DISPERSED SYSTEMS

LIQUIDS

MDALegaspi 2016

MDALegaspi 2016

DRUGS
defined as an agent intended for use in the
diagnosis, mitigation, treatment, cure, or
prevention of disease in humans or in other
animals (Food, Drug, and Cosmetic Act, 1938)

MDALegaspi 2016

Drug product
means a finished dosage form, for example,
tablet, capsule, solution, etc., that contains an
active drug ingredient generally, but not
necessarily, in association with inactive
ingredients (CFR21)
The term also includes a finished dosage form
that does not contain an active ingredient but is
intended to be used as a placebo.

MDALegaspi 2016

Component
means any ingredient intended for use in the
manufacture of a drug product, including those
that may not appear in such drug product

MDALegaspi 2016

Components of Drug Product:

Except
PLACEBO
w/c do not
contain AI

Active Ingredients
+
Inactive Ingredients

MDALegaspi 2016

Active ingredient (AI)

means any component that is intended to furnish
pharmacological activity or other direct effect in
the diagnosis, cure, mitigation, treatment, or
prevention of disease, or to affect the structure or
any function of the body of man or other animals
The term includes those components that may
undergo chemical change in the manufacture of the
drug product and be present in the drug product in
a modified form intended to furnish the specified
activity or effect.
AKA: Drug Substance or Active
Pharmaceutical Ingredient (API)

MDALegaspi 2016

Inactive ingredient
means any component other than an active
ingredient
AKA: Excipients/ Additives/Pharmaceutical
Adjuncts/Necessities

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Inactive ingredient
are agents used to :

Solubilize
Suspend
Thicken
Dilute
Emulsify
Stabilize
Preserve
Color
Flavor

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DRUG DELIVERY SYSTEM

means of administering drugs as formulated
preparations
formulations which provide a therapeutic amount
of drug to the proper site in the body promptly
and maintain the desired drug concentration

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DOSAGE FORM
Formulation containing a specific quantity of
active ingredient(s)in combination with one or
more excipients

Powders and
Granules
MDALegaspi 2016

Solid

Capsules

based on physical state

Tablets
Solutions
Liquid

Dispersed
Systems
Ointments

Creams
Semisolid
Gels
Gas
TDDS

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LIQUIDS

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SOLUTIONS

Aqueous
solutions

Sweet and other

Viscid Aqueous
Solutions

Non-Aqueous
Solutions

Aromatic water
MDALegaspi 2016

Aqueous Solutions

Aqueous Acids
Diluted Acids
Douches
Enemas
Gargles
Washes

Mouthwashes

Juices

Otic Solutions

Solutions

Nasal Solutions

Irrigation
Solutions

Sprays

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Sweet and
other Viscid
Aqueous
Solutions

Syrups

Honeys

Mucilage

Jellies

Collodions

MDALegaspi 2016

NON-AQUEOUS
SOLUTIONS

Elixirs
Glycerins
Inhalations and
Inhalants
Liniments

Oleovitamins
Spirits

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LIQUIDS

Dispersed Systems

MDALegaspi 2016

Coarse
Dispersion

Fine
Dispersion

Suspensions
Emulsions
Magmas
Gels

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SOLIDS

CAPSULES

MDALegaspi 2016

Hard Gelatin
Capsules (HGC)
Soft Gelatin
Capsules (SGC)

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SOLIDS

TABLETS

Compressed Tablets

MDALegaspi 2016

Multiply Compressed Tablets

Sugarcoated Tablets
Film-coated Tablets
Gelatin-coated Tablets
Enteric-Coated Tablets
Buccal and Sublingual Tablets
Chewable Tablets
Effervescent Tablets
Molded Tablets
Tablet triturates
Hypodermic Tablets
Dispensing Tablets
Immediate-Release Tablets

Instantly Disintegrating or Dissolving Tablets

Extended Release Tablets
Vaginal Tablets

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Classification of Dosage Form

