Lecture No.26 Pharm D.

1st

Course: Physical Pharmacy-I

Instructor: Dr. Gul Rehman Elmi

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Key Learning Objectives
❑Upon Completion of this lecture you will be able to understand:
❑Get knowledge about the formulation additives and preparation of
suspensions.

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Formulation Additives
❑In addition to vehicle, stabilizer, sweetening and flavoring agents,
following additives are required to prepare suspensions
1. Suspending and Thickening agents
2. Wetting Agents
3. Dispersing agent
4. Flocculating Agent
•Files
•Notes

Formulation Additives
1. Suspending and Thickening agents (Structured vehicles )
❑Increases apparent viscosity of continuous phase to prevent rapid
sedimentation of dispersed particles
a) Natural Polysaccharides: Gum acacia, Tragacanth, sod. Alginate
b) Semi-Synthetic Polysaccharides: Sodium Carboxymethyl
cellulose, Methyl cellulose, Hydroxypropyl methyl cellulose,
microcrystalline cellulose
c) Clays: Aluminum Magnesium Silicate, Bentonite, Hectorite
d) Synthetic Agents: Carbomer, Colloidal Silicon dioxide
Formulation Additives
2. Wetting Agents
❑Decrease hydrophobicity.
❑They get adsorbed at solid-liquid interface and promote wetting of
solid particles by liquid of dispersion medium.
a) Surfactants: polysorbates, esters, sodium lauryl sulfate, sodium
dioctyl sulfosuccinate
b) Hydrophilic Polymers: acacia, bentonite, colloidal silicon dioxide
and cellulose derivatives
c) Hydrophilic Liquids: alcohol, glycerol, propylene glycol
Formulation Additives
3. Dispersing agent
❑Aid in uniform distribution and dispersion of solid particles of
dispersed phase.
❑Wetting agents such as surfactants are often employed as
dispersing agents.
4. Flocculating Agent
❑Causes controlled aggregation of particles of dispersed phase in a
suspension.
❑They can be surfactants, electrolytes and hydrophilic polymers.
Preparation of Suspensions – general procedure
❑Reduce drug powder to desired size – HOW?
❑Add drug and wetting agent to solution
❑Prepare solution of suspending agent
❑Add other ingredients - electrolytes, color, flavor
❑Homogenize medium
❑Package
 Method of
Preparation Particles
Addition of wetting agent & dispersion medium
Uniform dispersion of deflocculated particles

A B C
Addition of Addition of
flocculating agent flocculating agent
Incorporation of
structured vehicle Flocculated suspension
Flocculated suspension
Incorporation of
as final product
structured vehicle
Deflocculated suspension
in structured vehicle as Flocculated suspension in
final product structured vehicle as final
product
 1. Suspensions containing diffusible solids

2. Suspensions containing indiffusible

Formulation solids
of 3. Suspensions containing poorly wettable
Suspensions solids

4. Suspensions of precipitate forming

liquids
1. Suspensions containing diffusible solids
❑Consist of solids insoluble in water but easily wettable.
❑On shaking with water solid particles diffuse readily via liquid and
remain suspended for long time.
❑Prepared by
▪ Triturating solids in mortar with sufficient quantity of vehicle to
form smooth cream.
▪ Soluble non-volatile substance is added by separately dissolving them
in small quantity of vehicle.
▪ More vehicles are then added and any foreign particle is strained via
muslin cloth.
▪ Any volatile component is added at this stage and adding required
quantity of vehicle makes up final volume.
❑Example: Magnesium Trisilicate Mixture
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2. Suspensions containing in-diffusible solids
❑Substances do not remain distributed in dispersion medium when
shaken for long time to ensure uniformity of dose.

❑Prepared by adding a suitable thickening agent to vehicle, which

increases viscosity of vehicle and delays separation or
sedimentation of in-diffusible particles.

❑Example: Calamine Lotion

 Consist of poorly soluble and poorly
wettable substances that clump together
with difficulty to disperse.

3. Suspensions Prepared by including suitable wetting

agent in formulation.
containing
poorly wettable These agents get adsorbed at solid/liquid
solids interface and promote wetting of solid
particles by liquid of dispersion medium.

Example: Sulphur Lotion

4. Suspensions of precipitate forming liquids
Consist of liquid tinctures - alcoholic or hydroalcoholic extract of
vegetable drugs which contain resinous material.
When tinctures are added to water they precipitate.
Precipitates are in-diffusible and stick to walls of container.

Prepared by adding suitable thickening agent prior to addition of

precipitate forming liquid - ?
Example: Lobelia and Stramonium Mixture
 Packaging and Storage of
Suspensions
❑Should be packaged in wide mouth containers
having adequate air space above liquid.
❑Should be stored in tight containers protected from:
freezing, excessive heat & light
❑Label: "Shake Before Use" – Why?
❑Stored in room temperature when dry powder
❑Stored in refrigerator after opening or reconstitute
(freezing should be avoided to prevent aggregation)
 Mian Problem in Stability of Suspension
❑Caking
❑Flocculation
❑Particle growth
❑Adhesion of particles to container wall
❑Sedimentation

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 A-Physical stability
• Appearance, color, odor and
taste B-Chemical stability:
Stability of • pH • Degradation of active
ingredient
• Specific gravity
Suspensions • Sedimentation • Viscosity change
• Zeta potential measurement • antimicrobial activity:
• Compatibility with container
• Compatibility with cap liner
• Microscopic examination
• Determination of crystal size
• Determination of uniform
drug distribution
Pharmaceutical Applications of Suspensions
1.Insoluble drug or poorly soluble drugs which required to be given
orally in liquid dosage forms (in case of children, elderly, and
patients have difficulty in swallowing solids dosage forms)
2.To mask taste:
▪ Examples, paracetamol suspension & chloramphenicol palmitate.
3.Some materials are needed to be present as finely divided forms to
increase surface area. For example, Mg carbonate and Mg trisilcate
are used to adsorb some toxins

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Pharmaceutical Applications of Suspensions
4. Suspension can be used as topical applications:
▪ Example calamine lotion BP  after evaporation of dispersing
media; the active agent will be left as light deposit
6. Can be used for parenteral administration  I/M to control rate of
absorption
7. In vaccines e.g., Diphtheria and Tetanus vaccines
8. X-ray contrast media: example, propyliodone oral and rectal
administration
9. In aerosol  suspension of active agents in mixture of propellants

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Pharmaceutical Applications of Suspensions

10. To over come instability of certain drug in aqueous solution:

a) Insoluble derivative formulated as suspension
▪ Example, oxytetracycline HCL (instable)  calcium salt (stable)
a) Reduce contact time between solid drug particles and dispersion
media  increase stability of drug like Ampicillin by making it as
reconstituted powder.
b) A drug that degraded in presence of water  suspended in non-
aqueous vehicles. Examples, phenoxymethypencillin/ coconut
oil and tetracycline HCL/ oil
Thank You – Your Questions?

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