Ointment

Include drug delivery systems and dosageInclude drug delivery systems and dosage
forms intended to be applied to the skin.forms intended to be applied to the skin.
CreamsCreams
OintmentsOintments
GelsGels
PastesPastes

Preparations are applied to the skin for:Preparations are applied to the skin for:
Physical effectsPhysical effects
skin protection, lubricants, emollients, drying agentsskin protection, lubricants, emollients, drying agents
Medical effectsMedical effects
•Treatment of skin conditions (non-systemic topical effect)Treatment of skin conditions (non-systemic topical effect)
as skin infections, itching, burns, diaper rash, insectas skin infections, itching, burns, diaper rash, insect
stings and bites, corns, calluses, warts, dandruff, acne,stings and bites, corns, calluses, warts, dandruff, acne,
psoriasis, and eczema.psoriasis, and eczema.
• Systemic effectSystemic effect

The SkinThe Skin
The skin has a wide variety of functions:The skin has a wide variety of functions:
Protect the organism from water loss andProtect the organism from water loss and
mechanical, chemical, microbial, and physicalmechanical, chemical, microbial, and physical
influences.influences.

Structure of the SkinStructure of the Skin
The skin is the largest human organ and is composed of:The skin is the largest human organ and is composed of:
 A film of emulsified material present upon the surface ofA film of emulsified material present upon the surface of
the skin composed of a complex mixture of sebum, sweatthe skin composed of a complex mixture of sebum, sweat
 Three functional layers:Three functional layers:
 Epidermis,Epidermis,
 Dermis (true skin)Dermis (true skin)
 HypodermisHypodermis
(Subcutaneous fat layer).(Subcutaneous fat layer).
 Blood capillaries andBlood capillaries and
nerve fibersnerve fibers
 Sweat glandsSweat glands
 Hair folliclesHair follicles

The epidermis is the outermost layer of the skinThe epidermis is the outermost layer of the skin
 0.02 to 5 mm thickness0.02 to 5 mm thickness
 It has five layers,It has five layers,
o Barrier layer (stratum germinativum)Barrier layer (stratum germinativum)
 Beneath the hornylayerBeneath the hornylayer
 Composed of living epidermal cellsComposed of living epidermal cells
o Horny layerHorny layer
(stratum corneum)(stratum corneum)
 The uppermost layerThe uppermost layer
Composed of dead epidermal cells forms the permeability barrierComposed of dead epidermal cells forms the permeability barrier

The stratum corneum consists of:The stratum corneum consists of:
Horny skin cellsHorny skin cells (corneocytes)(corneocytes) which are connectedwhich are connected
via protein-rich attachments of the cell membranevia protein-rich attachments of the cell membrane
The corneocytes are embedded in a lipid matrix inThe corneocytes are embedded in a lipid matrix in
““Brick and mortarBrick and mortar” structure.” structure.
The corneocytes of hydrated keratin comprise theThe corneocytes of hydrated keratin comprise the
bricks and the epidermal lipids fill the spacebricks and the epidermal lipids fill the space
between the dead cells like mortarbetween the dead cells like mortar

Routes of skin PenetrationRoutes of skin Penetration
Include transport via:Include transport via:
1-1- Hair follicles and sebaceousHair follicles and sebaceous
glandsglands
2-2- Sweat glandsSweat glands
1 2
These routes avoid penetration through the stratumThese routes avoid penetration through the stratum
corneum and therefore known ascorneum and therefore known as shunt routesshunt routes..
The Transappendageal route:The Transappendageal route:The Transappendageal route:The Transappendageal route:
There are two diffusional routes to penetrate intact skinThere are two diffusional routes to penetrate intact skin::

1 2
 Although these routes offer high permeability, they are ofAlthough these routes offer high permeability, they are of
minor importance because of their relatively small area,minor importance because of their relatively small area,
0.1% of the total skin area.0.1% of the total skin area.
The transappendageal routeThe transappendageal route
seems to be most important forseems to be most important for
ions and large polar moleculesions and large polar molecules
which hardly permeate throughwhich hardly permeate through
the stratum corneum.the stratum corneum.
The transappendageal routeThe transappendageal route
seems to be most important forseems to be most important for
ions and large polar moleculesions and large polar molecules
which hardly permeate throughwhich hardly permeate through
the stratum corneum.the stratum corneum.

