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Topical delivery dosage forms


Definition and applications


Hydrocarbon bases

Absorption bases

Water-removable bases

Water-soluble bases

Selection of ointment bases

Preparation of ointments

Some requirements for ointments

Other dosage forms: cream, gel/jelly, paste

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Ointments are semi-solid preparations
intended for external use. They are
easily spread.

Typically used as:

Emollients to make skin more pliable

Protective barriers

Vehicles in which to incorporate
medication www.DuloMix.com 3


Ointment bases

Absorption bases

Water-removable bases

Water-soluble bases

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Hydrocarbon bases

. Petrolatum, USP
Yellow petrolatum/petrolatum jelly

Vaseline (Chesebrough-Ponds/Unilever) (vahser-elaion)

Melts at 38-60oC

White petrolatum, USP
Decolored petrolatum,

White petroleum jelly/white vaseline

Yellow ointment, USP
Yellow wax (5%, w/w), petrolatum (95%)

White ointment, USP
White wax/white petrolatum

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Mineral oil

. Liquid petrolatum

Is a mixture of refined liquid saturated
hydrocarbons obtained from petroleum

Levigating agent to incorporate lipiphilic

An excipient in topical formulations where
its emollient properties are exploited as an
ingredient in ointment bases.

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Oleaginous bases

1. Synthetic esters:

glyceryl monostearate, isopropyl
myristate, isopropyl palmitate, butyl
stearate, butyl palmitate, and long-chain
alcohol (cetyl alcohol, stearyl alcohol, PEG)

2. Lanolin derivates:

Lanolin oil, hydrogenated lanolin

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Hydrocarbon bases

Oleaginous bases

Emollient effect: hydrates skin due to sweat

Occlusive dressing

Difficult to wash-off/remove

Small amount of water can be incorporated into it
with difficulty and can be protective to water
labile drugs such as tetracycline and bacitracin.

Is greasy and can stain clothing.
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Absorption bases

Those that permit the incorporation of aqueous solution resulting in
he formation of w/o emulsions

–hydrophilic petrolatum, USP
Cholesterol 30 g, Stearyl alcohol 30 g

White wax 80 g, White petrolatum 860 g
–Aquaphor: A gentle healing ointment to help heal dry, cracked

(Petrolatum. Other Ingredients: Mineral Oil, Ceresin, Lanolin

Alcohol, Panthenol, Glycerin, Bisabolol)
Those that are w/o emulsion

Hydrous lanolin: w/o emulsion containing 25% of water
lanolin USP: Anhydrous, contains < 0.25% of water, absorbs

twice its weight in water, also called wool wax, wool fat, or wool
grease, a greasy yellow substance from wool-bearing animals, acts
as a skin ointment, water-proofing wax, and raw material (such as
in shoe polish). www.DuloMix.com 9


Properties of absorption bases

Absorption bases (anhydrous)



Absorbs water


W/O emulsion



Contains water, absorbs additional water

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Water-removable bases

Water-washable bases, O/W emulsion

Hydrophilic ointment, USP

Methylparaben 0.25 g

Propylparaben 0.15

SDS 10

Propylene alcohol 120

Stearyl alcohol 250

White petrolatum 250

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Vanishing cream:
o/w emulsion contains la large % of water and
humectant. An excess of stearic acid in the
formula helps to form a thin film when the water

a hypoallergenic, greaseless emulsion

non-greasy emulsion base has pH close to that of

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Water-washable, easier to

Non/less greasy

Can be diluted with water

Non/less occlusive

Better cosmetic appearance

Better compliance

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Water-soluble bases
PEG ointment, NF

– PEG 3350 400 g, PEG 400 600 g

– Polyethylene glycol 200, 300, 400 (4-8oC),
600 (20- 25oC), 1000, 1450, 3350, 4000, 6000,
8000 and 20000

– Only a small amount of liquid (<5%) can be

– If 6-25% of liquid is to be incorporated, 50 g
of the 400 g of PEG 3350 may be replaced
with stearyl alcohol

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ZOVIRAX®, (acyclovir), GSK, Ointment 5%

BACTROBAN® SmithKline Beecham Mupirocin
Topical Antibiotic (Each g of ointment contains:
mupirocin 20 mg (2%) in a bland water-soluble
ointment base consisting of PEG 400 and PEG 3 350
(PEG ointment, USP).

