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Topical Preparations Unit 5
Topical Preparations Unit 5
TOPICAL PREPARATION
The term "cutaneous" refers to the skin. Subcutaneous means beneath, or under, all the layers of the skin
Percutaneous (from the Latin words per, meaning: “through”, and cutis, meaning: “skin”) is the medical term for a route
that penetrates the skin taken by medications, injection needles or other medical devices.
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Introduction
• The topical agents" are those substances, which applied to body surface including applications within the
body cavities that open outside . (e.g. the oral vaginal)
• These are the compound that act locally with skin or mucous membrane mainly by mechanical or physical
manner.
• Topical agents does not absorbed directly into the circulation.
• Compounds have little pharmacological effect.
• The facts of compounds are that when they are applied produces variety of effects like adsorbent,
Ointment
• Ointments are semi-solid dosage forms that are widely used in medicine for treating various skin
conditions. These are made by combining a drug or a combination of drugs with a base or vehicle, which
is typically a mixture of petrolatum and mineral oil.
• Example of ointment: Mupirocin Ointment IP 2% w/w, Betamethasone valerate and Salicylic acid skin
Ointment, etc.
Advantage
• Enhanced Drug Delivery: Ointments are often used to deliver drugs to the skin because they can
penetrate the skin more effectively than other topical formulations, such as creams or lotions. This allows
the drug to be absorbed more quickly and effectively, resulting in faster and more complete healing.
• Long-lasting Effects: Ointments have a longer duration of action than other topical formulations. This is
because they remain on the skin for a longer period of time, allowing the drug to be absorbed more
slowly and providing sustained release of the active ingredient.
• Protection: Ointments form a protective barrier on the skin that can help to prevent further damage or
infection. This is particularly useful in treating conditions such as burns or open wounds, where the skin is
vulnerable to infection.
• Minimal Irritation: Ointments are generally less irritating to the skin than other topical formulations, such
as creams or lotions. This is because they contain fewer preservatives and additives that can cause skin
irritation.
• They are easy to handle than the bulky liquid dosage form
• They are chemically more stable than liquid dosage form
• They are directly applied to the target area avoiding the other body parts
Disadvantage
• Greasy Texture: Ointments have a greasy texture that can make them uncomfortable to use. This is
particularly true for people with oily or acne-prone skin, who may find that the ointment clogs their pores
and exacerbates their condition.
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• Staining: Ointments can stain clothing and bedding, which can be inconvenient and unsightly. This is
particularly true for ointments that contain strong dyes or pigments.
• Limited Use: Ointments are not suitable for all skin conditions. For example, they may not be effective in
treating conditions that require the active ingredient to be absorbed quickly into the skin, such as acne.
• Allergic Reactions: Some people may be allergic to the ingredients in ointments, which can cause skin
irritation, itching, or a rash. This is particularly true for people with sensitive skin or those who have a
history of allergic reactions.
• They are bulkier than the solid dosage form
• They are less stable than the solid dosage form
2. Absorption Bases: Absorption bases are ointment bases that are designed to be absorbed into the skin.
They are made up of mixtures of hydrophilic and lipophilic substances, such as lanolin, beeswax, and
petrolatum. Absorption bases are ideal for use in wet skin conditions, such as weeping eczema, as they
absorb the excess moisture from the skin.
Advantages
• Compatible with most of the medicaments
• Absorb large quantity of water or aqueous substances
• Relatively heat stable
• Easily spreadable
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3. Emulsion Bases:
i) Water-in-Oil Emulsions(W/O): Water-in-oil emulsions are ointment bases
that contain a mixture of water and oil. They are designed to be used on wet
or exudative skin conditions, such as weeping eczema or dermatitis. They
provide a cooling and soothing effect and are easily spreadable.
Ex- Sulfur and zinc ointment ii) Oil-in-Water Emulsions: Oil-in-water emulsions are ointment bases
that contain a mixture of oil and water. They are ideal for use on dry skin conditions and provide a
moisturizing effect. They are easily absorbed into the skin and do not leave a greasy residue. Ex-
Vanishing cream
Advantage
• Miscible with exudates from lesions
• Does not interfere with skin function
• Good contact with skin because of surfactant content • High cosmetic acceptability.
• Easy removable from the hair.
Disadvantages
• W/o emulsion greasy and sticky
• Its acceptance is less
• Difficult to remove from body and clothing
4. Water-Soluble Bases(Greaseless base): Water-soluble bases are ointment bases that are composed of
water-soluble polymers such as polyethylene glycol. They are ideal for use in ointments that require easy
washability and for delivering water-soluble drugs.
Ex-
i) Carbo waxes 200,300…1500. (For viscous liquids)
ii) Carbo waxes 1540, 3000.. 6000(For Viscous solids
iii) Pectin, Tragacanth & Cellulose derivatives (Form
plants)
iv) Gelatin (Animal)
v) Silica Gel, Bentonite (Chemical)
vi) For low viscosity - Glycerin, Glyceryl mono
stearate.
5. Combination Bases: Combination bases are ointment bases that combine two or more types of bases to
provide a synergistic effect. For example, a combination of hydrocarbon and absorption bases can be
used to provide both occlusive and absorbent properties.