Transepidermal transportTransepidermal transport
means that molecules crossmeans that molecules cross
the intact horny layerthe intact horny layer
The
The transepidermal route :
transepidermal route :
The
The transepidermal route :
transepidermal route :

Two potential micro-routes are existingTwo potential micro-routes are existing
**The transcellular (intracellular) routThe transcellular (intracellular) rout
*The intercellular pathways*The intercellular pathways
The principal pathway taken byThe principal pathway taken by
drugs is decided by its partitiondrugs is decided by its partition
coefficientcoefficient
Hydrophilic drugs partition into the intracellular pathways,Hydrophilic drugs partition into the intracellular pathways,
whereas lipophilic drugs traverse the stratum corneum viawhereas lipophilic drugs traverse the stratum corneum via
the intercellular route.the intercellular route.

Factors Affecting PercutaneousFactors Affecting Percutaneous
AbsorptionAbsorption
 Factors concerning the nature of the drugFactors concerning the nature of the drug
 Factors concerning the nature of the vehicleFactors concerning the nature of the vehicle
 Factors concerning the condition of the skinFactors concerning the condition of the skin
Percutaneous absorptionPercutaneous absorption is the absorption of substancesis the absorption of substances
from outside the skin to positions beneath the skin,from outside the skin to positions beneath the skin,
including entrance into the blood stream.including entrance into the blood stream.

1.1. Drug concentration Percutaneous absorptionDrug concentration Percutaneous absorption
2.2. Drug partition coefficient (greater attraction to the skinDrug partition coefficient (greater attraction to the skin
than to the vehicle) Percutaneous absorptionthan to the vehicle) Percutaneous absorption
3.3. Molecular weight below 800Molecular weight below 800
Percutaneous absorptionPercutaneous absorption
4.4. Particle SizeParticle Size
5. Solubility in mineral oil and water5. Solubility in mineral oil and water
 Factors concerning the nature of the drugFactors concerning the nature of the drug

1.1. Spreadability of the vehicleSpreadability of the vehicle
2.2. Mixing with the sebumMixing with the sebum
3.3. Hydration of the skin Percutaneous absorptionHydration of the skin Percutaneous absorption
Oleaginous vehicles act as moisture barriers throughOleaginous vehicles act as moisture barriers through
which the sweat from the skin cannot pass, thuswhich the sweat from the skin cannot pass, thus
increased hydration of the skin beneath the vehicle andincreased hydration of the skin beneath the vehicle and
increase Percutaneous absorption.increase Percutaneous absorption.
Factors concerning the nature of the vehicleFactors concerning the nature of the vehicle

 Factors concerning the condition of the skinFactors concerning the condition of the skin
Transdermal absorption followTransdermal absorption follow Fick’s First LawFick’s First Law ofof
DiffusionDiffusion
Js =Js = Km D CsKm D Cs
EE
Js = Flux of solute through the skinJs = Flux of solute through the skin
Km = Distribution coefficient of drug between vehicleKm = Distribution coefficient of drug between vehicle
andand
stratum corneumstratum corneum
Cs = Concentration difference of solute across theCs = Concentration difference of solute across the
membranemembrane
D = Membrane Diffusion coefficient for drug in stratumD = Membrane Diffusion coefficient for drug in stratum
corneumcorneum

1.1. The thickness stratum corneumThe thickness stratum corneum
2.2. Multiple application dosingMultiple application dosing
Percutaneous absorption than single ApplicationPercutaneous absorption than single Application
3.3. Time of contact with the skinTime of contact with the skin
PercutaneousPercutaneous
absorptionabsorption
4.4. Broken skin permit (remove of the stratum corneum)Broken skin permit (remove of the stratum corneum)

Percutaneous Absorption Enhancers
Mechanisms of action by which Materials enhanceMechanisms of action by which Materials enhance
absorption through stratum corneum is either byabsorption through stratum corneum is either by
 Enhancing drug release from the formulation to the skinEnhancing drug release from the formulation to the skin
 Reduction of the resistance of the stratum corneum byReduction of the resistance of the stratum corneum by
altering it physicochemical propertiesaltering it physicochemical properties

 Alteration of the hydration of the stratumAlteration of the hydration of the stratum
corneum using occlusive formulationscorneum using occlusive formulations
 Carrier mechanisms in the transport of ionisableCarrier mechanisms in the transport of ionisable
drugsdrugs
 Enhance absorption by directly influencingEnhance absorption by directly influencing
the stratum corneumthe stratum corneum
(CHEMICALLY or PHYSICALLY)(CHEMICALLY or PHYSICALLY)
This can be achieved by the followingThis can be achieved by the following
mechanisms:mechanisms:

