ADDITIONAL STANDARDS

Test for viscosity and for in vitro drug release to ensure within-lot
and lot-to-lot uniformity.

In vitro drug release tests include diffusion cell studies to

determine the drug's release profile from the semisolid product.
CREAMS
 CREAMS
 Primary application: Semisolid preparations
for skin and mucous
containing one or more
membranes, such as
rectally and vaginally.
medicinal agents
dissolved or dispersed in
either a water-in-oil (W/O)
 Preferred by patients
emulsion or an oil-inwater
and physicians
(O/W) emulsion or in
because they are
easier to spread and another type of water-
remove. washable base.
 Have a relatively soft,
spreadable consistency CREAMS
Semisolid preparations
 Cold cream (W/O containing one or more
cream) medicinal agents
 Hydrophilic ointment dissolved or dispersed in
(O/W cream) either a water-in-oil (W/O)
emulsion or an oil-inwater
 Water-washable (O/W) emulsion or in
formulation is generally another type of water-
inferred when term washable base.
“cream is used.
 Creams
Preparation of Creams

Formulated from a variety of oils, Both phases are heated to a

both mineral and vegetable, and from
fatty alcohols, fatty acids, and fatty
esters.
Emulsifying agents include non-ionic
surfactants, detergents, and soaps.
temperature above the melting point
of the highest melting component.
The phases then are mixed, and the
mixture is stirred until reaching
ambient temperature or the mixture
has congealed.

Preparation usually involves

separating the formula components
into two portions: lipid and aqueous.
GELS
 Can be administered GELS (JELLIES)
by the topical
oromucosal routes. Semisolid systems
consisting of dispersions
 Medicated gels may of small or large
be prepared for molecules in an aqueous
administration by the liquid vehicle rendered
skin, the eye, the jellylike by the addition of
nose, the vagina, and a gelling agent.
the rectum.
 Gelling Agents:
• Carboxymethylcellulose
GELS (JELLIES)
• Hydroxypropyl
methylcellulose Semisolid systems
• Tragacanth consisting of dispersions
• Carbomer 910 of small or large
• Carbomer 934 molecules in an aqueous
• Carbomer 934P liquid vehicle rendered
• Carbomer 940 jellylike by the addition of
a gelling agent.
• Carbomer 941
• Carbomer 1342
 Single-phase gels
→ Gels in which the
macromolecules are
uniformly distributed GELS (JELLIES)
throughout a liquid with no
apparent boundaries Semisolid systems
between the dispersed consisting of dispersions
macromolecules and the of small or large
liquid. molecules in an aqueous
liquid vehicle rendered
 Two-phase System (Magma) jellylike by the addition of
→ Gel mass consisting of a gelling agent.
floccules of small distinct
particles.
→ E.g. Milk of magnesia
 Gel solvents:
• Alcohol
• Propylene glycol
GELS (JELLIES)
 Antimicrobial Semisolid systems
Preservatives: consisting of dispersions
• Methylparaben of small or large
• Propylparaben molecules in an aqueous
liquid vehicle rendered
• Chlorhexidine
jellylike by the addition of
gluconate
a gelling agent.

 Gel Stabilizer:
• Edetate disodium
 Gels
Packaging and Storage

Gels should be stored in

tight containers to prevent
water loss.

Avoid freezing gels.

 Penetration enhancers:
• Dimethyl Sulfoxide
• Ethanol
• Propylene Glycol TRANSDERMAL
• Glycerin PREPARATIONS
• PEG
Topical ointments,
• Urea creams, and gels
• Dimethylacetamide designed to deliver a
• Sodium lauryl Sulphate drug systemically by
• Poloxamers addition of penetration
enhancers to the topical
• Spans
vehicle.
• Tweens
• Lecithin
• Terpenes
 Example of Transdermal
Preparations:
TRANSDERMAL
PREPARATIONS
• Pluronic lecithin Topical ointments,
organogel creams, and gels
designed to deliver a
→ Aids in rapid drug systemically by
penetration of many addition of penetration
active drugs through enhancers to the topical
the skin. vehicle.
 Prepared in the same
manner as ointments but a
portion of the base is often
used rather than a liquid,
which would make it softer.
 Remain in place after
application and employed
to absorb serous secretions
because of its stiffness.
 Not suited for application to
hairy parts of the body.
PASTES
Semisolid preparations
intended for application to
the skin. They generally
contain a larger
proportion of solid
material (such as 25%)
than ointments and
therefore are stiffer.
 PASTES
 Example of Pastes: Semisolid preparations
intended for application to
the skin. They generally
• Zinc oxide paste
contain a larger
(Lassar's Plain Zinc
proportion of solid
Paste)
material (such as 25%)
than ointments and
therefore are stiffer.
 Rubber base or a
synthetic resin
• Adhesive material
PLASTERS
 Applied to the skin to
provide prolonged contact Solid or semisolid
at the site. adhesive masses spread
on a backing of paper,
fabric, moleskin, or
 Unmedicated plasters plastic.
• Provide protection or
mechanical support at
the site of application.
 Medicated plasters
• Provide effects at the
site of application
• May be cut to size to
conform to the surface PLASTERS
to be covered.