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Preparation of ointments
i) Trituration
ii) Fusion
iii) Chemical
reaction
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iv) Emulsification
1. Trituration
Method
Widely used method:-
• For extemporaneous preparation of ointments.
• When the base is soft and medicament is solid insoluble
• Small amount of liquid to incorporated in the base
Advantage- Involves mixing as well as size reduction
Procedure:
i) Reduce the solid medicament to fine powder ii) Medicament is mixed with small amount of base on
ointment slab with a stainless steel spatula until a homogeneous product is formed.
iii) Add remaining quantities of base with uniform mixing iv) Incorporate any liquid ingredient if present
(mortar and pestle to be used in case of large quantity of liquid)
2. Fusion method –
Suitable when ointment base contains number of solid ingredients of different melting points.
Procedure:
i) Ointment base are melted in decreasing order of their melting point. ii)
Highest melting point should be melted first, low melting point next.
iii) This avoids over heating of substances of low melting point iv)
Incorporate medicament slowly to the melted mass
v) Stir thoroughly until mass cools down and homogeneous product is formed.
vi) Liquid ingredients or aqueous substance should be heated to the same temperature as the
melted bases before addition.
vii) If not, wax or solids will cool down quickly and get separated Precautions:
• Strring is done continously- homogeneous mass
• Vigorous stirring should be avoided to prevent entrapment of air
• Rapid cooling should be avoided to get a uniform product.
• To remove the dust or foreign particles strain through muslin cloth
3. Chemical reaction method
Preparation of some ointment involves chemical reactions
Eg – (a)Iodine ointment (iodine free form)
(b)Iodine ointment (iodine combined form with ointment base)
a) Ointments containing free iodine
• Iodine is slightly soluble in fats and vegetable oils.
• Readily soluble is potassium iodide solution in water due to formation of polyiodides (KI.I2, KI.2I2
,KI.3I2)
• Poly iodides are readily soluble in water, alcohol and glycerin.
• These solution may be incorporated with the absorption type ointment base.
b) Ointments containing combined iodine
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• Fixed oils and many fats obtained from vegetable and animal sources contain unsaturated
constituents
• Iodine combines with double bonds
• Free iodine is not available, So ointments appear dark, greenish black in colour
• Leaves no stain when rubbed into the skin, Hence known as non- staining iodine ointment
4. Emulsification method
i) Fats, oils and waxes are melted together to a temperature of 70oC.
ii) Aqueous solution of the heat stable, water soluble compounds is also heated to the same
temperature.
iii) Solution is slowly added to the melted bases, with continuous stirring until cool.
Emulsifying agent is needed to make a stable emulsion
• Water soluble soaps are commonly used as emulsifier for semisolid o/w emulsions.
• Combination of triethanolamine stearate soap and cetyl alcohol is used in o/w emulsion •
Bees wax and divalent calcium ions used in w/o emulsion.
Packaging of ointment
a) Ointment jars
•Made of colorless or colored glass
•Amber colored for light sensitive
preparation
• with screw caps
• with impermeable liners
b) Collapsible tubes
•Made of tin or plastic
•Supplied with the applicator
Storage
• Store in a well closed container and in cool place
• Protect from high temperature/ direct sunlight.
• Prevent the loss of volatile constituents
• High temperature soften or melt base
• Separation of phases may take place
Labeling:
“ FOR EXTERNAL USE ONLY ”
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CREAMS
Introduction
• In pharmacy the term ‘cream’ is used for external preparations.
• Creams are viscous semi-solid emulsions for external use.
• Medicaments can be dissolved or suspended in creams.
• A cream may be ‘water-in-oil’ or ‘oil-in-water’ depending on the emulsifying agent used.
• A cream is always miscible with its continuous phase.
Definition
According British Pharmacopoeia (BP)-Creams are formulated to provide preparations that are
essentially miscible with the skin secretion. They are intended to be applied to the skin or certain
mucous membranes for protective, therapeutic or prophylactic purposes especially where an occlusive
effect is not necessary.
Advantage of Cream
• They gives prolong contact in their site of application than any other
pharmaceutical semi-solid dosage forms
• Injured area can be dried quickly by creams than other semi-solid preparations
• Non-irritating when applied to the skin
• Easily water washable. Easy to wipe away
• Less greasy compared to ointment
• Easy to spread on the skin surface
Disadvantage
• Stability is not good as ointment
• They are less hydrophobic than other semi-solid preparation therefore risk of contamination is high.
• Possibility of allergic reaction
• Poor permeability of some drugs through the skin
Ideal properties
• It should liquify at body temperature
• It should penetrate the epidermis via natural opening
• Its viscosity should be low enough to permit easy spreading
• It should be non-toxic
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Classification of creams
Creams can be classified on various bases
1. According nature or type of emulsion
a) O/W emulsion type cream
• Dispersed phase-oil Continuous phase- water
• They are less greasy and more easily washed off using water.
• eg: Fluocinolone Acetonide Cream, Vanishing cream, foundation cream
b) W/O emulsion type cream
• Dispersed phase- Water Continuous phase- Oil
• More difficult to handle.