Chemicals used to enhance absorption by directlyChemicals used to enhance absorption by directly
influencing the stratum corneuminfluencing the stratum corneum
Chemicals interact with theChemicals interact with the keratin structurekeratin structure in the stratumin the stratum
corneum and open the tight protein structure, this leadscorneum and open the tight protein structure, this leads
increase the diffusion coefficient D for substances which useincrease the diffusion coefficient D for substances which use
the transcellular route:the transcellular route:
Surfactants, Dimethylsulfoxide (DMSO)Surfactants, Dimethylsulfoxide (DMSO) and Urea
Solvents extract lipids and making the stratum corneum moreSolvents extract lipids and making the stratum corneum more
permeable:permeable: Dimethylsulfoxide (DMSO) and EthanolDimethylsulfoxide (DMSO) and Ethanol

Chemical enhancersChemical enhancers which intercalate into the structuredwhich intercalate into the structured
lipids of the horny layer and disrupt the packing. Thuslipids of the horny layer and disrupt the packing. Thus
make the regular structure more fluid and increases themake the regular structure more fluid and increases the
diffusion coefficient of drugs:diffusion coefficient of drugs:
Azone, Oleic acid, and isopropyl myristateAzone, Oleic acid, and isopropyl myristate
Solvents increase solubility and improve partitioning:Solvents increase solubility and improve partitioning:
Alcohol, acetone, polyethylene and propylene glycolAlcohol, acetone, polyethylene and propylene glycol

Ointments are semisolid preparations intended forOintments are semisolid preparations intended for
external application.external application.
 Ointments may be medicated or non-medicatedOintments may be medicated or non-medicated
Non-medicatedNon-medicated ointment bases used for theirointment bases used for their
emollient, lubricating effect or as vehicles in theemollient, lubricating effect or as vehicles in the
preparation ofpreparation of medicated ointmentsmedicated ointments

Ointment bases are classified into 4 groups:Ointment bases are classified into 4 groups:
(1)(1) Hydrocarbon bases (Oleaginous Base)Hydrocarbon bases (Oleaginous Base)
(2)(2) Absorption basesAbsorption bases
(3)(3) Water-removable basesWater-removable bases
(4)(4) Water -soluble basesWater -soluble bases
Ointment BasesOintment Bases

1.1. Water-freeWater-free
2.2. Difficult to wash offDifficult to wash off
3.3. Aqueous preparations are difficult to beAqueous preparations are difficult to be
incorporated into themincorporated into them
4.4. Used as occlusive dressings for their emollient effectUsed as occlusive dressings for their emollient effect
(helps the skin retain moisture)(helps the skin retain moisture)
It can treat diaper rash (protect skinIt can treat diaper rash (protect skin
fromfrom
urine) and dry skin (retain moisture)urine) and dry skin (retain moisture)
5. Stable, don’t dry upon aging
Hydrocarbon bases (oleaginous basesHydrocarbon bases (oleaginous bases))

Petrolatum (Soft Paraffin)Petrolatum (Soft Paraffin)
Yellow Petrolatum (Vaseline)Yellow Petrolatum (Vaseline)
Mixture of semisolid hydrocarbons obtained from petroleum.Mixture of semisolid hydrocarbons obtained from petroleum.
Melts at temperatures between 38° and 60°CMelts at temperatures between 38° and 60°C
Form an ointment-like gel with Polyethylene (PLASTIBASE)Form an ointment-like gel with Polyethylene (PLASTIBASE)
which is compatible with most medicaments.which is compatible with most medicaments.
White Petrolatum (White Vaseline)White Petrolatum (White Vaseline)
Decolorized petrolatumDecolorized petrolatum
More esthetically acceptable to patients than petrolatum.More esthetically acceptable to patients than petrolatum.

