Pharmaceutical Suspensions

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PHARMACEUTICAL

SUSPENSIONS

SUSPENSIONS
CONTENTS
Definition.

Classification.

Advantages & disadvantages.

Applications

Theoretic consideration of suspensions.

•Sedimentation
•Brownian movement
•Electrokinetic properties

SUSPENSIONS
DISPERSE SYSTEM

The term "Disperse System" refers to a system in which one


substance (The Dispersed Phase) is distributed, in discrete
units, throughout a second substance (the continuous
Phase ).

Each phase can exist in solid, liquid, or gaseous state .

Suspensions are heterogeneous system consisting of 2


phases.
3 SUSPENSIONS
Definition

A Pharmaceutical suspension is a coarse dispersion in which internal


phase/insoluble solids (therapeutically active ingredient)is
dispersed uniformly throughout the external phase with the help of
suspending agents.

4 SUSPENSIONS
 The internal phase consists of insoluble solid particles
having a size range of 0.5 to 5 microns which is
maintained uniformly throughout the suspending vehicle
with aid of single or combination of suspending agent.

 The external phase (suspending medium) is generally


aqueous in some instance, may be an organic or oily
liquid for non oral use.

5 SUSPENSIONS
A solid in liquid dispersion in which the particles are
of colloidal size.

DISPERSE SYSTEM

DISPERSED MEDIUM DISPERSED PHASE

oAqueous oily liquid oInsoluble solid

6 SUSPENSIONS
The reasons for the formulation of a pharmaceutical suspension:

• If patient has a difficulty of swallowing solid dosage


forms (a need for oral liquid dosage form).

• Faster rate of dissolution and oral absorption than


solid dosage forms, yet slower than solutions.

• Bulky insoluble powders as kaolin or chalk are better


formulated as suspensions so that they are easier to
take.

• Drugs that have very low solubility are usefully


formulated as suspensions.

• Drugs that have an unpleasant taste in their soluble


forms (e.g., chloramphenicol (soluble) vs.
chloramphenicol palmitate (insoluble). 10/13/2024
• Prolongation of effect (e.g. I.M and S.C.
suspensions).

• Stability and instability issues:


 Insoluble forms of drugs may prolong the
action of a drug by preventing rapid
degradation of the drug in the presence of
water (e.g., Oxytetracycline hydrochloride
(soluble, hydrolyses rapidly) vs
oxytetracycline calcium salt (insoluble,
stable).

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SOME MARKETED
SOME PHARMACEUTICAL SUSPENSIONS
SUSPENSIONS

1. Antacid oral suspensions


2. Antibacterial oral suspension
3. Dry powders for oral suspension
(antibiotic)
4. Analgesic oral suspension
5. Anthelmentic oral suspension
6. Anticonvulsant oral suspension
7. Antifungal oral suspension

9 SUSPENSIONS
Classification
Based On General Classes
 Oral suspension
eg: Paracetamol suspension
antacids, Tetracycline HCl.

 Externally applied suspension


eg :Calamine lotion.

 Parenteral suspension
eg: Procaine penicillin G
Insulin Zinc Suspension
10 SUSPENSIONS
Based on Proportion of Solid Particles
 Dilute suspension (2 to10%w/v solid)

Eg: cortisone acetate, predinisolone acetate

 Concentrated suspension (50%w/v solid)

Eg: zinc oxide suspension

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Based on Nature of Solid Particles

 Flocculated suspension

 Deflocculated suspension

12 SUSPENSIONS
Based on Size of Solid Particles

Colloidal suspensions (< 1 micron)

- Suspensions having particle sizes of suspended solid less than


about 1micron in size are called as colloidal suspensions.

13 SUSPENSIONS
Coarse suspensions (>1 micron)
Suspensions having particle sizes of greater than about
1micron in diameter are called as coarse suspensions.

Coarse dispersion
Barium sulphate

Nano suspensions (10 ng)


 Suspensions are the biphasic colloidal dispersions of
nanosized drug particles stabilized by surfactants.
Size of the drug particles is less than 1mm.

14 SUSPENSIONS
THEORITIC CONSIDERATION OF SUSPENSIONS

A knowledge of the theoretic considerations pertaining to


suspension s technology ultimately help formulator to select
ingredients that are

 Appropriate for suspension preparation

 That are available for milling

 Mixing equipment

15 SUSPENSIONS
Some theoretic considerations are :

 Particle size control.

 Wetting

 Sedimentation

 Brownian movement

 Electokinetic

 Aggregation
SUSPENSIONS
16
Particle size control:
- Particle size of any suspension is critical and must
be reduced within the range .
-Too large or too small particles should be avoided.
Larger particles will:
 settle faster at the bottom of the container
 particles > 5 um impart a gritty texture to the product
and also cause irritation if injected or instilled to the eye
 particles > 25 um may block the needle

-Too fine particles will easily form hard cake at the bottom
of the container.

17 SUSPENSIONS
Wetting of the particles
 Hydrophilic materials (talc, ZnO, Mg 2CO3) are easily wetted by
water while hydrophobic materials (sulphur , charcoal) are not due
to the layer of adsorbed air on the surface.

 Thus, the particles, even high density, float on the surface of the
liquid until the layer of air is displaced completely.

 The use of wetting agent allows removing this air from


the surface and to easy penetration of the vehicle into the pores.

 However hydrophobic materials are easily wetted by


non-polar liquids.

18 SUSPENSIONS
Wetting
The insoluble medicament may be :
• Diffusible solids (dispersible solids): These are insoluble solids
that are light and easily wetted by water. They mix readily
with water, and stay dispersed long enough for an adequate
dose to be measured. After settling they redisperse easily.
Examples include magnesium trisilicate, light magnesium
carbonate, bismuth carbonate and light kaolin.

• Indiffusible solids: Most insoluble solids are not easily wetted,


and some particles may form large porous clumps in the
liquid, whereas others may remain on the surface. These
solids will not remain evenly distributed in the vehicle long
enough for an adequate dose to be measured. They may not
redisperse easily. Examples for internal use includes aspirin,
phenobarbital and sulfadirnidine, and for external use
calamine, hydrocortisone, sulphur and zinc oxide.

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Wetting

 Because of the high interfacial tension between


indiffusible solids and water; air may be trapped in
these poorly wetted particles which causes them to
float to the surface of the preparation and prevents
them from being readily dispersed throughout the
vehicle.

 Wetting of the particles can be encouraged by


reducing the interfacial tension between the solid
and the vehicle, so that adsorbed air is displaced
from solid surfaces by liquid.
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Wetting

Wetting agents:
 Hydrophilic colloids such as acacia and tragacanth
can act as wetting agents.

 Intermediate HLB (hydrophilic-lipophilic balance)


surfactants such as polysorbates (tweens) and
sorbitan esters (spans) are used for internal
preparations. While Sodium lauryl sulphate is used in
external preparations.

 Solvents such as ethanol, glycerol and the glycols


also facilitate wetting.

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