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Water-soluble bases
Glyceryl monstearate

polyhdric alcohol esters

wildly used in cosmetic and ointment bases

Cellulose derivatives


Hydroxyethyl cellulose

synthetic high MW polymers of acrylic acid cross-

linked with either allysucrose or allyl ethers of

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Properties of water-soluble bases

Water soluble and washable


Non/less occlusive

Lipid free

Synthetic base

Relatively inert

Does not support mold growth

Little hydrolysis, stable

May dehydrate skin and hinder percutaneous absorption.
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Desired release rate of drug

Desirability for topical or
percutaneous absorption

Desirability of occlusion

Stability of drug in ointment

Effect of drug on ointment base

Desire for easy removable

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Incorporation: components are mixed until a
uniform preparation is attained.

— Incorporation of solid:

— Incorporation of liquid:

Fusion: All or some components are combined
by being melted together and cooled with
constant stirring until congealed.

— High melting temperature bases such as
beewax, paraffin, stearyl alcohol, and high Mw

Ointments having emulsion bases usually involve
melting and emulsification steps.

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A spatula with a long, broad blade should
be used

Insoluble substances should be powdered
finely in a mortar and mixed with an equal
amount of base until a smooth mixture is
obtained. The rest of the base is added in

Levigation of powders into small portion
of base is facilitated by the use of
levigating agents.

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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.

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.

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Medication order

Sulfur (3-6%, usually)

Salicylic acid, 600 mg

White petrolatum, 30 g

The particle sizes of sulfur and salicylic
acid are reduced separately in a mortar
and then blended together. The powder
mixture is then levigated with the base
using geometric dilution.

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Used when the base contains solids that have higher
melting points. Also for solid medications that are
readily soluble in melted bases.

The oil phase should be melted separately, starting with
materials having the highest melting point.

The ingredients in the water phase are combined and
heated separately to temperature equal to above that of
the oil phase

The two phases are them combined. If a w/o system is
desired, the hot aqueous phase is incorporated into the
hot oil phase with agitation.

Volatile materials are added after the melted mixture
cools to desired temperature.

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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

Minimum fill:

Packaging, storage, labeling: (label should
include the type of base used)

Additional standards: viscosity, in vitro

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Topical dosage form








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Semisolid preparations containing one or
more medicinal agents dissolved in either
an o/w or w/o emulsion or in another type
of water-washable base.

Vanishing cream: o/w with high % of
water and stearic acid.

Cold cream: (an emulsion for softening and
cleansing the skin): w/o, white wax,
spermaceti, almond oil, sodium borate.

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Typically of low viscosity, two phase system (w/o
or o/w)
Appears “creamy white” due to the scattering of
Traditionally, it is the w/o cold cream
Currently and most commonly, it is the o/w

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Cold cream

w/o emulsion frequently using a borax-beewax
combination as the emulsifying agent and
mineral oil or vegetable oil as the oily phase. A
protective film remains on the skin following the
evaporation of the water. The slow evaporation
of water gives the skin a cooling effect.
To prepare, melt white wax, spermaceti, and
almond oil together, adding host aqueous
solution of sodium borate, and stir until the
mixture is cool.

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A formula
Water, 34.6%,
Borax, 1,
methylparaben, 0.25
Light mineral oil,50%,
synthetic beewax, 13,
Glyceryl monostearate,
1, propylparaben, 0.15.

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Gels and jellies

Jellies are water soluble bases prepared from
natural gums such as tragcanth, pectin,
alginates, boroglycerin, or from synthetic
derivatives of natural substances such as
methylcellulose and NaCMC.

Gels: semisolids consisting of dispersions of
small or large molecules in an aqueous liquid
vehicle rendered jelly-like through the
addition of a gellingw waw.gDuelonMitx..com 32


Single-phase gel:

Carbomers: high Mw water soluble polymers of
acrylic acid cross-linked with allyl ethers of sucrose
or pentaerythritol.

Two-phase system: magma/milk of
magnesia/magnesia magma, a gelatinous precipate
of magnesium hydroxide

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Semisolid contains a larger proportion
of solid materials than ointments.
Stiffer than ointment
Good protective barriers

Opague, water impermeable, prevent
Good absorbent Lasser’s plain zinc paste

Zinc oxide 25%
Starch, 25%
White petrolatum, 50%

Anthralin in for psoriasis