White Ointment (Simple Ointment)White Ointment (Simple Ointment)
Contains 5% of White wax and 95 % of White petrolatumContains 5% of White wax and 95 % of White petrolatum
Contains 5% of yellow wax and 95 % of petrolatum.Contains 5% of yellow wax and 95 % of petrolatum.
Yellow Wax, is the purified wax obtained from the honeyYellow Wax, is the purified wax obtained from the honey
Yellow Ointment (Simple Ointment)Yellow Ointment (Simple Ointment)

Absorption BasesAbsorption Bases
An absorption base is an oleaginous base that permit theAn absorption base is an oleaginous base that permit the
incorporation of aqueous solutions, and can be used asincorporation of aqueous solutions, and can be used as
emollientsemollients
Like the oleaginous bases,Like the oleaginous bases,
• Absorption bases are not water washableAbsorption bases are not water washable
• They can incorporate 50% of their volume water,They can incorporate 50% of their volume water,
where aqueous solution first incorporated into thewhere aqueous solution first incorporated into the
absorption base, then added into the oleaginous baseabsorption base, then added into the oleaginous base

2)2) Water-in-oil emulsions (emulsion bases) that permit theWater-in-oil emulsions (emulsion bases) that permit the
incorporation of small, additional quantities of aqueousincorporation of small, additional quantities of aqueous
solutionssolutions
(e.g. Lanolin and Cold cream)(e.g. Lanolin and Cold cream)
There are two types of absorption bases:There are two types of absorption bases:
1)1) Contains a w/o emulsifying agent:Contains a w/o emulsifying agent:
When water is taken up into the base, it will form aWhen water is taken up into the base, it will form a w/ow/o
emulsionemulsion
(e.g. Hydrophilic Petrolatum and Anhydrous Lanolin)(e.g. Hydrophilic Petrolatum and Anhydrous Lanolin)

It has the ability to absorbIt has the ability to absorb
water (upto 3 times itswater (upto 3 times its
weight), with formation ofweight), with formation of
water-in-oil emulsion W/Owater-in-oil emulsion W/O
Hydrophilic Petrolatum (Aquaphor)Hydrophilic Petrolatum (Aquaphor)
Hydrophilic Petrolatum is composed of 3% cholesterol,Hydrophilic Petrolatum is composed of 3% cholesterol,
3% stearyl alcohol, 8% white wax, and 86% white3% stearyl alcohol, 8% white wax, and 86% white
petrolatum.petrolatum.

Obtained from the wool of sheepObtained from the wool of sheep
 It is a water-in-oil emulsion W/O that contains betweenIt is a water-in-oil emulsion W/O that contains between
25 and 30% water25 and 30% water Additional water may be incorporated intoAdditional water may be incorporated into
lanolin by mixinglanolin by mixing
Lanolin (Hydrous Wool Fat)Lanolin (Hydrous Wool Fat)
It is insoluble in water, but mixesIt is insoluble in water, but mixes
without separation with water twicewithout separation with water twice
its weight of water with theits weight of water with the
formation of a water-in-oil emulsionformation of a water-in-oil emulsion
Anhydrous Lanolin (Wool Fat)Anhydrous Lanolin (Wool Fat)

 Oil in Water emulsionsOil in Water emulsions
 Have the general formula: 30 % Emulsifying waxHave the general formula: 30 % Emulsifying wax
50 % White soft Paraffin50 % White soft Paraffin
20 % Liquid Paraffin20 % Liquid Paraffin
 Water washableWater washable
 They can be diluted with water or with aqueousThey can be diluted with water or with aqueous
solutions. “solutions. “water-lovingwater-loving ““
 They have the ability to absorb serous dischargesThey have the ability to absorb serous discharges
in dermatologic conditionsin dermatologic conditions
Water-Removable BasesWater-Removable Bases
oil-in-water emulsionsoil-in-water emulsions

Methyl and propyl parabens are used as preservativesMethyl and propyl parabens are used as preservatives
Sodium Lauryl SulfateSodium Lauryl Sulfate 1 %1 % emulsifying agentemulsifying agent
Stearyl AlcoholStearyl Alcohol 25 %25 % emulsifying agentemulsifying agent
White PetrolatumWhite Petrolatum 25 %25 % oleaginous phaseoleaginous phase
Propylene GlycolPropylene Glycol 12 %12 % aqueous phaseaqueous phase
Purified WaterPurified Water 37 %37 % aqueous phaseaqueous phase
Hydrophilic OintmentHydrophilic Ointment
Have the general formula:Have the general formula:

Water-Soluble Bases (Water-Soluble Bases (greaseless bases)greaseless bases)Water-Soluble Bases (Water-Soluble Bases (greaseless bases)greaseless bases)
Unlike water-removable basesUnlike water-removable bases,,
which contain both water-soluble and water-insolublewhich contain both water-soluble and water-insoluble
components, water-soluble bases contain only water-solublecomponents, water-soluble bases contain only water-soluble
components with the absence of any oleaginous materialscomponents with the absence of any oleaginous materials
Like water-removable basesLike water-removable bases,,
They are water washableThey are water washable
Because they soften greatly with the addition of water, aqueousBecause they soften greatly with the addition of water, aqueous
solutions are not preferred to be incorporated into these bases.solutions are not preferred to be incorporated into these bases.
They are better used for the incorporation of nonaqueous orThey are better used for the incorporation of nonaqueous or
solid substancessolid substances