• e.g.: Moisturizing & Cold cream, Cleansing lotion, cleansing cream, cleansing milk, cold cream or
moisturizing cream or cold cream
2. Cosmetic cream- all creams except medicated cream
3. Medicated cream-
• They contain active pharmaceutical ingredient
• Ex-
i) Cetrimide cream used as antiseptic ii) Zinc
oxide cream used as astringent iii)
Hydrocortisone cream used to treat rashes
4. According to function. Ex- cleansing, foundation, massage cream etc.
5. According characteristic properties. Ex -cold cream, vanishing cream etc.
6. Other creams
• All purpose cream and general cream
• Night cream or massage cream
• Skin protective cream
Some creams
i) Cold cream
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• It is W/O emulsion cream which when applied to skin, a cooling effect is produced due to slow
evaporation of water present in the emulsion
• Cold cream are O/W type of emulsion but after application on the skin, sufficient water evaporates
to permit phase inversion to W/O emulsion
b)
Liquefying type
• This type of creams consist of a mixture of oil and water which are translucent in nature.
• They are anhydrous creams with thixotropic character i.e., they liquefy when applied on skin.
• These are applied to the face to provide a smooth emollient base for the application of facial
makeup.
• Foundation creams act as skin protectives to prevent the damage caused by environmental
factors like
sun, wind, dirt etc.
Vanishing cream
Foundation cream
• Cold and dry winds are responsible for chapping(फटन ) of the skin. Chapping occurs due to loss of
moisture from the skin, which is also associated with cracking.
• Water is sufficient to treat the dryness of the skin, but evaporation of water takes place rapidly, which
again, makes the skin dry and no emollient effect is produced.
• In case, if hands are immersed in water for longer time then abnormal hydration takes place. This
hydration will lead to swelling of cells in stratum corneum, which ultimately results in rupturing of cells.
Hence, hand and body creams are formulated with suitable emollient, which not only make water
available but also regulates the water take-up by the cells of stratum corneum.
vii) All-Purpose creams/
sports creams
• These creams are used by sport persons and also by people who do outdoor activities. Hence, they are
called as sport creams.
• They are oily in nature but non-greasy type.
• They provide protective film to the skin.
• They make the rough surfaces of the skin smooth.
When it is applied in more quantity, it acts as
(a) Nourishing agent
(b) Protective cream to protect the skin from sunburn.
(c) Night cream.
(d) Cleansing cream
When it is applied in less quantity, it act as
(a) Hand creams
(b) Foundation creams
Formulation componenet
• Antioxidant ex.-TBHT, Ascorbic acid.
• Base- ex. White petrolium, Lanolin, cholesterol.
• Buffer- ex. Citrate buffer ,phosphate buffer.
• Chelating Agents- ex. EDTA , Citric acid.
• Emulsifying Agent- ex. Detergent ,Cetostearyl alchohol.
• Humectant- ex. Glycerin,propylene glycol, PEG.
• Permeation enhancer ex. Ethanol , oleic acid, PEG
• Preservative – ex. Benzoic acid,phenyl ethyl alcohol, Methylparabens, propyl parabens, phenols, benzoic
acid, sorbic acid
• Thickening Agent- ex. Cellolose, pectin ,carbopol.
• Fragrances- ex. Lavender oil,rose oil, lemon oil
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Evaluation of creams
1. Determination of pH
2. Primary skin irritation test
3. Visual appearance
4. Viscosity in cps v/s shear rate in sec-1.
5. Spreadability
6. Stability studies
7. Reheological studies
8. Thermal behavior
9. Saponification value 10. Acid value
11. In-vitro method(Skin is excised)- Tests are carried out to know the performance of the products.
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a) Tensile strength tester-This method is useful for determining the tensile property of the excised
stratum corneum of the skin. It provides information on the water content present in stratum
corneum and also acts as a screening device for moisturizing ingredients.
b) Hargen's Gas Bearing Electro dynamometer (GBE)- This instrument is helpful in determining and
monitoring the viscoelastic behavior of the skin. It also helps in determining the effects on the skin
by passing it through various treatments. It is used both as in-vitro and in-vivo test.
c) Occlusive potential of ingredients- The occlusive potential of raw materials or ingredients used in the
formulation of skin cream, are determined by knowing the water diffusion rate. Membranes used in
this method can be stratum corneum of neonatal rat or artificial membrane.
d) Gravimetric analytical method.-This method is helpful in establishing relationship between water
content present in stratum corneum and relative humidity
e) Thermal analytical methods- They are used in order to provide information about the effect of
temperature which causes changes in the stratum corneum.
f) Electrical methods- Various electrical properties such as capacitance, impedance and dielectric
constant are measured by electrical methods which provide information about the variations in the
water content present in the stratum corneum of the skin.
12. In-vivo method (skin remain attach to body)- In-vivo methods are helpful in providing information on
hydration or moisturization process of the skin
a) Transpirometry- This method helps in measuring Trans Epidermal Water Loss (TEWL) of the skin
which helps in providing information on moisturizing potential.
b) Skin friction- Damp (slightly wet) skin has high friction surface compared to wet and dry skin.
