COARSE DISPERSIONS

By: Daisy Marie A. Tecson and Claire R. Lago

PHARMACEUTICAL SUSPENSION
 is a COARSE DISPERSION in which
insoluble solid particles are
dispersed in a liquid medium.
 particles have a diameter greater
than 0.1 µm.
 particles are observed under the
microscope to exhibit Brownian
movement if the dispersion has a
low viscosity.
SUSPENSIONS
 Oral Suspension:
- Ex. Oral Antibiotic syrups
 Antacid and Radiopaque suspensions
- contains high concentrations of
dispersed solids.
 Externally applied suspensions
- for dermatologic, cosmetic, and
protective purposes.
 Parenteral suspensions – contain from
0.5% to 30% of solid particles.
VISCOSITY AND PARTICLE SIZE
 are significant factors because they
affect the ease of injection and the
availability of the drug in depot
therapy.
 QUALITIES OF AN ACCEPTABLE
SUSPENSION:
 The suspended material should not settle
rapidly.
 The particles that do settle to the bottom
of the container must not form a hard
cake but should be readily redispersed
into a uniform mixture when the
container is shaken.
 Suspension must not be too viscous to
pour freely from the orifice of the bottle
or to flow through a syringe needle.
 INTERFACIAL PROPERTIES OF
SUSPENDED PARTICLES
- Particles are highly energetic and tend to
regroup in such a way as to decrease the total
area and reduce the surface free energy. The
particles in a liquid suspension therefore tend to
flocculate, that is, to form light, fluffy
conglomerates that are held together by a weak
van der Waals forces.
THEORY OF SEDIMENTATION
 The velocity of sedimentation is expressed by
Stroke’s Law:

Where v is the terminal velocity in cm/sec, d is

the diameter of the particle in cm, ρi and ρe
are the densities of the dispersed phase and
dispersion medium, g is the acceleration due
to gravity, and η is the viscosity of the
dispersion in the medium in poise.
 In dilute suspensions, the particles
do not interfere with one another
during sedimentation, and free
settling occurs.
SEDIMENTATION OF
FLOCCULATED PARTICLES
 It is observed that the flocs tend to fall
together, producing a distinct between the
sediment and the supernatant liquid.
 In accordance to Stroke’s law, the larger the
particles settle more rapidly than the smaller
particles.
 According to Hiestand, the initial rate of
settling of flocculated particles are
determined by the floc size and the porosity
of the aggregated mass.
SEDIMENTATION PARAMETERS
 Two useful parameters that can be derived
from sedimentation studies are:
1. sedimentation volume, V, or height, H
2. degree of flocculation

 A more useful parameter for flocculation is ß,

the degree of flocculation.
FORMULATION OF SUSPENSIONS
 Wetting of Particles
 Controlled Flocculation
 Flocculation in Structured Vehicles
 Rheologic Considerations
 Preparation of Suspension
 Physical Stability of Suspensions
WETTING OF PARTICLES
 The wettability of a powder can be
ascertained easily by observing the
contact angle that powder makes with
the surface of the liquid. A powder
that floats low in the liquid has a
lesser angle, and one that sinks shows
no contact angle.
 Powders that are not easily wetted by
water and show a large contact angle
are said to be hydrophobic.
Example: Sulfur, Charcoal and Magnesium
Stearate