By Physical State

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Dispersed Systems
types of liquid preparations containing
undissolved or immiscible drug distributed
throughout a vehicle
In these preparations, the substance distributed
is referred to as the dispersed phase, and the
vehicle is termed the dispersing phase or
dispersion medium

Suspensions
Coarse
Dispersion
MDALegaspi 2016

Emulsions
Dispersed
Systems

Magmas
Fine
Dispersion

Gels

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Coarse Dispersion
Dispersions containing coarse particles, usually
10 to 50 m
consist of at least two phases
dispersed or internal phases (one or more )
dispersion medium or vehicle (continuous or
external phase )

Preparations:
suspensions
emulsions

MDALegaspi 2016

Fine Dispersion
Dispersions containing particles of smaller size
(0.5 to 10 m)
Preparations:
Magmas
Gels

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Dispersed Systems: Coarse Dispersion

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SUSPENSIONS
defined as preparations containing finely
divided drug particles (the suspensoid)
distributed somewhat uniformly throughout a
vehicle in which the drug exhibits a minimum
degree of solubility

MDALegaspi 2016

SUSPENSIONS
are two-phase system consisting of an
undissloved or immiscible material dispersed in
a vehicle (solid, liquid, or gas).
coarse dispersion containing finely divided drug
particles distributed uniformly throughout the
vehicle in which the drug exhibits a minimum
degree of solubility
requires suspending and dispersing agents to be
diluted and agitated with a specified quantity of
vehicle, usually purified water

MDALegaspi 2016

SUSPENSIONS
the particle diameter is 1 to 50 m
Availability:
Oral Suspension are available as dry
powders intended for suspension in liquid vehicles
for Oral Suspension are most frequently
supplied as dry powder mixtures for
reconstitution at the time of dispensing

MDALegaspi 2016

Reasons for Suspensions

Stability
Easy to administer
Pallatability

MDALegaspi 2016

Features Desired in a
Pharmaceutical Suspension
1. A properly prepared pharmaceutical
suspension should settle slowly and should be
readily redispersed upon gentle shaking of the
container
2. The particle size of the suspensoid should
remain fairly constant throughout long periods
of undisturbed standing
3. The suspension should pour readily and evenly
from its container

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Sedimentation Rate of the

Particles of a Suspension

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Stokes equation
was derived for an ideal situation in which
uniform, perfectly spherical particles in a very
dilute suspension settle without producing
turbulence, without colliding with other particles
of the suspensoid, and without chemical or
physical attraction or affinity for the dispersion
medium

MDALegaspi 2016

Brookfield viscometer
Measures viscosity by the force required to
rotate a spindle in the fluid being tested

MDALegaspi 2016

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Physical Features of the Dispersed

Phase of a Suspension
the particle diameter is 1 to 50 m
particle shape of the suspensoid should not
induce caking and product stability

MDALegaspi 2016

Micropulverization
one of the most rapid, convenient, and
inexpensive methods of producing fine drug
powders of about 10 to 50 m size
Micropulverizers are high-speed attrition
or impact mills that are efficient in reducing
powders to the size acceptable for most oral and
topical suspensions

MDALegaspi 2016

Micropulverization METHODS:
fluid energy grinding
spray drying

MDALegaspi 2016

fluid energy grinding

Aka: jet milling or micronizing
for still finer particles under 10 m
PROCESS:

the shearing action of high velocity compressed airstreams

on the particles in a confined space produces the desired
ultrafine or micronized particles
The particles to be micronized are swept into violent
turbulence by the sonic and supersonic velocities of the
airstreams.
The particles are accelerated to high velocities and collide
with one another, resulting in fragmentation.

employed when the particles are intended for parenteral

or ophthalmic suspensions

MDALegaspi 2016

spray drying
produces particles of extremely small
dimensions
Spray Dryer is a cone-shaped apparatus
into which a solution of a drug is sprayed and
rapidly dried by a current of warm, dry air
circulating in the cone

MDALegaspi 2016

Physical Features of the Dispersed

Phase of a Suspension
the particle diameter is 1 to 50 m
particle shape of the suspensoid should not
induce caking and product stability