Investigation of friction surface shows the relation between the effect of hydration on stratum
corneum and process of moisturization. Frictional properties are also related to elastic nature of skin
and helps in evaluating the performance of the product.
c) Sensitivity tests- these tests are performed in order to measure the irritancy, sensitization potential
and phototoxicity of the skin.
i) 21 Day (or 3 Weeks) Cumulative Irritancy Patch test: In this test, the test material is applied
daily on the same site i.e., fore arms of 24 subjects under the occlusive tapes. Then score are
recorded daily. This test is carried out for 21 days or until irritation produced on the fore
arm. This irritation is noted as maximum score. The core ranges from 0-4, where '0' score
indicates no visible reaction on typical erythema (redness of the skin dale to dilation and
congestion) of capillaries) and '4' score indicates erythema with edema and vesicular erosion
(erosion of vesicles).
ii) Draize-shelanski repeat-insult Patch Test: This test is carried out on 100 individuals to
measure the extent of sensitization and irritation caused by the product to the skin. The test
material is repeatedly applied on the same site under occlusion for 10 alternate days. After a
gap of 7 days, test material is again applied to a new site only for 24 hours. The scores are
recorded after the removal of occlusive tape. Then the score is again recorded after 24
hours. The score ranges from 0-4, where '0' score indicates no visible reaction on erythema
and '4' score indicates erythema with edema and vesicular erosion.
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iii) Kligman “Maximization" Test: This test is used to measure sensitizing potential of the
product, when it comes in contact with the skin. The test material is applied on the site by
using an occlusive tape for a period of 48 hours. Then the site is treated with sodium lauryl
sulfate solution on each exposure under occlusion. After a gap of 10 days, the test material is
again applied on a new site under occlusion for a period of 48 hours, which is then treated
with solution of sodium lauryl sulfate.
d) Scanning electron microscopy (SEM)
e) Optical microscopy and macro photography.
:.
•
•
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PASTE
Introduction
• Pharmaceutical paste are semisolid dosage form that contain one or more drug and additives intended
for topical application
• The term applied to ointment which contains high percentage of insoluble solid (20% to 50 %) which are
finally dispersed into suitable vehicle. As they contain larger amount of finely dispersed solid so they are
thicker and stiffer.
• Paste form protective coating and mainly used as antiseptic, protective or smoothing dressing.
• Paste adhere well to skin and are benefit in treatment of chronic lesions
• Ex- Zinc oxide paste
Characteristics of paste
• Pastes are stiffer than other semisolid dosage forms such as ointments and creams hence they remain
stable at site of application.
• Because of high powder contents pastes are porous; hence, perspiration can escape.
• They do not interfere with the non-infected areas of the skin.
• These are considerably less greasy when compared to ointments.
• Most of the pastes are unsuitable for treating scalp conditions because they are difficult to remove from
• They are mostly applied over moist lesions as they possess good adhesive property towards the skin.
the hair.
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2. Water miscible bases- water miscible bases include emulsifying ointments and emulsifying wax. Ex-
3. Water soluble bases- water soluble bases are prepared from low and high molecular weight polyethylene
glycols (PEG). Ex-
Methods of preparations
Pastes are prepared by trituration and fusion methods.
• Trituration method is used when the base is liquid or semisolid.
• Fusion method is used when the base is semisolid/solid in nature.
1. Trituration method (same as ointment )
Compound Zinc Paste is prepared by both fusion and trituration method.
Procedure:
i) Zinc oxide and starch powder are passed through sieve No. 180.
ii) Soft paraffin is melted on a water bath.
iii) Required amount of powder is taken in a mortar, triturated with little melted base until smooth and
gradually rest of the base is added.
2. Fusion method (same as ointment)
Zinc and coal tar Paste B.P.C. is prepared by fusion method.
Method 1
The components are melted in decreasing order of their melting point i.e., higher M.P. the substance should
be melted first. The medicament is added slowly in the melted ingredients and stirred thoroughly until the
mass cools down.
Method 2
All the components are taken in subdivided state and melted together.
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:
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GELS
Introduction
• Pharmaceutical gels are transparent or translucent, non-greasy semisolid preparations that contain one
or more medicines in a hydrophobic and hydrophilic base.
• Gels are made using suitable gelling agents, and may also contain antioxidants, preservatives, and
stabilizers.
• Gel can be single phase or biphasic system
• Gels and jellies both are semi-solid system dosage form but jellies have soften consistency than gels.
• Gels are formed by using synthetic polymers such as carbomer 934 & cellulose such as
hydroxypropylcellulose & hdroxypropylmethylcellulose.
• Tragacnth, pectin, agar natural gums are used in the formulation of gels.
• As per NF, six polymers are used for gel formulation. Those are followings,
Carbomers 910
Carbomer 934
Carbomer 934P
Carbomer 940
Carbomer 941 And Carbomer
1342
• Carbomer 940 produce highest viscosity between 40,000 & 60,000 centipoises in 0.5% aq. Solution.
• Gel may thicken on standing, forming a thixotrope(thixotropic behaviour) and must be shaken before use
to liquefy the gel.
• Gel contains drug substance with water.
• Also contain solvents such as, alcohol or propylene glycol.
• Antimicrobial preservatives used in gel formulation such as, methylparaben, propylparaben etc.
• It also contains stabilizers e.g. edetate disodium (EDTA).
• Medicated gels prepared for administration by various routes for eye, nose, vaginal & rectum.
