SUSPENSIONS PHARM.

D 3rd Semester
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Suspensions may be 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.
Some suspensions are available in ready to-use form, that is, already distributed
through a liquid vehicle with or without stabilizers and other additives. Other
preparations are available as dry powders intended for suspension in liquid vehicles.
Generally, this type of product is a powder mixture containing the drug and
suitable suspending and dispersing agents to be diluted and agitated with a specified
quantity of vehicle, most often purified water.
 FEATURES DESIRED IN A
PHARMACEUTICAL SUSPENSION
There are many considerations in the development and preparation of a
pharmaceutically elegant suspension.
In addition to therapeutic efficacy, chemical stability of the components of the
formulation, permanency of the preparation, and aesthetic appeal of the
preparation—desirable qualities in all pharmaceutical preparations—a few other
features apply more specifically to the 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
SUSPENSION INGREDIENTS
1. Drug
2. External phase
3. Wetting agents
4. Suspending agents
5. Flocculating agents
6. Preservatives
7. Sweeteners, colorants and flavorants
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1. External Phase
The external phase is water for oral preparations; however, other polar
liquids, such as glycerin or alcohol, may be considered to control
solubility, stability, and taste.
The selection of the external phase is based on taste, viscosity, density,
and stability.
Non-polar liquids, such as aliphatic hydrocarbons and fatty esters, may be
considered, if the preparation is used for external purposes.
2. Drug
Drug that is insoluble in the vehicle is used to prepare suspension.
Water insoluble drug is usually suspended in the aqueous vehicle
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3. Wetting Agents
Wetting agents are used to improve the flow of the liquid vehicle across the particle
surface, which in turn improves the homogeneity of distribution of the drug
particles throughout the formulation. They do this by reducing the interfacial
tension between the solid particle and liquid medium
A wetting agent is a surfactant with an HLB value between 7 and 9.
Surfactants with higher HLB values are sometimes recommended, such as
polysorbates and poloxamers.
They are employed at a low concentration (0.05–0.5%) to allow the
displacement of air from hydrophobic material and permit the liquid, usually
water, to surround the particles.
Examples include Sodium Lauryl Sulfate, Polysorbate 80(tween 80)
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4. Flocculating agents
The last excipient to be added to the suspension formulation is the
flocculation modifier, its function being to adjust the flocculation
status of the particles to that which is intended.
The quantity of flocculation modifier required must be determined last,
once the levels and effects of all other functional excipients have been
resolved.
If it is desirable to flocculate the particles, then flocculating agents are
employed.
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5. Suspending Agents
Viscosity modifiers are also known as suspending agents as they will reduce the
sedimentation of the particles and keep them suspended for longer.
They may also interact with the surface of suspended particles to facilitate wetting and
reduce tendency of agglomeration.
The choice of an appropriate viscosity agent depends on the use of the product (external or
internal), the processing equipment, and the duration of storage.
The target viscosity for each preparation needs to be de ned so as to maintain the particles in
their suspended state for as long as possible, i.e. to retard sedimentation. However, this must
be balanced against the ease of use of the product; whilst a very viscous suspension will
show little, if any, sedimentation, it is unlikely to be patient-friendly. The product must be
pourable from a bottle onto a spoon for oral use or dispensable through a nozzle if it is
intended for ocular or nasal use.
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Commonly used suspending agents include
a) Cellulose derivatives (methyl cellulose, sodium carboxymethylcellulose and
hydroxypropyl methylcellulose)
b) Gums (acacia, xanthan)
c) Polymers (Carbomers )
Suspension preparations for internal use exhibiting good flow and suspending
properties often contain sodium carboxymethylcellulose 2.5%, tragacanth 1.25%,
or guar gum 0.5%.
For external applications, Carbopol polymers have been successfully used.
Other common viscosity producing agents include acacia, methylcellulose, sodium
alginate, or tragacanth.
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6. Preservatives
Preservatives are often added in
aqueous suspensions because
suspending agents and sweeteners are
good media for microbial growth.
Solvents, such as alcohols, glycerin,
and propylene glycol, may also have
some preservative effect depending on
their concentration.
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7. Sweeteners, flavors, and colorants:
Sweeteners are often added to suspensions to reduce any unpleasant
taste of the partially dissolved drug and to improve palatability in
general.
Examples include sorbitol, corn syrup, sucrose, saccharin and
aspartame.
Flavors are added to enhance patient’s acceptance of the product.
Colorants are added to provide a more esthetic appearance to the final
product.
Choice of colorant is usually tied to the choice of flavor, and their
choices are also linked to the patient population, such as age group and
geographic region, and the therapeutic need
PREPARATION OF SUSPENSIONS
The preparation of suspensions involves several steps; the first is to obtain
particles of the proper size, typically in the lower micrometer range.
Oral preparations should not feel gritty; topical preparations should feel smooth
to the touch; and injectables should not produce tissue irritation.
In the preparation of a suspension, the pharmacist must be aware of the
characteristics of both the intended diphase and the dispersion medium.
oIn some instances, the dispersed phase has an affinity for the vehicle to be
employed and is readily wetted by it.
o Other drugs are not penetrated easily by the vehicle and have a tendency to
clump together or to float on the vehicle
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oWhen drugs are not easily penetrated by vehicle, the powder must first be
wetted to make it more penetrable by the dispersion medium. Alcohol,
glycerin, propylene glycol, and other hygroscopic liquids are employed as
wetting agents when an aqueous vehicle is to be used as the dispersion
phase
In large-scale preparation of suspensions, wetting agents are mixed with
the particles by an apparatus such as a colloid mill; on a small scale in the
pharmacy, they are mixed with a mortar and pestle.
Once the powder is wetted, the dispersion medium (to which have been
added all of the formulation’s soluble components, such as colorants,
flavorants, and preservatives) is added in portions to the powder, and the
mixture is thoroughly blended before subsequent additions of vehicle.
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A portion of the vehicle is used to wash the mixing equipment free of
suspensoid, and this portion is used to bring the suspension to final
volume and ensure that the suspension contains the desired
concentration of solid matter.
 The final product is then passed through a colloid mill or other
blender or mixing device to ensure uniformity.
Whenever appropriate, suitable preservatives should be included in
the formulation of suspensions to preserve against bacterial and mold
contamination.
 EXAMPLES OF ORAL
SUSPENSIONS
oAntacid Oral Suspensions
oAntacids are intended to counteract the
effects of gastric hyperacidity and, as
such, are employed by persons, such as
peptic ulcer patients, who must reduce the
level of acidity in the stomach
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oAntibacterial Oral Suspensions

The antibacterial oral suspensions include preparations of antibiotic
substances (e.g., erythromycin derivatives and tetracycline and its
derivatives), sulfonamides (e.g., sulfamethoxazole and sulfisoxazole acetyl),
other anti-infective agents (e.g., methenamine mandelate and nitrofurantoin),
or combinations of these (e.g., sulfamethoxazole–trimethoprim).
Many antibiotic materials are unstable when maintained in solution for an
appreciable length of time, and therefore, from a stability standpoint, insoluble
forms of the drug substances in aqueous suspension or as dry powder for
reconstitution (discussed next) are attractive to manufacturers.
PACKAGING AND STORAGE OF
SUSPENSIONS
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.
It is important that suspensions be shaken before each use to ensure a
uniform distribution of solid in the vehicle and thereby uniform and
proper dosage.