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Suspension

The document provides a comprehensive overview of pharmaceutical suspensions, defining them as disperse systems where insoluble particles are distributed in a liquid medium. It classifies suspensions based on particle size, use, solid particle proportion, and electrokinetic nature, while also detailing the properties of a good suspension and methods for formulation. Additionally, it discusses the advantages and disadvantages of suspensions, packaging and storage considerations, and challenges faced during formulation such as sedimentation and flocculation.

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0% found this document useful (0 votes)
3 views

Suspension

The document provides a comprehensive overview of pharmaceutical suspensions, defining them as disperse systems where insoluble particles are distributed in a liquid medium. It classifies suspensions based on particle size, use, solid particle proportion, and electrokinetic nature, while also detailing the properties of a good suspension and methods for formulation. Additionally, it discusses the advantages and disadvantages of suspensions, packaging and storage considerations, and challenges faced during formulation such as sedimentation and flocculation.

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felay87719
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Suspension

Dr. Fatima Ahmad


• Many pharmaceutical preparations are disperse systems. The disperse
system refers to a system in which one substance ( the disperse phase)
is distributed in particulate form throughout another(the dispersion
medium or continuous phase).
• Definition:
“A pharmaceutical suspension is a disperse system in which internal
phase is dispersed as finely divided insoluble particles throughout
external phase.”
• Most pharmaceutical suspensions are aqueous, but an oily vehicle is
sometime used.
Classification of suspensions:
• Based on size:
i. Coarse suspension: suspensions, which have dispersed particles larger than 1micrometer.
ii. Colloidal suspension: suspensions having dispersed particles smaller than 1micrometer.
• Based on use:
i. Oral suspension: Paracetamol suspension, antacids
ii. Externally applied suspension: Calamine lotion
iii. Parenteral suspension: Procaine penicillin G
• Based on proportion of solid particles:
i. Dilute suspension (2-10% w/v solid) Prednisolone acetate
ii. Concentrated suspension (50% w/v solid) Zinc oxide suspension
• Based on electrokinetic nature of solid particles:
i. Flocculated suspension
ii. Deflocculated suspension
Properties of a good suspension:
1. After shaking, the medicament stays in suspension long enough for
removal of the correct dose from oral products. It can be achieved
by using suspending agent.
2. The sediment produced on standing is easily redispersed.
3. It is easily removed from container. It is pourable.
4. It is comparatively free from large particles, which spoil appearance,
give gritty taste to oral preparations and make external products
irritating to sensitive tissues.
Formulation of suspension:
• The three steps that can be taken to ensure formulation of an elegant
pharmaceutical suspension are
1. Control particle size: On small scale this can be done using a mortar
and pestle, to grind down ingredients to fine powder.
2. Use a thickening agent to increase viscosity of a vehicle, by using
suspending or viscosity increasing agent.
3. Use of wetting agent or surfactant

Coloring agents or preservatives may also be used.