Properties of Gels
i) Ideally, the gelling agent must be inert, safe and cannot react with other formulation constituents.
ii) The gelling agent should produce a sensible solid-like nature at the time of storage which is easily broken
when exposed to shear forces produced by squeezing the tube, trembling the bottle or at the time of
topical application.
iii) It should have suitable anti-microbial agent.
iv) The topical gel must not be sticky.
v) The ophthalmic gel must be sterile.
vi) The apparent viscosity or gel strength increases with an increase in the effective crosslink density of the
gel. However, a rise in temperature may increase or decrease the apparent viscosity, depending on the
molecular interactions between the polymer and solvent.
Advantage
• Gels are used to achieve optimal cutaneous and percutaneous drug delivery.
• They can avoid gastrointestinal drug absorption difficulties caused by gastrointestinal pH.
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• Gels are having property to avoid enzymatic activity and drug interaction with food and drinks.
• They can substitute for oral administration of medication when the route is unsuitable.
• They can avoid the first pass effect, that is, the initial pass of drug substance through the human body.
• They avoid systemic and portal circulation following gastrointestinal absorption.
• Gels are not deactivated by liver enzymes because the liver is bypassed.
• They are non-invasive and have patient compliance.
• They are applied over skin for slow and prolonged absorption.
• Gels have also been applied in pharmacy to some viscous suspension for oral use for example Aluminum
hydroxide gel.
• They have localized effect with minimum side effects. Disadvantages:
• Gels have possibility of allergenic reactions.
• Enzyme in epidermis may denature the drugs of gels.
• Drugs of larger particle size do not absorb through the skin.
• They have poor permeability of some drugs through the skin.
• Selection of area to be examined carefully during application of gels.
• Gels which are used for the introduction into body cavity or the eyes should be sterilized.
• They may cause application side reactions.
• They may cause skin allergy during application.
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Classification of gels
A. According to solubility of jelling agent into dispersion liquid, gels are classified into two class
1. One phase or Monophasic gel system- two types
• When the gelling agent is soluble in dispensing liquid, is called single phase gel system because no
definite boundaries exist between the dispersed molecule and the liquid
• Example- hydrophilic polymers in liquid
• Clear in appearance
• Rheology-Psuedoplastic flow(a fluid that increases viscosity as force is applied)
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• Single phase gel use high molecular weight hydrophilic polymers as gelling agent. Ex-Carbomers
• According to dispersing medium, one phase gel system is further classified into following two class a)
hydrogels and b) organogels
2. Biphasic or two phase gel system
• When Gelling agent is insoluble in dispersion liquid is called biphasic gel system. Ex- Aluminum gel and
Bentonite gel, Milk of magnesia (Magnesia magma) in that gelatinous precipitate of magnesium
hydroxide.
• frequently called as magma gels or inorganic gels
• They show thixotropic flow (The viscosity of thixotropic solutions (like that of pseudoplastic solutions)
decreases as the rate of shear increases, but it changes in a time-dependent manner rather than
instantaneously.)
• Turbid in appearance
2. Xerogels
• Xerogels are a type of solid-formed gels, which are being prepared through drying slowly at the room
temperature with an unconstrained shrinkage
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• Xerogels usually retain high porosity (15–50%) and enormous surface area (150–900 m2/g), along with
very small pore size (1–10 nm).
• When solvent removal occurs under supercritical conditions, the network does not shrink and a highly
porous, low-density material known as an aerogel is produced.
• E.g., Tragacanth ribbons, β-cyclodextrin, dry cellulose and polystyrene, gelatin sheets and acacia tears.
• Uses – in DDS
• The liquid can be, for example, an organic solvent, mineral oil, or vegetable oil.
• These systems are based on self -assembly of the structuring molecules.
Uses
• In pharmacy used as drug carrier for TDDS.
• In cosmetics for application & stability and food industry.
• Drug concentration
• pH
• Solubility
• Surfactant
Component of gels
1. Gelling agents
Natural polymer Semi-synthetic polymer Synthetic or Acrylic polymer
Acacia Micro-crystalline HPMC Carbomers
Pectin Carboxymethylcellulose (CMC) Polyacrylic acid
Starch Na. CMC
Tragacanth
Gelatin
Sodium alginate
Clays
Carageenan
Alginic acid
(=algin=seaweed)
2. preservatives- Ex-methyl and propyl parabens, benzoic acid, chlorocresol, Chlorhexidine acetate 3.
hygroscopic substance-
After applying the gel on skin , water quickly evaporate from gel, leads to formation of flakes on skin. To
prevent this hygroscopic agent is used Ex- glycerin, Propylene, Sorbitol
Chelating agent These agent inactivate heavy metals by forming complex with them, hence prevent
degradation of medicine sensitive to heavy metals.
Ex- EDTA
Methods of formulations
There are three methods of formulation
i) Fusion Method ii)
Cold Method iii)
Dispersion Method
1. Fusion method
• In this method various waxy materials employed as gellant in non polar media.
• Drug was added when waxy materials melted by fusion.
• Stirred slowly until uniform gel formed.
2. Cold method
• Water was cooled to 4-10oC and placed it in mixing container.
• Gelling agent was slowly added and agitating until solution is complete.
• Maintained temperature below 10oC .
• Drug is added in solution form slowly with gentle mixing
• Immediately transfer to container & allow to warm to room temperature where upon liquid becomes
clear gel.