Polyethylene glycols are polymers of ethylene oxide andPolyethylene glycols are polymers of ethylene oxide and
water represented by the formulawater represented by the formula
HOCHHOCH22(CH(CH22OCHOCH22)nCH)nCH22OHOH
The chain length varied to achieve polymers with differentThe chain length varied to achieve polymers with different
physical form (liquid, semisolid, or solid).physical form (liquid, semisolid, or solid).
Polyethylene Glycol OintmentsPolyethylene Glycol Ointments

PEGPEG APPEARANCE AT 25° CAPPEARANCE AT 25° C PHPH
AVERAGEAVERAGE
MOLECULARMOLECULAR
WEIGHTWEIGHT
MELTINGMELTING
POINTPOINT
HYDROXYLHYDROXYL
VALUEVALUE
MOISTUREMOISTURE
CONTENTCONTENT
MAX.MAX.
PEG-200PEG-200
Clear viscous colorlessClear viscous colorless
liquidliquid
4.0-7.04.0-7.0 190-210190-210 <65°C<65°C 500-550500-550 1.0%1.0%
PEG-300PEG-300
liquidliquid
4.0-7.04.0-7.0 290-310290-310 <15°C<15°C 340-394340-394 1.0%1.0%
PEG-400PEG-400
liquidliquid
4.0-7.04.0-7.0 390-410390-410 4-8°C4-8°C 264-300264-300 1.0%1.0%
PEG-600PEG-600
liquidliquid
4.0-7.04.0-7.0 590-610590-610 15-17°C15-17°C 176-200176-200 1.0%1.0%
PEG-1000PEG-1000 White waxy solidWhite waxy solid 4.0-7.04.0-7.0 950-1050950-1050 37-38°C37-38°C 105-120105-120 1.0%1.0%
PEG-1500PEG-1500 White waxy solidWhite waxy solid 4.0-7.04.0-7.0 1450-15501450-1550 44-45°C44-45°C 70-9070-90 1.0%1.0%
PEG-2000PEG-2000 White flakesWhite flakes 4.0-7.04.0-7.0 1950-20501950-2050 45-46°C45-46°C 50-7050-70 1.0%1.0%
PEG-4000PEG-4000 White flakesWhite flakes 4.0-7.04.0-7.0 3800-42003800-4200 53-56 °C53-56 °C 30-3630-36 1.0%1.0%
PEG-6000PEG-6000 White flakesWhite flakes 4.0-7.04.0-7.0 5500-65005500-6500 55-63 °C55-63 °C 16-2016-20 1.0%1.0%

Preparation of polyethylene glycolPreparation of polyethylene glycol
ointment base:base:
Combine polyethylene glycol 3350 (solid) 40 %Combine polyethylene glycol 3350 (solid) 40 %
and polyethylene glycol 400 (liquid) 60 %and polyethylene glycol 400 (liquid) 60 %
If an aqueous solution is to be incorporated into the base,If an aqueous solution is to be incorporated into the base,
substitution some of polyethylene glycol 3350 with an equalsubstitution some of polyethylene glycol 3350 with an equal
amount of stearyl alcohol would be advantageous to renderamount of stearyl alcohol would be advantageous to render
the final product more firm.the final product more firm.

OLEAINOUSOLEAINOUS
GG
OINTMENTOINTMENT
BASESBASES
ABSORPTIONABSORPTION
OINTMENTOINTMENT
BASESBASES
WATER-WATER-
REMOVABLEREMOVABLE
OINTMENT BASESOINTMENT BASES
WATER-WATER-
SOLUBLESOLUBLE
OINTMENTOINTMENT
BASESBASES
CompositioCompositio
nn
OleaginousOleaginous
compoundscompounds
OleaginousOleaginous
bases +bases +
w/o surfactantw/o surfactant
Oleaginous base +Oleaginous base +
Water (> 45%) +Water (> 45%) +
O/W surfac. (HLBO/W surfac. (HLB
>>9)9)
PolyethylenePolyethylene
Glycols (PEGs)Glycols (PEGs)
WaterWater
ContentContent
AnhydrousAnhydrous anhydrousanhydrous hydroushydrous
anhydrous,anhydrous,
hydroushydrous
Affinity forAffinity for
WaterWater
HydrophobicHydrophobic hydrophilichydrophilic hydrophilichydrophilic hydrophilichydrophilic
SpreadabilitSpreadabilit
yy
difficultdifficult difficultdifficult easyeasy
moderate tomoderate to
easyeasy
WashabilitWashabilit
yy
non-washablenon-washable non-washablenon-washable washablewashable washablewashable
StabilityStability
oils poor;oils poor;
hydrocarbonshydrocarbons
betterbetter
oils poor;oils poor;
hydrocarbonshydrocarbons
betterbetter
unstableunstable stablestable
DrugDrug
IncorporatiIncorporati
onon
•SolidsSolids
•Oils (oilOils (oil
•SolidsSolids
•OilsOils
•AqueousAqueous
• SolidSolid
• Aqueous solutionsAqueous solutions
•SolidSolid
•AqueousAqueous
solutionssolutions