Solid or semisolid
 Example of Plaster: adhesive masses spread
• Salicylic acid plaster on a backing of paper,
→ Used on the toes for fabric, moleskin, or
the removal of corns. plastic.
→ horny layers of skin
are removed by the
keratolytic action of
salicylic acid.
 Applied to the skin for the
long term.

 Melted, cooled to slightly

above body temperature,
and applied with a fine GLYCEROGELATINS
brush. Glycerogelatin
hardens, covered with a Plastic masses containing
bandage, and is allowed to gelatin (15%), glycerin (40%),
remain in place for weeks. water (35%), and an added
medicinal substance (10%),
 Zinc gelatin such as zinc oxide.
• Most recent official
glycerogelatin
• ,Used in the treatment
of varicose ulcers
 Preparation:
• First softening the gelatin
in the water for about 10 GLYCEROGELATINS
minutes, heating on a
steam bath until the gelatin Plastic masses containing
is dissolved, adding the gelatin (15%), glycerin (40%),
medicinal substance mixed water (35%), and an added
with the glycerin, and medicinal substance (10%),
allowing the mixture to cool such as zinc oxide.
with stirring until
congealed.
 PA S T E S , P L A S T E R S A N D G LY C E R O G E L AT I N S
Packaging Semisolid Preparations
Topical dermatologic products: jars, tubes, or syringes
• Ophthalmic, nasal, vaginal, and rectal semisolid products are almost always
packaged in tubes or syringes.

Ointment jars
Made of clear or opaque glass or plastic. Some are colored green, amber, or blue.
Vary in size from about 0.5 oz to 1 lb.
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations
Opaque jars
• Used for light-sensitive products
• Porcelain white, dark green, or amber in color
Tubes
• Light in weight, relatively inexpensive, convenient for use
• Compatible with most formulative components, and they provide greater protection
against external contamination and environmental conditions than jars
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations

Ointment tubes
• Aluminum tubes: Coated with an epoxy resin, vinyl, or lacquer to eliminate
any interactions between the contents and the tube.

• Plastic tubes:

• LDPE: Soft and resilient, and it provides a good moisture barrier

• HDPE: Provides a superior moisture barrier but is less resilient.
• PP: Has a high level of heat resistance.
• PET: Offers transparency and a high degree of product chemical
compatibility.
• Laminates: Provide an excellent moisture barrier because of the foil
content, high durability, and product compatibility
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations

1.5, 2, 3.5, 5, 15, 30, 45, 60, and 120 g

• Standard sizes of empty tubes

Ointments, creams, and gels are most frequently packaged in 5-, 15-, and 30-g
tubes.

When the ointment is to be used for ophthalmic, rectal, vaginal, aural, or nasal
application, they are packaged with special applicator tips.

Ophthalmic ointments
• Packaged in small aluminum or collapsible plastic tubes holding 3.5 g
• Sterilized before aseptically filled
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations

Syringes for injection / Syringes for oral

use
• Successfully used in packaging
semisolid preparations.

• Advantages:
• Exclusion of air from the system
• Accurate quantities can be applied
using the syringe to measure the
amount needed.
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations

Filling Ointment Jars

Small scale: Ointments prepared by fusion may be

poured directly into the ointment jar to
1. Carefully transfer the weighed congeal in it.
amount of ointment into the jar with a
spatula Pressure fillers (Large Scale)
2. The ointment is packed on the • Force the specified amount of
bottom and along the sides of the jar, ointment into the jars.
avoiding entrapment of air.
3. 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.
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations

Filling Ointment Tubes

(a) 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.