3. Dispersion method
• Gelling agent was dispersed in water with stirring at 1200 rpm for 30 min .
• Drug was dissolved in non-aqueous solvent with preservative.
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• This solution was added in above gel with continuous stirring. General method of preparation
• Generally the water soluble excipients are firstly dissolved in vehicle, in a mixing vessel by using
mechanical stirrer.
• To prevent aggregation, add hydrophilic polymer to the stirred mixture slowly.
• Stirring is continued until the dissolution of the polymer has occurred.
• The excessive stirring results in entrapment of air. The mixing rate must not be extreme or a mixing
vessel may be used to which a vacuum may be pulled, to prevent the entrapment of air.
Evaluation of gels
• pH determination
• Drug content
• Viscosity
• Spreadability
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LINIMENTS
Introduction
• It is dosage form for external use and a fat liquid or gelatinous mass, which melt at body temperature
• Liniments are solutions or mixtures of various substances in oil, alcoholic solutions of soap, or emulsions
and may contain suitable antimicrobial preservatives.
• Alcohol helps in penetration of medicament into the skin and also increases its counter irritant and
rubefacient action.
• In oily liniments arachis oil is commonly use which spreads more easily on the skin. Use of soap may ease
application.
• These preparations that may be liquid or semi-liquid are intended for external application and should be
so labeled.
• They are rubbed onto the affected area; because of this, they were once called embrocation.
• They are applied with friction and rubbing of the skin, the oil or soap base providing for ease of
application and massage.
• only suitable for external use
• Emulsions liniment or that contain insoluble matter must be shaken thoroughly before use
• Liniment should NOT be applied to skin that is bruised/Broken because excessive irritation might occur.
• Containers:- color fluted bottle in order to distinguish it from preparations meant for internal use.
• Labeling:- For External Use only, shake well before use and with a warning of not to be applied on broken
skin or
open wound.
• Storage:- air-tight containers in a cool place
Advantage
i) Medicinal substances of the liniment is well absorbed by the skin ii) High bioavailability iii) Absorbed
quickly by the skin iv) Cheap and easy to manufacture
v) Compared with ointments liniments better applied to the skin
vi) leaving fewer traces on skin and clothing of the patient compared to ointment
Disadvantages Of Liniments
i) Low stability
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Uses
• Antipruritic - used to relieve itching
• Astringents - causes biological tissue to contract
• Emollients - products that soften skin or treat dry skin
• Analgesics
• Rubefacient-A medicine for external application that produces redness of the skin. e.g. by causing
dilation of the capillaries and an increase in blood circulation. Substance that causes redness (Rubar)
• Counterirritant- A medicine applied locally to produce superficial inflammation in order to reduce deeper
inflammation.
Classification
Liniment may be classified as
A. On the basis of therapeutic activity:
i) Analgesic,
ii) Irritants,
iii) Anti-inflammatory,
iv) Astringent,
v) Fungicidal
B. On the basis of the dispersion medium liniments can be divided into : i)
Fatty Liniments
• Dispersion environment include fatty oils or fat-like substance (lanolin).
• The most commonly used medium is sunflower, linseed, castor oil.
• Medical substances can include both liquid (chloroform, turpentine, ether, tar) and
powder (camphor, menthol, novocaine, dermatol, etc.).
ii) Alcohol liniments-
Liniment alcohol contain alcohol and liqueurs (usually brandy peppers), as well as various
medicinal substances.
iii) Soap-alcohol liniments-
Soap-alcohol liniments, contained as a dispersion environment alcoholic solutions of soap.
They may be liquid (if they contain potassium soap) or jelly (if they contain sodium soap) When
rubbing the skin cause emulsification of sebum and rapidly absorbed into the skin, along with
drugs.
C. On the basis of disperse systems liniments can be divided into:
i) Homogenous: solvents and extraction ( oil extracts of various parts of medicinal plants) ii)
Heterogeneous: suspension liniments , emulsion liniments and combined
Preparation
• The vehicle should be selected for the type of action desired (rubefacient, counterirritant, massage) and
also on the solubility of the desired components in the various solvents
• Prepared in the same manner as solutions, emulsions, or suspensions
• Ex-
i) White liniment
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Procedure-
i) Mix oleic Acid with turpentine oil ii) Dilute ammonia solution with 45ml of water,
previously warmed. iii) Add to the oily solution and shake to form emulsion iv)
Dissolve Ammonium Chloride in water v) Add the emulsion
Preparation
Place the cottonseed oil into a suitable dry flask or bottle, heat on a steam bath, add camphor and
stopper the container securely. Agitate to dissolve the camphor without further heating.
Uses: Mild counterirritant for inflamed joints, sprains, rheumatism and in other inflammatory
conditions such as cold in throat and chest, in infants and children.
Remarks: The liniment should never be prepared in an open dish, as much of the camphor will
volatilize
Preparation:
Dissolve camphor and rosemary oil in alcohol, add the soap and sufficient quantity of purified water to
measure 1000ml. Agitate to dissolve the soap, set aside in a cool place for 24 hours and filter.
Uses: Local irritant, mild rubefacient, and weak local anesthetic for sprains, bruises and rheumatism. It
also forms the basis for other liniments.