General method for preparation of suspension:
1. Tare the container and weigh ingredients
2. Finely powder any ingredient not already in fine powder.
3. Mix the insoluble particles in mortar with vehicle containing wetting agent. The
ingredient of small bulk are added first and others are added in equal amounts to the
bulk already present in mortar. (doubling method)
4. Add enough vehicle to make a paste.
5. If necessary, dilute with the vehicle until pourable.
6. Examine the suspension carefully and if it contain any foreign particles, strain through
muslin or strainer.
7. Strain into tared bottle.
8. Rinse the bottle with vehicle.
9. Make up to volume with vehicle and shake thoroughly.
The difference between preparation of suspension with diffusible and indiffusible solids is
the addition of suspending agent.
Types of insoluble particles:
• Diffusible solids: (dispersible solids)
These are insoluble powders that are light and easily wetted by water. They readily
mix with water and on shaking, diffuse evenly through the liquid for long enough to
ensure even distribution in each dose. e.g. Calcium carbonate, light kaolin,
magnesium trisilicate
• Indiffusible solids:
Most insoluble solids are not easily wetted and may form large porous clumps in
the liquid. They will not remain evenly distributed in a vehicle long enough to
ensure uniformity of dose. They may not redisperse easily. e.g. For internal use
(aspirin, chalk, phenobarbitone), external use (calamine, zinc oxide,
hydrocortisone)
Types of suspending agents: (Thickening agent)
• The thickening agents used to stabilize suspensions are hydrophilic
colloids, i.e. substances that spontaneously form colloidal dispersion
with water because of an affinity between the dispersed particles and
dispersion medium.
• There are three major groups
1. Polysaccharides
2. Inorganic agents
3. Synthetic compounds
Polysaccharides:
The earliest suspending agents were natural polysaccharides but now a days semisynthetic compounds
are mostly used.
i. Natural : They are natural products; their quality and properties are variable.
Acacia: This is dried exudate from Acacia Senegal or other species of acacia. It forms viscous solutions in
water but is a poor thickener compared with other natural gums and semi synthetic compounds. It is
used in resinous tinctures. For heavy powders, acacia is combined with other thickeners and used as
compound powders or mucilage. Acacia contains an oxidase enzyme so an antimicrobial agent is
necessary (chloroform, benzoic acid).
Tragacanth: This is dried extract from Astragalus Gummifer and other species of astragalus. With water
it form gels, depending upon concentration. It is better thickener than acacia. Tragacanth produces less
sticky mucilage than acacia and hence suitable for external preparations. It is used in lotions, pastes and
creams.
Starch: Starch is sometimes used with other suspending agents because of the high viscosity of its
mucilage. It is ingredient of compound tragacanth powder.
ii. Semi-synthetic :
• These are derived from naturally occurring polysaccharides . The variety of
compounds differs in degree of substitute and length of cellulose chain.
Long chain molecules are more viscous. These are less susceptible to
microbial attack than natural gums.
Examples include :
• Methylcellulose
• Hydroxyethyl cellulose
• Sodium carboxymethyl cellulose
• Microcrystalline cellulose
Inorganic agents:
• Clays: These are naturally occurring inorganic materials, which are mainly hydrated
silicates. They hydrate readily, absorbing many time their own volume of water to
produce sols and gels, depending upon concentration. The gels are thixotropic i.e.
solid in absence of shearing force but become fluid when tapped or shaken.
• They are stable to heat and since hydration is quicker at high temperature, heating can
be used to fasten the preparation of dispersions.
Examples are
• Bentonite (hygroscopic powder )
7% pourable, 25% wool fat consistency, 2 % suspending indiffusible solids in external preparation)
• Aluminum magnesium silicate
0.5 -2 percent for internal and external preparation
• Hectorite
Synthetic compounds:
• These were introduced to overcome problems arising from the variable
quality of natural products.
Examples include:
• Carbomer: These are high molecular weight polymer of acrylic acid with
cross linkages of allyl sucrose. Carbomers are used as suspending agent in
low concentration. It is sensitive to oxidation when exposed to light. The
viscosity of gels are highest at pH range 6 to 11.
• Colloidal silicon dioxide: This is a form of silicon dioxide prepared by vapour
phase hydrolysis of silicon compounds(e.g. silicon tetra chloride). It acts as
thickening agent because, when suspended in a liquid the particles associate,
due to hydrogen bonding, producing a network that obstructs sedimentation.
Suspension containing poorly wettable solids:
• Some substances e.g. Sulphur and hydrocortisone are insoluble in
water and poorly wetted by it. When preparing simple aqueous
dispersions, it is difficult to disperse clumps and the form is produced
on shaking is slow to subside. To ensure satisfactory wetting, the
interfacial energy between solid and liquid must be reduced. This may
be achieved by adding wetting agent which is absorbed at solid/liquid
interface in such a way that the affinity of particles for surrounding
medium is increased.
• Example of wetting agent is Alcohol in tragacanth mucilage
Advantages of suspensions:
• Suspension can mask the bitter taste of insoluble drugs
• Insoluble drugs may be more stable
• Suspended insoluble powders are easy to swallow
• The suspension form enables easy administration of bulk insoluble
powders.
• Absorption will be quicker than solid dosage forms. High
bioavailability.
• It is possible to formulate sustained release preparations.
• Lotions will leave a cooling layer of medicament on the skin.
Disadvantage of suspension:
• Preparation requires shaking before use
• Accurate and uniform dose may not be achieved.
• Storage condition can affect disperse system
• Suspensions are bulky, difficult to transport and prone to container
breakage.
• Difficult to formulate.
Packaging, labelling and storage of suspension:
Packaging :
Suspensions are packed in the type of container appropriate to the class of dispensed medicine (i.e.
lotion, mixture) to which they belong. Suspensions that are very thick are packed in container with
wide mouth.
Labelling :
Suspensions should be labelled as
• Shake well before use
• Do not freeze
• Protect from direct light (for light sensitive preparations)
• In case of dry suspension, the specified amount of vehicle to be mixed may indicated directly on
label.
Storge :
It should be store in cool place. Freezing and very low temperatures may cause the suspended
particles to aggregate.
Problems encountered when formulating suspension:
• Sedimentation:
• Sedimentation is settling of particles or floccules under gravitational force in a liquid
dosage form. The factors affecting the rate of sedimentation of a particle are described in
stoke’s equation

• The rate of sedimentation is greater for larger particles . Also, the greater will be density
difference the greater will be sedimentation rate. Although, there is inverse relation with
viscosity of disperse medium.
Flocculation:
• The natural tendency of particles toward aggregation will determine the
properties of a suspension.
• In deflocculated suspension, the dispersed solid particles remain
separate and settle slowly. However, the sediment eventually form is
hard to redisperse and described as ‘cake’.
• In flocculated suspension, individual particles forms loose aggregates or
clumps in a suspension. Because these floccules are larger than
individual particles, the sedimentation rate is rapid but the sediments
are loose and easily dispersible.
• The deflocculated system with sufficient high viscosity or controlled
flocculation should be achieved.
Dispersion of oils in inhalations:
• One class of inhalations consists of one or more volatile oils in water
and to ensure uniform dispersion of oil on shaking, a light magnesium
carbonate, a diffusible soild, is added to absorb some of oil, and finely
subdivided the remainder. Unlike emulsification, this is better method
of dispersing oil, the powder does not interfere with free evaporation
of oil when the inhalation is added to water at about 65oC for use.
• If the quantity is not included in formula, 1g of light magnesium
carbonate for each 2ml of oil. E.g. eucalyptus oil Or 2g volatile solids
(menthol, thymol) gives satisfactory results.

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