MDALegaspi 2016

Pre-Formulation Consideration factors:

1. Wetting or wettability property
2. Particles interaction and behavior
3. Sedimentation rate

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Wettability Property
Involves the affinity of the solid and the liquid
portion of the suspension
Aids to increase the wetting characteristics of
powder:
1. Use of Surfactant to decrease the solid-liquid
interfacial tension
2. Use dispersion aids for hydrophobic solids
Example:

Hydrophobic Polymers (sodium carboxymethylcellulose)

Water insoluble hydrophilic materials (bentonite, veegum)
Colloidal silica

MDALegaspi 2016

Particle interaction and behavior

Sensitivity of electrolytes
Flocculation occurs at the following ion
concentration:
For monovalent ions = 25-150 mmol/L
For divalent ions = 0.5-2.0 mmol/L
For trivalent ions = 0.01-0.1 mmol/L

MDALegaspi 2016

Types of Suspension Systems

1. Flocculated System
2. Deflocculated System

MDALegaspi 2016

Flocculated System
Aka: Coagulated System or Colloidaly Unstable
System
Characteristics:
a) particles appears as floccules or like tufts of
wool with loose fibrous structure
b) Forms a clear particle free supernatant liquid
and a sediment
c) Exhibit a minimum of serious separation

MDALegaspi 2016

Deflocculated System
Aka: Peptized System or Colloidaly Stable
System
Characteristics:
a) The particles settle as a dense sediment and
becomes compact after a given time interval
b) Results in poor suspension

MDALegaspi 2016

Relative Properties of Flocculated and

Deflocculated Particles in Suspension
FLOCCULATED
1.
2.
3.
4.

5.

Particles form loose aggregates.

Rate of sedimentation is high, as particles
settle as a floc, which is a collection of
particles.
A sediment is formed rapidly.
The sediment is packed loosely and
possesses a scaffold-like structure.
Particles do not bond tightly to each
other, and a hard, dense cake does not
form. The sediment is easy to redisperse,
so as to reform the original suspension.
The suspension is somewhat unsightly,
due to rapid sedimentation and the
presence of an obvious, clear supernatant
region. This can be minimized if the
volume of sediment is made large.
Ideally, volume of sediment should
encompass the volume of the suspension.

DEFLOCCULATED
1.
2.
3.
4.

5.

Particles exist in suspension as separate

entities.
Rate of sedimentation is slow, as each
particle settles separately and particle
size is minimal.
A sediment is formed slowly.
The sediment eventually becomes very
closely packed, due to weight of upper
layers of sedimenting material. Repulsive
forces between particles are overcome
and a hard cake is formed that is difficult,
if not impossible, to redisperse.
The suspension has a pleasing
appearance, as the suspended material
remains suspended for a relatively long
time. The supernate also remains cloudy,
even when settling is apparent.

MDALegaspi 2016

Sedimentation Rate
The velocity of sedimentation is directly
proportional to the particle size and inversely
proportional with the viscosity of the
formulation

MDALegaspi 2016

Problems in Suspension:
1. Caking
formation of cement like substance due to small
partcles
Irreversible process
Solution: Flocculated System

2. Sedimentation
The rapid settling of particles
Reversible Process
Solution: Suspending Agents

MDALegaspi 2016

Rheology
the study of flow, addresses the viscosity
characteristics of powders, fluids, and semisolids
Two (2) general categories of materials flow:
1. Newtonian flow is characterized by
constant viscosity, regardless of the shear rates
applied
2. non-Newtonian is characterized by a
change in viscosity characteristics with
increasing shear rates
Example materials include colloidal solutions,
emulsions, liquid suspensions, and ointments

MDALegaspi 2016

three general types of

non-Newtonian materials
1. Plastic
2. Pseudoplastic
3. Dilatant

MDALegaspi 2016

Plastic
Substances that exhibit plastic flow are called
Bingham bodies
Plastic flow does not begin until a shearing
stress corresponding to a certain yield value is
exceeded

MDALegaspi 2016

Pseudoplastic
Pseudoplastic substances begin flow when a
shearing stress is applied; therefore, they exhibit
no yield value.
With increasing shearing stress, the rate of shear
increases; consequently, these materials are also
called shear-thinning systems

MDALegaspi 2016

Dilatant
Dilatant materials are those that increase in
volume when sheared, and the viscosity
increases with increasing shear rate.
These are also called shear-thickening
systems.
Dilatant systems are usually characterized by
having a high percentage of solids in the
formulation.