Remarks: The official hard soap should be used; soap made from animal oils will cause gelatinization. If
soap having from bar soap are used, dry thoroughly and then run through a mill or grater.
v) Chloroform Liniment, NF
Other Name: Linimentum Chloroformi Formula:
Chloroform 300 ml
Camphor and Soap Liniment 700 ml
To make 1000 ml
LOTION
Introduction
• A lotion is a low- to medium-viscosity medicated or nonmedicated topical preparation, intended for
application to unbroken skin without friction.
• Applied to skin with absorbent(cotton).
• It is used for cooling, soothing or protective purpose.
• Antiseptic action:- e.g. calamine lotion.
• Alcohol is sometimes included in aqueous lotions for its cooling and soothing effect. E.g. salicylic acid
lotion
• Solid particles incorporated in lotions should be in a finely divided state to avoid grittiness.
• Most lotions are o/w emulsions, but w/o lotions are also formulated.
• The key components of a lotion are the aqueous and oily phases, an emulsifying agent to prevent
separation of these two phases
• A wide variety of other ingredients such as fragrances, glycerol, petroleum jelly, dyes, preservatives, and
stabilizing agents are commonly added to lotions for improved organoleptic and preservation
characteristics.
• Lotions can be used for the topical delivery of medications such as antibiotics, antiseptics, antifungals,
corticosteroids, antiacne agents, and soothing/protective agents (such as calamine).
Noncomedogenic(that do not block the natural pores of the skin) lotions, products are recommended for
use on pimples or acne-prone skin. These lotions are also termed as nonocclusive. Thus, they may
reduce acne or reduce the incidence of pimples.
• The same drug substance can be formulated into a lotion, cream, and ointment. Creams are the most
convenient of the three but are inappropriate for application to regions of hairy skin such as the scalp;
whereas a lotion is less viscous and may be readily applied to these areas. Many medicated shampoos
are, in fact, lotions. Lotions also have an advantage that they may be spread thinly compared to a cream
or ointment and may economically cover a larger area of skin.
• Containers:- Color fluted bottles in order to distinguish them from preparations meant for internal use.
• Labeling:- for external use only, shake well before use.
• Storage:- Store in well filled, well closed in an air tight container in cool and dry place.
Properties of Lotions
• Most lotions are water or water alcohol systems; a small amount of alcohol is added to help dissolve the
active ingredients and accelerate the evaporation of the solvent from the skin surface.
• Most acne lotions are water alcohol that evaporates quickly, they are not sticky and dry.
• Emulsion type lotion is usually not dry, depending on water content (higher water and/or less oil will
make drying drier).
• Lotion is easy to spread on large areas.
• Lotion is suitable for hair area, prone to folliculitis / acne skin, trigeminal region.
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Advantage
i) Evaporate well ii) Good for large areas iii) Good for
hairy areas iv) Drugs from the lotion are well absorbed
by the skin
v) Drugs in the form of lotion have higher bioavailability
vi) Lotions have long term stability vii) Lotions are non-
greasy in nature
viii) Lotion spread on the skin very easily over large area
Disadvantage
i) Alcohol base will irritate or sting ii) Lotion may
clog skin pores and increase acne
iii) During application of lotion care needs to be taken to avoid accidental exposure to eyes iv)
Lotion may accelerate the skin aging
v) Lotion may show systemic side effects
Indication
• Eczema
• Impetigo
• Sun burn
• Dermatitis itching
• Varicose ulcers
• Psoriasis
Some lotions
i) Sunscreen lotion :- Sunscreen lotion absorbs or reflects the harmful UV rays and protects the skin.
ii) Body lotion :- These lotions are used to stop moisture leaving the skin and keep the skin soft, smooth and
hydrated
iii) Hair lotion :- These lotions are used on hair to improve and stimulate the hair follicles.
iv) Face lotion :- These are called bleaching lotions which alter the colour of the skin v) Humectant lotion :- This
lotion keeps the skin hydrated.
v) vi) Astringent lotion :- It is dual purpose lotion that cleanses and moisturises the face it helps to remove
makeup residues, dirt, dust and other impurities from skin
Often leaves a residue on skin Absorbed into the skin without leaving residue Ex- Turpentine liniment
Ex- calamine lotion, bentonite lotion Difference between cream and lotion
Preparation
• Lotions are prepared by triturating the ingredients to a smooth paste and then adding the remaining liquid
phase with trituration.
• Example
i) Calamine lotion I P
Calamine- 150g
Zinc oxide- 50g Bentonite- 30g
Sodium citrate- 5g
Liquified phenol- 5ml
Glycerine- 50ml
Rose water up to 1000ml
Method- Dissolve the sodium citrate in rose water. Triturate the calamine, zinc oxide and bentonite in a solution
of sodium citrate . Add the liquified phenol. Add the glycerine. Add purified water in sufficient quantity to produce
the required volume. Transfer the lotion to a bottle, cork, label and dispense. Ingredients Calamine –
• ZnO(98%) + Fe2O3 (2%)
• Fe2O3:- imparts color and it is irritant. So applied to only over intact skin, not on open wound
• ZnO :- Antiseptic, astringent, Protective and soothing agent. It is Substances that precipitate proteins but
do not penetrate cells, thus affecting superficial layer only.
