Suspensions Flashcards

1
Q

What is a pharmaceutical suspension?

A

a coarse dispersion containing:
-finely divided particulate material suspended in a liquid or
semisolid medium (continuous phase or vehicle)

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2
Q

What is the criteria for a suspension?

A

particles are uniformly distributed
particles have minimal solubility in the continuous phase
the size distribution of the particles ranges from 1-100um
- 1-50um: fine dispersion
- 50-100um: coarse dispersion

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3
Q

What are the advantages of suspensions?

A

deliver poor water-soluble drugs
suitable for patients with difficulty in swallowing a tablet or capsule
palatability (masking taste)
chemical stability
sustained release
can be given for both systemic (antibiotics) and local therapeutic effects (activated charcoal to adsorb excess Gi fluids)

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4
Q

What are the disadvantages of suspensions?

A

physical instability, settling over time results in lack of uniformity of the dose
manufacturing difficulties

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5
Q

Describe the preparation of acceptable suspensions.

A

should not precipitate rapidly
redispersed quickly by shaking
correct viscosity to pour from the bottle/flow through an administration needle
for topical formulations sufficiently fluid to spread over the skin

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6
Q

What are the two phases of a suspension?

A

internal phase (drug, active, or dispersed phase)
external phase (dispersion medium, vehicle)

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7
Q

What are the solids that can be used in the internal phase of a suspension?

A

hydrophilic solids: readily wetted by water
-clays (kaolin, talc, magnesium aluminum silicate)
-hydroxides and oxides of calcium, magnesium, zinc,
aluminum & titanium
hydrophobic solids: not wetted by water, but “wetted” by oils
-most pharmaceutical substances: charcoal, sulfur, aspirin,
phenobarbital

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8
Q

What is the selection of the external phase based on?

A

safety
density
viscosity (important in stability)
taste stability

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9
Q

What are some liquids that can be used in the internal phase of suspensions?

A

polar liquids:
-water: up to 100%
-simple syrup (sucrose): 50-100%
-cherry syrup: 50-100%
non-polar liquids:
-oils: up to 100%
-fatty esters: up to 100%
-hydrocarbons: up to 100%
structured vehicles:
-acacia: 0.5-2%
-tragacanth: 0.5-5%
-carbopol: 0.5-5%
-methyl cellulose derivatives: 0.5-5%
-colloidal silicon dioxide: 1.5-3.5%

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10
Q

What are structural vehicles?

A

0.5-5% polymer in final composition
aqueous dispersions of polymeric materials

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11
Q

What are the properties of structured vehicles?

A

protective colloids at low concentrations, while they function as viscosity-inducing agents at higher concentrations
-concentration varies based on viscosity requirement
some thixotropic behaviour may also be observed (by stirring or shaking)
-not used for parenteral administration

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12
Q

What are the other ingredients used in suspensions?

A

buffers
colouring agents
flavours
sweetening agents
preservatives
suspending (flocculating) agents
viscosity modifiers

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13
Q

What are examples of suspending (flocculating) agents?

A

electrolytes
ionic surfactants
polymeric flocculating agents

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14
Q

Describe electrolytes as suspending agents.

A

capable of reducing zeta potential
ex: sodium chloride, calcium salts
concentration of electrolyte used: 0.01-1%

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15
Q

Describe ionic surfactants as suspending agents.

A

capable of decreasing zeta potential

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16
Q

Describe polymeric flocculating agents as suspending agents.

A

form a gel-like network to cross-link the suspended particles
also increase viscosity (i.e methylcellulose)

17
Q

What are examples of viscosity modifiers?

A

polysaccharides
water soluble cellulose derivatives
hydrated silicates
acrylic acid polymers
colloidal silicon dioxide

18
Q

Describe polysaccharides as viscosity modifiers.

A

used only for extemporaneous compounding because of their increased susceptibility to microbial growth
ex: acacia gum, tragacanth, alginates

19
Q

Describe water soluble cellulose derivates as viscosity modifiers.

A

semi-synthetic cellulose derivatives make greater viscosity ranges available by combining agents in specific proportions
ex: methylcellulose, MCC

20
Q

What is an examples of a hydrated silicate?

21
Q

Describe acrylic acid polymers as viscosity modifiers.

A

high molecular weight cross-linked polymers of acrylic acid forms gels in neutralized aqueous dispersions
ex: Carbopol (carboxypolyethylene)

22
Q

Describe colloidal silicon dioxide as viscosity modifiers.

A

“fluffy” white powder used as either a suspending/thickening agent or a tablet/capsule diluent

23
Q

What are the properties of an ideal suspending agent/viscosity modifier?

A

readily dissolved/dispersed without special techniques
readily and uniformly incorporated into the formulation
ensures formulation of loosely packed system (flocculated)
no effect on the bioavailability of the drug
inert, no incompatibilities with other components
stability over wide pH range

24
Q

What are some examples of oral suspensions?

A

antibiotics
antacids
radiopaque suspensions

25
What is an example of a topical suspension?
calamine lotion
26
What are some examples of parenteral suspensions?
intramuscular subcutaneous intralesional intraarticular
27
Describe deflocculated suspensions.
dispersed particles are small, discrete units the smaller the particle size, the slower the gravitational setting because of slow settling no liquid becomes trapped between particles sediment is compacted and very difficult to redisperse; small volume of sediment the supernatant remains cloudy even after settling occurs
28
What is a serious physical problem with deflocculated suspensions?
caking
29
Which type of products should not be formulated as deflocculated suspensions?
products which must be stored for a long period of time
30
Describe flocculated suspensions.
dispersed particles form loose aggregates (flocs) particles settle as flocs the rate of sedimentation is relatively rapid the sediment contains trapped liquid between flocs making the volume of sediment large and "fluffy" (a hard cake doesnt form) the loosely packed sediment is easily redispersed by moderate aggregation the supernatant is relatively clear after settling occurs
31
What are the properties of well formulated pharmaceutical suspensions?
must be easily resuspendable after shaking the dispersed phase is suspended long enough to remove a dose particles should be sufficiently small to appear smooth has suitable viscosity
32
What happens with high zeta potential?
repulsive forces>attractive forces system will be dispersed or deflocculated upon settling the suspension will cake-->difficult to resuspend
33
What happens with low zeta potential?
attractive forces>repulsive forces system will be flocculated (prevents caking)
34
What are some compounding tips for suspensions?
dust masks should be worn when working with powders aerosolizing powders make them easier to work with, by compacting them with a few drops of alcohol, water or mineral oil, as appropriate magnesium stearate, <1% enhances flowability sodium lauryl sulfate, <1% neutralizes static electricity