This document discusses various topical dosage forms including ointments, creams, gels, and pastes. It defines ointments as semisolid preparations for external use that are easily spread. Various ointment bases are described such as hydrocarbon bases like petrolatum, absorption bases, water-removable bases, and water-soluble bases. Methods for preparing ointments like incorporation and fusion are outlined. Requirements for ointments regarding microbial content, packaging and labeling are also summarized.

1. PRESENTED BY:
L.GOPI M.PHARM FIRST YEAR
AADHI BHAGAWAN COLLEGE OF PHARMACY
RANTHAM
GUIDED BY:
Dr.V.KALVIMOORTHY M.PHARM.,PhD
PROF OF DEPARTMENT OF
PHARMACEUTICS
AADHI BHAGAWAN COLLEGE OF
PHARMACY
RANTHAM

2. OINTMENT

3. Topical delivery dosage forms
 Ointments
 Definition and applications
 Classification
 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

4. Ointments
 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

5. Ointment bases
 Hydrocarbon
 Absorption bases
 Water-removable bases
 Water-soluble bases

6. 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

7. Mineral oil
 . Liquid petrolatum
 Is a mixture of refined liquid saturated
hydrocarbons obtained from petroleum
 Levigating agent to incorporate lipiphilic
solids
 An excipient in topical formulations where
its emollient properties are exploited as an
ingredient in ointment bases.

8. 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

9. Hydrocarbon bases
 Oleaginous bases
 Emollient effect: hydrates skin due to sweat
accumulation
 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.

10. 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
skin
(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).

11. Properties of absorption bases
Absorption bases (anhydrous)
Emollient
Occlusive
Absorbs water
Greasy
W/O emulsion
Emollient
Occlusive
Contains water, absorbs additional water
Greasy

12. 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
 Water 370

13. 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
evaporates.
Dermovan:
a hypoallergenic, greaseless emulsion
Unibase:
non-greasy emulsion base has pH close to that of
skin

14. Water-washable, easier to
remove
Non/less greasy
Can be diluted with water
Non/less occlusive
Better cosmetic appearance
Better compliance

15. 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
incorporated
- If 6-25% of liquid is to be incorporated, 50 g
of the 400 g of PEG 3350 may be replaced
with stearyl alcohol

16.  EXAMPLE

 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).

17.  Glyceryl monstearate
 polyhdric alcohol esters
 wildly used in cosmetic and ointment bases
 Cellulose derivatives
 Methylcellulose
 Cellulose
 Hydroxyethyl cellulose
 Carbopol/carbomer
 synthetic high MW polymers of acrylic acid cross-
linked with either allysucrose or allyl ethers of
pentaerythritol.
Water-soluble bases

18.  Water soluble and washable
 Non-greasy
 Non/less occlusive
 Lipid free
 Synthetic base
Relatively inert
Does not support mold growth
Little hydrolysis, stable
May dehydrate skin and hinder percutaneous absorption.
Properties of water-soluble bases

21.  Desired release rate of drug
substance
 Desirability for topical or
percutaneous absorption
 Desirability of occlusion
 Stability of drug in ointment
 Effect of drug on ointment base
 Desire for easy removable

22.  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
PEG.
 Ointments having emulsion bases usually involve
melting and emulsification steps.

23.  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
increment.
 Levigation of powders into small portion
of base is facilitated by the use of
levigating agents.
Incorporation

24. 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.

25.  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.
Example

26.  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.
Fusion

27.  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
Requirement for ointments

28.  Ointments
 Creams
 Pastes
 Gels/jellies
 Solution
 Plasters
 Aerosols
 Powders
Topical dosage form

29. Cream
 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.

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

31. 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.

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

33. 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 gelling agent.

34. 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

35. Pastes
Semisolid contains a larger proportion
of solid materials than ointments.
Stiffer than ointment
Good protective barriers
Opague, water impermeable, prevent
dehydration
Good absorbent Lasser’s plain zinc paste
Zinc oxide 25%
Starch, 25%
White petrolatum, 50%
Anthralin in for psoriasis

36. THE END