Bentonite
• Hydrated aluminium silicate.
• When water is added it, swells up to give a gel- like but non-viscous consistency.
• It acts as suspending agent and reduce viscosity.
• It helps to make the lotion uniform.
Glycerin
• Hygroscopic in nature.
• Prevents drying of lotion, so lotion remains at the site of application for a longer time.
• Also antiseptic and emollient (oily substance). Sooths and softens the skin.
• Forms an occlusive film over skin and prevent evaporation, thus restores elasticity of cracked and dry
skin.
Precaution
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Should not be applied on wounds or injured areas because it precipitates proteins and form a layer
which prevents healing.
Lactocalamine
• It is market preparation which contains casein and phenol besides the normal constituents.
• Casein acts as soothing agent, while phenol acts as a preservative and antiseptic
Quality control test
i) pH test ii) physical
appearance test iii) viscosity
test iv) Assay
v) Irritancy test
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Uses of Suppositories:
• Suppositories are great for patients with constipation. There are various types of laxative suppositories like
bisacodyl suppositories, glycerin suppositories, etc.
• Rectal suppositories are very useful for hemorrhoids and piles patients. It reduces swelling and discomfort.
• Vaginal and urethral suppositories are great for fungal infection in the vagina and urethra. (clotrimazole,
miconazole, etc are used as a drug.)
Advantages of Suppository:
• It's easy to use for those patients, who are unable to take oral medication. (like unconscious patients,
children)
• Does not cause nausea and vomiting due to gastric irritation as in case of oral therapy
• Increase the bioavailability of drugs.
• Very useful to get local effects.
• It avoids the first-pass metabolism.
• It provides rapid action.
• Beneficial for patients suffering from severe vomiting
• Can be administered to unconscious patients
• Oral intake restricted before surgery
• Can be used as a targeted drug delivery system
• Localized action with reduced systemic distribution
• Get to the site of action with a lower dose reducing systemic toxicity
• Highly beneficial in hemorrhoids or vaginal infections
• Prolonged drug action achieved
• Best for vaginal and rectum fungal infection.
• Convenient for those drug causes GIT irritation, nausea, vomiting, destroyed by the hepatic circulation,
stomach pH, enzymes etc Disadvantages of Suppository:
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Classification of suppositories:
A. There are 5 types of suppositories according to the route of administration i)
Rectal suppositories-
• Rectal suppositories for adults weigh 2 gm and are torpedo
shape.
• Children's suppositories weigh about 1 gm ii) Vaginal
suppositories (Pessaries)-
Vaginal suppositories or Pessaries weigh about 3-5gm and are molded in globular or oviform shape or
compressed on a tablet press into conical shapes.
iii) Urethral suppositories (Bougies)- they also called bougies and are pencil
shape.
Those intended for males weigh 4 gm each and are 100-150 mm long. Those for females are 2 gm each
and 60-75 mm in length.
iv) Nasal suppositories (Buginaria)-
• They are also called nasal bougies or buginaria meant for introduction in to nasal cavity.
• They are prepared with glycerogelatin base.
• They weigh about 1 gm and length 9-10 cm.
v) Ear suppositories (Aurinaria)-
• They are also called Aurinaria and meant for introduction into ear.
• Rarely used
• Theobroma oil is used as base.
• Prepared in urethral bougies mould and cut according to size.
ii) Layered Suppositories- Layered suppositories are made with different drugs in different layers to avoid
incompatibility between those drugs.
iii) Coated Suppositories-Coated suppositories made with free unsaturated fatty acids, polyethylene glycol,
etc. for their smooth lubricating properties.
iv) Capsule Suppositories- Capsule suppositories are made with soft gelatin in various sizes and shapes. It is
filled with solid, semisolid, and liquids drugs.
Suppository Bases:
Suppository bases are those materials that maintain their shape and solidity. There are various types of bases
like theobroma oil, glycerogelatin base & polyethylene glycol, etc.
Types of Suppository Bases:
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• The automatic mold method is the fastest method for the bulk production of suppositories. All the
processes from mixing, filling, ejection, and molding are totally automatic. Due to high-speed
production, the production output 5000-10000 suppositories per hour. By automatic machine, the extra
materials are collected and re-used after the solidification of the suppositories.
Suppository Molds:
For small-scale production, each suppository molds have the capacity to produce 6 or 12 suppositories.
Industrial or bulk production suppository molds are capable to produce thousands of suppositories in a
single time.
• For automated production, a huge amount of raw materials and storage areas are required
Packaging of Suppositories:
• Normally suppositories are packed one by one in plastic or aluminum foil. Most of the suppositories are
stored in a cold place to maintain their proper size and shape. Refrigeration is required. In the case of
polyethylene glycol suppositories, room temperature is enough for storage, and a refrigerator is not
required.
Testing of suppositories:
1. Uniformity of weight test:
• In this test, the weight measurement is done for those suppositories which are produced in the same
mold. To maintain the uniformity of the weight.
2. Melting Range test:
• Macro-melting range: Here the time is measured that takes for the entire suppository to melt when
immersed in a constant temperature (37 degrees Celcius) in the water bath.
• Micro-melting range: Here the melting range is measured in capillary tubes for the oily or fat base only.