(b) 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.

(c) The bottom of the tube is flattened, folded, and

sealed with a crimping tool or clip.
 Pastes, Plasters and Glycerogelatins
Packaging Semisolid Preparations
Filling Ointment Tubes Filling Syringes

“Caulkinggun” System Syringes can be filled by:

• Semisolid is filled into the
chamber and the product is
delivered into the tube.
• Tubes can then be heat-sealed
using a heat-sealing crimper for
a nice, professional appearance.
Electronic mortars and pestles can
be used to prepare an ointment,
cream, or gel in the dispensing
container.
1. Drawing the semisolid into the
barrel using the plunger (it may
be necessary to soften the
preparation by gentle heating
first); or
2. Removing the plunger and filling
through the back end of the
syringe.
 OINTMENTS, CREAMS, AND GELS
Features and Use of Dermatologic Preparations
Dosage forms used in the topical In treating skin diseases, drug in a
treatment of conditions and diseases medicated application should
of the skin: penetrate and be retained in the skin

• Ointments, Creams, Gels for a while.

• Pastes Drug penetration factors:

• Plasters • Physicochemical properties of

• Solutions the medicinal substance

• Powders • Characteristics of the

pharmaceutical vehicle
• Transdermal drug delivery
systems • Skin conditions
 OINTMENTS, CREAMS, AND GELS
Features and Use Of Ophthalmic Ointments and Gels

Dosage forms: Drug penetration depends on a

• Ointments, Gels
• Solutions, Suspensions
• Inserts
Simple diffusion via the cornea.
• Major route by which drugs enter
the eye.
Conjunctiva and Sclera
• Alternate route for drugs that are
poorly absorbed by the cornea.
drug's ability to traverse the three
layers of the cornea.
• Lipophilic drugs are more
capable of penetration than
hydrophilic compounds
Ophthalmic ointments must meet the
USP sterility tests and the test for
metal particles in ophthalmic
ointments
 OINTMENTS, CREAMS, AND GELS
Features and Use Of Nasal Ointments and Gels

Dosage forms:
• Ointments
• Gels
Drugs introduced into the nasal
passage are primarily for local effects
on the mucous membranes and
underlying tissues.
Drug absorption to the general
circulation also does occur through
the rich blood supply feeding the
nasal lining.
Example:
• Cyanocobalamin (Nascobal
Gel)
→ Intranasal administration,
self-administered as a nasal
gel
→ Used in the treatment of
vitamin B12 deficiency,
including pernicious anemia.
 OINTMENTS, CREAMS, AND GELS
Features and Use of Rectal Preparations

Dosage forms: and discomfort associated with

• Ointments
• Gels
• Creams
• Creamlike aerosol foams
Used for topical application to the
perianal area and for insertion within
the anal canal
Treat local conditions of anorectal
pruritus, inflammation, and the pain
haemorrhoids.
• Astringents (e.g., zinc oxide),
• Protectants and lubricants (e.g.,
cocoa butter, lanolin)
• Local anesthetics (e.g., pramoxine
HCl)
• Antipruritics
• Anti-inflammatory agents (e.g.,
hydrocortisone)
• Antiepileptics (diazepam)
 OINTMENTS, CREAMS, AND GELS
Features and Use of Vaginal Preparations

Dosage forms: manufactured and tested to be free of

• Ointments offending microorganisms, yeasts,
• Gels and molds.
• Creams
• Creamlike foams Once-a-day administration is best
done at bedtime

Topical products are used to treat

vulvovaginal infections, vaginitis,
conditions of endometrial atrophy,
and for contraception with
spermatocidal agents.

These products should be

 OINTMENTS, CREAMS, AND GELS
Drug Release From Semisolid Dosage Forms

In vitro release testing is recommended by the FDA as a measure of “product

sameness” during scale-up and post approval changes for semisolids (SUPAC-
SS).

Franz diffusion cell

• Used where the semisolid dosage form is placed on a membrane that is
situated on top of a receptor chamber containing a receptor solution
• Drug is released from the dosage form and passes through the membrane
into the receptor solution where it is sampled and analyzed for content.
• Results are plotted as the concentration of the drug in the receptor fluid
versus time.
• Rates of drug release can be calculated and compared.
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