MDALegaspi 2016

Stability Consideration of Suspension

The physical stability of a suspension is normally
assessed by the:
1. Measurement of its sedimentation rate
2. Measurement of the final volume or height of
sediment
3. Ease of redispersion of the product

Suspending Agents Used in the Formulation of

Pharmaceutical Suspensions
MDALegaspi 2016

MDALegaspi 2016

Formulation of Suspensions
Factors to be considered in formulating
suspensions:
1. Type of suspension desired (flocculated or
deflocculated)
2. Formulation adjuvants
3. Preparation techniques
4. Incompatiblities

MDALegaspi 2016

Type of suspension
Flocculated System

Deflocculated System

Reduction of interfacial tension

Application of Surfactants
SLS
Sodium dioctyl succinate
Nonionic Surfactants (spans,
tweens, carbowax)
Drainage of the preparation
especially for oral, parenteral,
ophthalmic or topical
useaddition of protective
colloid
Silica Gel (a form of
precipitated silicic acid upto
10% conc) topical prepn

Retardation of settling and

agglomeration of the particles by
functioning as an energy barrier
minimizing interparticulate
attraction and ultimate
deflocculation
Modified cellulose polymer
(CMC, methocel)
Proteins (gels)
Synthetic Polymers
(carbopol) used in external
lotions and gels prepn
Clays (bentonite, veegum)

MDALegaspi 2016

Formulation adjuvants

Dispersion medium
Wetting agents
Buffer
Other adjuvants:

Preservatives
Colorants
Flavorants
Perfumes

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Methods of Manufacture/Preparation
of Suspension:
1. By dispersion method
2. By precipitation method

MDALegaspi 2016

Incompatibilities
Formation of dark color
Oil separation
Chemical reaction

MDALegaspi 2016

Packaging and Storage of Suspension

All suspensions should be packaged in widemouth
containers having adequate airspace above the
liquid to permit thorough mixing by shaking and
ease of pouring
Most suspensions should be stored in tight
containers protected from freezing, excessive heat
and light
Should have the auxiliary label SHAKE WELL
before used to ensure a uniform distribution of
solid in the vehicle and thereby uniform and proper
dosage

MDALegaspi 2016

Purposes of Suspension

Sustaining effect
Stability
Taste
Basic solubility

MDALegaspi 2016

Application of Suspension

Low solubility of active ingredient

Patients difficulty to swallow (suspension vs solids)
Unpleasant taste
Rate of absorption
Rapid degeneration
Unstable in desired vehicle
Degraded drug in aqueous form but not in
nonaqueous
Bulk insoluble powder
Prolong release effect
Topical prepn

MDALegaspi 2016

Formation of suspensions
The following steps may minimize stability problems
1.
The particle size of all powders used in the formulation should be
reduced.
2. A thickening (suspending) agent may be used to increase viscosity.
Common thickening agents include alginic acid, bentonite, VEEGUM,
methylcellulose, and tragacanth.
3. A levigating agent may aid in the initial dispersion of insoluble particles.
Common levigating agents include glycerin, propylene glycol, alcohol,
syrups, and water.
4. Flavoring agents and preservatives should be selected and added if the
preparation is intended for oral use. Common preservatives include
methylparaben, propylparaben, benzoic acid, and sodium benzoate.
Flavoring agents may be any fl avored syrup or flavored concentrate
5. The source of the active ingredients (e.g., bulk powders vs. tablets or
capsules) must be considered; if commercial dosage forms are used, the
inactive ingredients must be considered and only immediate-release
tablets or capsules should be used and not modified release, unless
necessary and they can be used appropriately.