 Powders that are readily wetted by

water when free of adsorbed
contaminants are called hydrophilic.
Example: Zinc Oxide, Talc and Magnesium
Carbonate
CONTROLLED FLOCCULATION
 Electrolytes act as flocculating agents by
reducing the electric barrier between the
particles, by a decrease in the zeta potential
and the formation of a bridge between
adjacent particles so as to link them
together in a loosely arranged structure.
RHEOLOGIC CONSIDERATION
 The principles of rheology can be applied to
a study of the following factors:
 The viscosity of a suspension as it affects the
settling dispersed particles
 The change in flow in properties of the
suspension when the container is shaken and
when the product is poured from the bottle
 The spreading qualities of the lotion when it is
applied to an affected area
PHYSICAL STABILITY OF
SUSPENSIONS
 Raising the temperature often leads to
flocculation of sterically stabilized
suspensions, that is, suspensions stabilized
by nonionic surfactants.
 When the suspension is heated, the energy of
repulsion between the particles can be
reduced owing to dehydration of the
polyoxyethylene groups of the surfactant.
The attractive energy is increased and the
particles flocculate.
EMULSIONS
 is a thermodynamically unstable system
consisting of at least two immiscible liquid
phases, one of which is dispersed as globules
in the other liquid phase, stabilized by the
presence of an emulsifying agent.
EMULSION TYPES
 Oil-in-Water (o/w) emulsion – when the
oil phase is dispersed as globules
throughout an aqueous continuous phase.

 Water-in-Oil (w/o) emulsion- when the oil

phase serves as the continuous phase.
THEORIES OF EMULSIFICATION
 For a theory to be meaningful, it should
be capable of explaining:
(a) the stability of the product
(b) the type of emulsion formed

Emulsifying agents can be divided into three

groups:
(a) Surface-active agents
(b) Hydrophilic colloids
(c) Finely divided solid particles
MICROEMULSIONS
 May be a misnomer because microemulsions
consist of large or “swollen” micelles
containing the internal phase, much like that
found in a solubilized solution.
 They can be used to increase the
bioavailability of drugs poorly soluble in
water by incorporation of the drug into the
internal phase and as topical drug delivery
systems.
SEMISOLIDS
 Gel – solid or a semisolid system of at
least two constituents, consisting of a
condensed mass enclosing and
interpenetrated by a liquid.
 When coherent matrix is rich in liquid ,
the product is often called a jelly.
 Gel is known as a xerogel .
 Examples are gelatin sheets, tragacanth
ribbons and acacia tears.
SYNERESIS AND SWELLING
 Syneresis – is when a gel stands for some
time, it often shrinks naturally, and some of
its liquid is pressed out.
 The opposite of syneresis is the taking up of
the liquid by a gel with an increase in
volume. This phenomenon is known as
swelling.
 Gels may also take up a certain amount of
liquid without a measurable increase in
volume, and it is called imbibition.
CLASSIFICATION OF SEMISOLID BASES
I. Organogels
A. Hydrocarbon Type
Ex. Petrolatum, mineral oil-polyethylene gel
B. Animal and vegetable fats
Ex. Lard, hydrogenated vegetable oils,
Theobroma oil
C. Soap base greases
Ex. Aluminum stearate, mineral oil gel
D. Hydrophilic organogels
Ex. Carbowax bases, polyethylene glycol
ointment
II. Hydrogels
A. Organic hydrogels
Ex. Pectin paste, tragacanth jelly
B. Inorganic hydrogels
Ex. Bentonite gel, colloidal magnesium
aluminum silicate gels
III. Emulsion-type semisolids
A. Emulsifiable bases
1. Water-in-oil (absorption)
Ex. Hydrophilic petrolatum, wool fat
2. Oil-in-water
Ex. Anhydrous Tween base
B. Emulsified bases
1. Water-in-oil
Ex. Hydrous wool fat, rose water
ointment
2. Oil-in-water
Ex. Hydrophilic ointment, vanishing
cream
EMULSION-TYPE BASES
Two classes of emulsion bases:
(a) Emulsifiable bases. They contain no
water but are capable of taking it up
to yield w/o and o/w emulsion.
(b) Emulsified bases. Water-in-oil bases
in which water is incorporated during
manufacture are referred as
emulsified w/o bases to differentiate
then from the emulsifiable w/o
bases, which contain no water.
 The oil phase of the ointment may
contain petrolatum, natural waxes,
fatty acids or alcohols, solid esters,
and similar substances that increase
the consistency of the base and
provide certain desirable application
properties.