Continue Continue
OLEAGINOUOLEAGINOU
SS
OINTMENTOINTMENT
BASESBASES
ABSORPTIONABSORPTION
OINTMENT BASESOINTMENT BASES
WATER-WATER-
REMOVABLEREMOVABLE
OINTMENTOINTMENT
BASESBASES
WATER-WATER-
SOLUBLESOLUBLE
OINTMENTOINTMENT
BASESBASES
DrugDrug
ReleaseRelease
poorpoor
poorpoor
but > oleaginousbut > oleaginous
fair to goodfair to good goodgood
OcclusivenesOcclusivenes
ss
yesyes yesyes nono nono
UsesUses
•ProtectantsProtectants
•EmollientsEmollients
• Vehicles forVehicles for
hydrolysablehydrolysable
drugsdrugs
•ProtectantsProtectants
•Vehicles forVehicles for
aqueousaqueous
solutions, solids,solutions, solids,
and nonand non
hydrolyzablehydrolyzable
drugsdrugs
• Vehicles forVehicles for
solid, liquid, orsolid, liquid, or
non-hydrolyzablenon-hydrolyzable
drugsdrugs
DrugDrug
vehiclesvehicles
ExamplesExamples
•YellowYellow
PetrolatumPetrolatum
• WhiteWhite
• YellowYellow
OintmentOintment
• HydrophilicHydrophilic
(Aquaphor®),(Aquaphor®),
• AnhydrousAnhydrous
LanolinLanolin
HydrophilicHydrophilic
OintmentOintment
PEGPEG
OintmentOintment

Selection of the Appropriate BaseSelection of the Appropriate BaseSelection of the Appropriate BaseSelection of the Appropriate Base
The condition of the patient's skin, e.g. oozing or dryThe condition of the patient's skin, e.g. oozing or dry
The rule in dermatology thatThe rule in dermatology that
if a patient's skin is dry-wet it, If it is wet-dry itif a patient's skin is dry-wet it, If it is wet-dry it
if a patient's skin is dry, occlusive ointment base that retainif a patient's skin is dry, occlusive ointment base that retain
moisture is preferablemoisture is preferable
The selection of the base of an ointment
depends on many factors:
Patient FactorsPatient Factors

Physicochemical FactorsPhysicochemical Factors
The desired release rate of the drug from the ointment base
The desired enhancement of the percutaneous absorption
of the drug
The desired occlusion of moisture from the skin by the base
The stability of the drug in the ointment base, for a drug that
hydrolyzes rapidly as antibiotics, a hydrocarbon base would
provide the greatest stability
The influence of the drug on the consistency of the ointment
11
22
33
44
55

The influence of the drug on the consistency of the ointment
base
The desired washability of the base as for application to
hairy regions, a Polyethylene Glycol base is preferred
For ophthalmic ointments, non-irritant bases are desired.
Absorption O/W emulsion bases and water soluble bases
are irritants due to the effect of the surfactants in the base
It is preferred to use yellow paraffin but not white due to the
irritation effect of the bleaching agents
88
77
66

Preparation of OintmentsPreparation of Ointments
depending on the nature of the ingredientsdepending on the nature of the ingredients
ointments are prepared by two methods:ointments are prepared by two methods:

