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Pharmaceutics > Oral Solutions > Flashcards

Oral Solutions Flashcards

1
Q

What is a solution?

A

A mixture of two or more components that form single homogenous phase at molecular level

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2
Q

What is a solute?

A

Components dispersed as molecules or ions in solvent

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3
Q

What is a solvent?

A

Liquid capable to dissolve a substance + usually major component in a solution + determine phase of system

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4
Q

Is a solution optically clear?

A

YES

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5
Q

What are the advantages of solutions?

A

Fast onset of action
Dose uniformity assured = doesn’t need shaking
Vol of liquid dose can be measure accurately
Easy to swallow
Easy to manufacture

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6
Q

What are the disadvantages of solutions?

A

Increased drug instability compared to solid state
Some liquids require cold storage to maintain shelf-life
Many drugs poorly soluble in H2O
Liquids bulky to carry
Packaging costs higher

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7
Q

What are the oral solution properties?

A 
Stable throughout shelf-life 
Palatable: flavouring + colouring added
Appropriate viscosity for palatability + pourability
At physiological pH where possible  
Dose in multiples pf 5ml for convenience
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8
Q

What is the most solvent?

A

H2O

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9
Q

Why is H2O most common solvent?

A

Lack of toxicity

Low cost

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10
Q

What is problem with H2O as solvent?

A

Contains dissolved substances that could interfere with drug formulation

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11
Q

What must happen to H2O if solvent for manufacturing of oral solutions?

A

Purified

Produced by distillation, ion exchange or reverse osmosis

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12
Q

What co-solvents are used?

A

Ethanol, propylene glycol + glycerol

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13
Q

Why are co-solvents used?

A

Many drugs not H2O soluble

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14
Q

What do co-solvents do?

A

Less innocuous than water = conc within formulation low

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15
Q

Why does drug conc need to be below saturation solubility?

A

To avoid drug precipitation

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16
Q

What excipients are used?

A 
Viscosity enhancers
Preservatives
Sweeteners
Antioxidants
Flavouring agents
Colouring agents 
Other for non-oral solutions
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17
Q

Why are viscosity enhancers used?

A

Improve pourability

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18
Q

What are examples of viscosity enhancers?

A

Hydroxyethyl, cellulose, povidone, carbomer + glycerol

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19
Q

Why are preservatives used?

A

Prevent microbial growth

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20
Q

What are examples of preservatives?

A

Benzoic acid, benzalkonium chloride, sodium benzoate + glycerol

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21
Q

Why are sweeteners used?

A

Improve palatability of oral solutions

22
Q

What are examples of sweeteners?

A

Sucrose, sorbitol + mannitol

23
Q

Why are antioxidants used?

A

Improve stability of solutions by minimising oxidation

24
Q

What are examples of antioxidants?

A

Ascorbic acid + sodium bisulphate

25
Q

Why are flavouring agents used?

A

Mask unpleasant taste of drugs

26
Q

What are examples of flavouring agents?

A

Vanilla, orange oil, menthol + liquorice

27
Q

Why are colouring agents used?

A

Correlate with flavouring agent

28
Q

What are examples of colouring agents?

A

Green with mint

Red with strawberry

29
Q

What other excipients may be added for non-oral solutions?

A

Density modifiers

Isotonicity modifiers

30
Q

Why must a solution remain stable?

A

For shelf-life

31
Q

What properties of solution must remain the same for stability?

A 
Physical
Chemical 
Microbiological 
Therapeutic 
Toxicological
32
Q

What causes solution degradation?

A

High temp
pH
UV light
Catalyst

33
Q

What enhances solution stability?

A

Formulate at suitable pH
Include excipients that enhance product stability
eg. antioxidants
Packaged in containers that reduce light transmission
Purging solution with nitrogen to create nitrogen headspace

34
Q

When are excipients stable?

A

Non toxic
Compatible with drug, containers + other excipients
Functional throughout shelf life

35
Q

What does drug solubility depend on?

A 
Molecular structure
Crystal structure
Particle size
pKa
pH of medium
36
Q

What can you use to increase drug solubility?

A

pH modification
Co-solvents
Complexation
Surfactants + micelles

37
Q

What can altering pH of medium cause?

A

Increase drug ionisation = increase drug solubility

38
Q

What is ionisation governed by?

A

pH = pKa + log (base/acid)

39
Q

When are WA drugs ionised?

A

When solvent pH increased

HA ⇌ H+ + A-

40
Q

When are co-solvents used?

A

Used for non-ionic drugs where solubility cannot be adjusted by pH control

41
Q

What do non-polar drugs dissolve in?

A

Non-polar solvents

42
Q

Describe cyclodextrin complexation

A 
Family of compounds made up of sugar molecules bound together in a ring
6-membered sugar ring = alpha
7-membered = beta
8-membered = gamma 
Hollow truncated cone shape 
Interior cavity hydrophobic
Exterior hydrophilic
43
Q

What can cyclodextrin do because of hydrophobic interior?

A

“Capture” hydrophobic molecules via non-covalent bonds

44
Q

What can cyclodextrin do because of hydrophilic exterior?

A

Highly H2O soluble

45
Q

What is cyclodextrin overall effect?

A

Increase solubility of drug

46
Q

What happens with cyclodextrin oral administration?

A

Drug released from cyclodextrin + free drug absorbed

47
Q

What do surfactants + micelles have to pass?

A

Hydrophilic head + hydrophobic tail

48
Q

What happens to surfactants + micelles?

A

Accumulate at boundary between 2 phases

49
Q

What do surfactants + micelles do?

A

Reduce surface tension of liquids

50
Q

What can surfactants + micelles do to poorly H2O soluble drugs?

A

Solubilise in micelles to enhance drug solubility

Pharmaceutics (21 decks)

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