MDALegaspi 2016

Preparation of suspensions
1.
2.

3.
4.
5.
6.
7.
8.

The insoluble powders are triturated to a fi ne powder.

A small portion of liquid is used as a levigating agent, and the
powders are triturated until a smooth paste is formed.
The vehicle containing the suspending agent is added in divided
portions. A high-speed mixer greatly increases the dispersion.
The preparation is brought to the required volume using the
vehicle.
The final mixture is transferred to a tight bottle for dispensing
to the patient.
All suspensions are dispensed with a shake well label.
Suspensions are not filtered.
The water-soluble ingredients, including flavoring agents, are
mixed in the vehicle before mixing with the insoluble ingredients.

MDALegaspi 2016

Example of Suspension Formulation

Amount

Function

Aluminum hydroxide gel, USP

6g

Antacid

Sodium benzoate

0.5g

Preservative

Sodium saccharin

0.005g

Sweetener

Sorbitol

1.4 mL

Viscosity builder

Peppermint oil

0.005 mL

flavorant

Purified water,

to make 60 mL

Solvent

MDALegaspi 2016

Dispersed Systems: Coarse Dispersion

MDALegaspi 2016

EMULSION
is a dispersion in which the dispersed phase is
composed of small globules of a liquid distributed
throughout a vehicle in which it is immiscible
have dispersed particles ranging in diameter from
0.1 to 100 m
is a dispersed system containing at least two
immiscible liquid phases
Two (2) phases:

1. Internal or Discontinuous Phase the

dispersed phase
2. External or Continuous Phase the dispersion
medium

MDALegaspi 2016

Types of Emulsion
1)
2)
3)
4)

oil-in-water (O/W) emulsion

water-in-oil (W/O) emulsion
multiple emulsions
Microemulsions

MDALegaspi 2016

oil-in-water (O/W) emulsion

emulsions with an oleaginous internal phase and
an aqueous external phase
oral products and external, washable products

MDALegaspi 2016

water-in-oil (W/O) emulsion

emulsions having an aqueous internal phase and
an oleaginous external phase
used for external preparations when emollient,
lubricating, or protective properties are desired

MDALegaspi 2016

multiple emulsions
three phases are present
Forms:
W/O/W
O/W/O

In these emulsions within

emulsions, any drug
present in the innermost
phase must now cross two
phase boundaries to reach
the external, continuous
phase

MDALegaspi 2016

Microemulsions
appear translucent or
transparent
have droplet diameter
in the nanometer size
range

MDALegaspi 2016

Detection of Emulsion type

1. Dilution Test

The dilution method depends on the fact that an O/W

emulsion can be diluted with water and a W/O emulsion
with oil

2. Conductivity Test

An emulsion in which the continuous phase is aqueous

can be expected to possess a much higher conductivity
than an emulsion in which the continuous phase is an oil

3. Dye-solubility Test

The knowledge that a watersoluble dye will dissolve in the

aqueous phase of an emulsion while an oil-soluble dye
will be taken up by the oil phase provides a third means
of determining emulsion type

MDALegaspi 2016

FACTORS THAT DETERMINE

EMULSION TYPE
1. Emulsifier
some emulsifiers form either w/o or o/w
emulsions, others form only one type

2. Phase ratio (relative amounts of oil and water)

phase present in greater concentration tends to be
the external phase

3. Order of mixing
the phase that is being added by portions tends to
be the internal phase

MDALegaspi 2016

Purposes of Emulsion:

Increased drug solubility

Increased drug stability
Prolonged drug action
Improved taste
Improved appearance

MDALegaspi 2016

Emulsifying Agent
Any compound that lowers the interfacial tension
and forms a film at the interface can potentially
function as an emulsifying agent.
The effectiveness of the emulsifying agent depends
on its chemical structure, concentration, solubility,
pH, physical properties, and electrostatic effect