A- INCORPORATION OF SOLIDS:A- INCORPORATION OF SOLIDS:
Using the geometric dilution methodUsing the geometric dilution method
The powdered components reduced to fine powders toThe powdered components reduced to fine powders to
prevent grittinessprevent grittiness
Fine powdered drugs are blendedFine powdered drugs are blended
Then powder are levigated with agent that is compatibleThen powder are levigated with agent that is compatible
with the base, e.g., mineral oil or glycerinwith the base, e.g., mineral oil or glycerin
The amount of levigating agent equal to the material to beThe amount of levigating agent equal to the material to be
levigatedlevigated
Incorporation methodIncorporation method

Solid materials soluble in a solvent that is compatibleSolid materials soluble in a solvent that is compatible
with the product may first be dissolvedwith the product may first be dissolved
e.g., dissolve salicylic acid crystals in alcohole.g., dissolve salicylic acid crystals in alcohol
Mix with a portion of the base until the product is smoothMix with a portion of the base until the product is smooth
and uniformand uniform
Another portion of the base is added to theAnother portion of the base is added to the
mixturemixture
The process being repeated until all of theThe process being repeated until all of the
ointment base has been incorporatedointment base has been incorporated

Ointment roller mills resulting in a productsOintment roller mills resulting in a products
that are smooth and uniform in compositionthat are smooth and uniform in composition
and textureand texture

INCORPORATION OF LIQUIDSINCORPORATION OF LIQUIDS
For aqueous solutions:For aqueous solutions:
 Water-absorbable or hydrophilic ointment bases are suitableWater-absorbable or hydrophilic ointment bases are suitable
 In oleaginous ointment base, a portion of the base mustIn oleaginous ointment base, a portion of the base must
be replaced with a hydrophilic base,be replaced with a hydrophilic base,
 Incorporates the solution in it, and mixes the productIncorporates the solution in it, and mixes the product
with the original basewith the original base

For Alcoholic solutionsFor Alcoholic solutions
 Oleaginous vehicles or emulsion bases are suitableOleaginous vehicles or emulsion bases are suitable
Other liquid materials as natural balsamsOther liquid materials as natural balsams
(Peru balsam)(Peru balsam)
 It is difficult to be incorporated into ointment basesIt is difficult to be incorporated into ointment bases
 Mix balsam with an equal portion of castor oil beforeMix balsam with an equal portion of castor oil before
incorporating it into the baseincorporating it into the base
This procedure reduces the surface tension of theThis procedure reduces the surface tension of the
balsambalsam
and aid in distribution of the balsam through the vehicleand aid in distribution of the balsam through the vehicle

Ointment bases containing components as:Ointment bases containing components as:
beeswax, paraffin, stearyl alcohol, and high molecularbeeswax, paraffin, stearyl alcohol, and high molecular
weight polyethylene glycols, which do not mix well byweight polyethylene glycols, which do not mix well by
incorporation, are prepared by fusionincorporation, are prepared by fusion
Fusion methodFusion method

The components of an ointment are combined by beingThe components of an ointment are combined by being
melted together and cooled with constant stirring untilmelted together and cooled with constant stirring until
congealedcongealed
Components not melted are added to the congealingComponents not melted are added to the congealing
mixture during cooling and stirringmixture during cooling and stirring
Heat-labile and volatile substances are added when theHeat-labile and volatile substances are added when the
temperature of the mixture is low enoughtemperature of the mixture is low enough

Many substances are added to the congealingMany substances are added to the congealing
mixture in solution, others are added as insolublemixture in solution, others are added as insoluble
powders levigated with a portion of the basepowders levigated with a portion of the base
Once congealed, the ointment may be passedOnce congealed, the ointment may be passed
through an ointment mill to ensure a uniformthrough an ointment mill to ensure a uniform
texturetexture

If the item having the highest melting point isIf the item having the highest melting point is
melted first and the other components are added tomelted first and the other components are added to
this hot liquid, all the components will be subjectedthis hot liquid, all the components will be subjected
to this high temperature, irrespective of their ownto this high temperature, irrespective of their own
individual melting pointsindividual melting points

By melting the component having the lowestBy melting the component having the lowest
melting point first and adding the components ofmelting point first and adding the components of
higher melting points in order of their individualhigher melting points in order of their individual
melting points a lower temperature is usuallymelting points a lower temperature is usually
sufficient to achieve fusionsufficient to achieve fusion
*This is due to the solvent action exerted by the first*This is due to the solvent action exerted by the first
melted component on the other componentsmelted component on the other components

In the preparation of ointments having anIn the preparation of ointments having an
emulsion type:emulsion type:
Melting process and emulsification process are usedMelting process and emulsification process are used
 The water- immiscible components such as oil andThe water- immiscible components such as oil and
waxes are melted together in a steam bath to aboutwaxes are melted together in a steam bath to about
70 to 75°C70 to 75°C
 Aqueous solution of all of the heat-stable, water-solubleAqueous solution of all of the heat-stable, water-soluble
components is prepared in the amount of water in thecomponents is prepared in the amount of water in the
formula and heated to the same temperature as theformula and heated to the same temperature as the
oleaginous componentsoleaginous components
The aqueous solution is slowly added to the meltedThe aqueous solution is slowly added to the melted
oleaginous mixture, with constant stirringoleaginous mixture, with constant stirring

 The temperature is maintained for 5 to 10 minutesThe temperature is maintained for 5 to 10 minutes
to prevent crystallization of waxes.to prevent crystallization of waxes.
Then the mixture is slowly cooled with the stirringThen the mixture is slowly cooled with the stirring
until congealinguntil congealing

Preservation of OintmentsPreservation of Ointments
 Semisolid preparations as ointments especiallySemisolid preparations as ointments especially
those utilizing bases which contain water requirethose utilizing bases which contain water require
the addition of antimicrobial preservatives tothe addition of antimicrobial preservatives to
inhibit the contaminationinhibit the contamination
Using preservatives as p-hydroxybenzoates,Using preservatives as p-hydroxybenzoates,
phenols, benzoic acid, sorbic acid, quaternaryphenols, benzoic acid, sorbic acid, quaternary
ammonium saltsammonium salts
Ultra filtration of the vehicle and using asepticUltra filtration of the vehicle and using aseptic
manufacturing processesmanufacturing processes

Packaging and Storage of OintmentsPackaging and Storage of OintmentsPackaging and Storage of OintmentsPackaging and Storage of Ointments
Semisolid preparations must be protectedSemisolid preparations must be protected
through proper packaging and storage from thethrough proper packaging and storage from the
destructive influences of air, light, moisture, anddestructive influences of air, light, moisture, and
heat, and the possible chemical interactionsheat, and the possible chemical interactions
between the preparation and the containerbetween the preparation and the container

Opaque and colored-glass containers are useful forOpaque and colored-glass containers are useful for
ointments containing drugs that are light sensitiveointments containing drugs that are light sensitive
Jars for ointments may vary in size from as little as 1/2 ozJars for ointments may vary in size from as little as 1/2 oz
to 1lb or moreto 1lb or more
Ointments are usually packaged
either in jars or in tubes
May be made of Plastic or glass,May be made of Plastic or glass,
uncolored, colored green, amber, oruncolored, colored green, amber, or
blue, or opaque and porcelain-white.blue, or opaque and porcelain-white.

Ointment jars are filled by forcing the ointment down andOintment jars are filled by forcing the ointment down and
along the sides of the jar to avoid the entrapment of airalong the sides of the jar to avoid the entrapment of air
Ointments prepared by fusion may be poured directly intoOintments prepared by fusion may be poured directly into
the ointment jars for congealing within the jarthe ointment jars for congealing within the jar
Most ointments must be stored at temperatures belowMost ointments must be stored at temperatures below
30°C to avoid the softening and liquefying of the base,30°C to avoid the softening and liquefying of the base,
o to prevent settling of insoluble medicaments to the bottomto prevent settling of insoluble medicaments to the bottom
of the containersof the containers
o to prevent separation of emulsionto prevent separation of emulsion
bases into two phasesbases into two phases

Some tubes co-packaged with special tips when theSome tubes co-packaged with special tips when the
ointment is to be used for rectal, ophthalmic, vaginal orointment is to be used for rectal, ophthalmic, vaginal or
nasal applicationnasal application
Tubes of ointments for topical use are ofTubes of ointments for topical use are of 5 g to 30 g size5 g to 30 g size
TubeTube
ss
The collapsible tubes areThe collapsible tubes are
made ofmade of tin or plastictin or plastic
Tubes of ointments for ophthalmic use areTubes of ointments for ophthalmic use are
most commonly packaged in small, tin ormost commonly packaged in small, tin or
plastic collapsible tubes holding about 3.5 gplastic collapsible tubes holding about 3.5 g
of ointmentof ointment

Tubes are filled by pressure fillers from the open back endTubes are filled by pressure fillers from the open back end
which is then closed and sealedwhich is then closed and sealed
Ointments in tubes are less exposed to air andOintments in tubes are less exposed to air and
contaminants and are more stablecontaminants and are more stable
than ointments packaged in jarsthan ointments packaged in jars
11
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