True emulsifying agents (primary agents) can

form and stabilize emulsions by themselves
Stabilizers (auxiliary agents) do not form acceptable
emulsions when used alone, but assist primary agents
in stabilizing the product (e.g., increase viscosity).

are either natural or synthetic

MDALegaspi 2016

Classification of Emulsifying Agents

1. Natural Emulsifying Agent
2. Finely Divided Solids
3. Synthetic Emulsifying Agent

MDALegaspi 2016

Natural Emulsifying Agent

derived from animal or plant sources
Animal:
Gelatin
egg yolk
casein

Plant:

Acacia
Tragacanth
Pectin
cellulose derivatives

MDALegaspi 2016

Acacia
forms a good, stable emulsion of low viscosity
It tends to cream easily, is acidic, and is stable at
a pH range of 2 to 10.
Like other gums, it is negatively charged,
dehydrates easily, and usually requires a
preservative.
It is incompatible with Peruvian balsam,
bismuth salts, and carbonates

MDALegaspi 2016

Tragacanth
forms a stable emulsion that is coarser than
acacia emulsion
It is anionic, is difficult to hydrate, and is used
mainly for its effects on viscosity.
Less than 1/10 of the amount used for acacia is
needed.

MDALegaspi 2016

Agar
is an anionic gum that is primarily used to
increase viscosity.
Its stability is affected by heating, dehydration,
and destruction of charge.
It is also susceptible to microbial degradation.

MDALegaspi 2016

Pectin
is a quasi-emulsifier that is used in the same
proportion as tragacanth

MDALegaspi 2016

Gelatin
provides good emulsion stabilization in a
concentration of 0.5% to 1.0%
It may be anionic or cationic, depending on its
isoelectric point.
Type A gelatin (+), prepared from an acid-treated
precursor, is used in acidic media.
Type B gelatin (-), prepared from an alkali-treated
precursor, is used in basic media.

MDALegaspi 2016

Methyl cellulose
is nonionic and induces viscosity.
It is used as a primary emulsifier with mineral
oil and cod liver oil, and yields an o/w emulsion.
It is usually used in 2% concentration.

MDALegaspi 2016

Carboxymethylcellulose
is anionic and is usually used to increase
viscosity
It tolerates alcohol up to 40%, forms a basic
solution, and precipitates in the presence of free
acids.

MDALegaspi 2016

Finely Divided Solids

Aka: CLAY
Veegum -Magnesium aluminumsilicate
Bentonite -Native Colloidal Hydrated Aluminum
Silicate

MDALegaspi 2016

Synthetic emulsifying agents

are anionic, cationic, or nonionic
Although these surfactants are amphiphilic
molecules, their lipophilic and hydrophilic regions
are seldom inverse equals of each other
Some surfactant molecules tend to be
predominantly lipophilic, whereas others are
predominantly hydrophilic.
This imbalance is reflected in the hydrophilic
lipophilic balance (HLB) scale:
The larger the HLB value, the more hydrophilic the
molecule.

MDALegaspi 2016

Anionic synthetic agents

include sulfuric acid esters (e.g., sodium lauryl
sulfate), sulfonic acid derivatives (e.g., dioctyl
sodium sulfosuccinate), and soaps. Soaps are for
external use.
They have a high pH and are, therefore, sensitive to
the addition of acids and electrolytes.
Alkali soaps are hydrophilic and form an o/w
emulsion.
Metallic soaps are water insoluble and form a w/o
emulsion.
Monovalent soaps form an o/w emulsion.
Polyvalent soaps form a w/o emulsion.

MDALegaspi 2016

Cationic synthetic agents

are used as surface-active agents in 1%
concentration
They are incompatible with soaps
e.g., benzalkonium chloride

MDALegaspi 2016

Nonionic synthetic agents

are resistant to the addition of acids and
electrolytes
a. The sorbitan esters known as Spans are
hydrophobic in nature and form w/o emulsions.
b. The polysorbates known as Tweens are
hydrophilic and tend to form o/w emulsions.
They may form complexes with phenolic
compounds.

MDALegaspi 2016

HYDROPHILICLIPOPHILIC BALANCE
(HLB)
HLB Value Range

Surfactant Application

03

Antifoaming agents

46

Water-in-oil emulsifying agents

79

Wetting agents

8 18

Oil-in-water emulsifying agents

13 - 15

Detergents

10 - 18

Solubilizing agents

MDALegaspi 2016

COMMONLY USED SURFACTANTS AND THEIR HYDROPHILIC

LIPOPHILIC BALANCE (HLB) VALUES

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Preparation
A. Classical, acacia-stabilized emulsions are
prepared by one of the following four methods:
1.
2.
3.
4.

Wet gum (English) method

Dry gum (continental) method
Bottle method
Nascent soap method

B. Emulsions stabilized by synthetic emulsifying

agents are readily prepared by a two-phase
procedure.

MDALegaspi 2016

Wet gum (English) method

A primary emulsion of fixed oil, water, and acacia
(in a 4:2:1 ratio) is prepared as follows:
a. Two parts of water are added all at once to one part
of acacia. The mixture is triturated until a smooth
mucilage is formed.
b. Oil is added in small increments (1 to 5 mL), with
continuous trituration, until the primary emulsion is
formed.
c. The mixture (an o/w emulsion) is triturated for
another 5 mins.
d. The o/w mixture can then be brought to volume with
water and mixed to achieve homogeneity.

MDALegaspi 2016

Dry gum (continental) method

A primary emulsion of the fixed oil, water, and acacia (in
a 4:2:1 ratio) is prepared as follows:
a.

b.
i.

Oil is added to the acacia, and the mixture is triturated

until the powder is distributed uniformly throughout the
oil. Water is added all at once, followed by rapid
trituration to form the primary emulsion.
Any remaining water and other ingredients are added to
finish the product.

Electrolytes in high concentration tend to crack an

emulsion. They should be added last and in as dilute a form
as possible.
ii. Alcoholic solutions tend to dehydrate and precipitate
hydrocolloids. They should be added in as dilute a
concentration as possible.

MDALegaspi 2016

Bottle method
a variation of the dry gum method used for
volatile oils
Oil is added to the acacia in a bottle.
The ratio of oil, water, and acacia should be 3:2:1
or 2:1:1.
The low viscosity of the volatile oil requires a
higher proportion of acacia.

MDALegaspi 2016

Nascent soap method

A soap is formed by mixing relatively equal volumes of an oil
and an aqueous solution that contains a sufficient amount of
alkali.
The soap acts as an emulsifying agent.
a.

b.

c.

This method is used to form an o/w or a w/o emulsion,

depending on the soap formed. For example, olive oil, which
contains oleic acid, is mixed with lime water during the
preparation of calamine lotion to calcium oleate, an
emulsifying agent.
A 50:50 ratio of oil to water ensures sufficient emulsion,
provided that the oil contains an adequate amount of free fatty
acid. Olive oil usually does. Cottonseed oil, peanut oil, and
some other vegetable oils do not.
The addition of an acid destroys the emulsifying soap and
causes the emulsion to separate.

MDALegaspi 2016

Emulsions stabilized by synthetic emulsifying agents are

readily prepared by a two-phase procedure.
1.
a.

2.
a.

3.

Oil-miscible ingredients and water-miscible ingredients are

separately admixed, using heat if necessary to ensure liquefaction
and ease of mixing of each phase.
High melting point oil-miscible ingredients (e.g., waxes) are melted
before lower melting point ingredients (e.g., oils) are added.

The two phases are heated to 70 to 80C and then combined with
stirring until the resultant emulsion has cooled.
In general, heat-labile or volatile ingredients should not be
incorporated in the separate phases but in the resultant emulsion aft
er it has cooled to about 40C or less.

Further mechanical processing of the emulsion by a hand

homogenizer, immersion blender, or other equipment may be
warranted to improve the homogeneity and stability of the
product.

MDALegaspi 2016

Incorporation of medicinal agents

A. Addition of a drug during emulsion formation
B. Addition of a drug to a preformed emulsion
can present some difficulty, depending on the
type of emulsion and the nature of the
emulsifier

MDALegaspi 2016

Addition of a drug to a preformed emulsion can present

some difficulty, depending on the type of emulsion and
the nature of the emulsifier
1.

Addition of oleaginous materials to a w/o emulsion presents no problem because of the

miscibility of the additive with the external phase. However, addition of oleaginous
materials to an o/w emulsion can be difficult after emulsion formation.
a.
b.

2.

3.

4.

Occasionally, a small amount of oily material is added if excess emulsifier was used in the
original formation.
A small amount of an oil-soluble drug can be added if it is dissolved in a very small
quantity of oil with geometric dilution techniques.

Addition of water or an aqueous material to a w/o emulsion is extremely difficult, unless

enough emulsifier has been incorporated into the emulsion. However, addition of
aqueous materials to an o/w emulsion usually presents no problems if the added
material does not interact with the emulsifying agent. Potential interactions should be
expected with cationic compounds and salts of weak bases.
Addition of small quantities of alcoholic solutions to an o/w emulsion is possible if the
solute is compatible or dispersible in the aqueous phase of the emulsion. If acacia or
another gum is used as the emulsifying agent, the alcoholic solution should be diluted
with water before it is added.
Addition of crystalline drugs to a w/o emulsion occurs more easily if the drugs are
dissolved or dispersed in a small quantity of oil before they are added.

MDALegaspi 2016

Formation and preparation of

emulsions
1.

A mortar and pestle are frequently all the equipment

that is needed.
2. Electric mixers and hand homogenizers are useful for
producing emulsions after the coarse emulsion is formed in
the mortar.
3. The order of mixing of ingredients in an emulsion
depends on the type of emulsion being prepared (i.e., o/w
or w/o) as well as the emulsifying agent chosen.
4. Preservatives. If the emulsion is kept for an extended
period, refrigeration is usually sufficient. The preparation
should not be frozen. If a preservative is used, it must be
soluble in the water phase to be effective.
5. Flavoring agents. If the addition of a flavor is needed to
mask the taste of the oil phase, the flavor should be added
to the external phase before emulsification

MDALegaspi 2016

FLAVOR SELECTION GUIDE

Taste

Masking Flavor

Salt

Butterscotch, maple

Bitter

Wild cherry, walnut, chocolate mint, licorice

Sweet

Fruit, berry, vanilla

Acid

Citrus

MDALegaspi 2016

PROBLEMS IN EMULSION
1. creamingupward
2. sedimentationdownward
3. aggregationglobules come together but do
not fuse
4. coalescenceglobules come together and
fuse
5. crackingcomplete separation
6. inversion o/ww/o vice versa

MDALegaspi 2016

GELS
are semisolid systems consisting of dispersions
of small or large molecules in an aqueous liquid
vehicle rendered jelly-like by the addition of a
gelling-agent

MDALegaspi 2016

PHENOMENA IN GELS
Thixotropy is the ability of the gel to become fluid
on agitation, only to resume their solid or semisolid
state after remaining undisturbed for a period of
time.
Imbibition is the taking up of a certain amount of
liquid without a measurable increase in volume
Swelling is also the taking up of liquid by a gel but
with an increase in volume.
Syneres is phenomenon where liquid comes out of
the gel and the gel shrinks
Xerogel is formed when the liquid is removed from
a gel and only the frameworkremains

MDALegaspi 2016

GLYCEROGELATINS
are plastic masses containing

glycerin (40%)
water (35%)
gelatin (15%),
and an added medicinal substance (10%) such as
zinc oxide

MDALegaspi 2016

MAGMAS / MILK
A two-phase system gel consisting of floccules of
small distinct particles
ex. Milk of Magnesia / Magnesia Magma