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Pharmaceutics Year 2 > Section 4 - Preformulation/Flavouring > Flashcards

Section 4 - Preformulation/Flavouring Flashcards

1
Q

What does flavour involve a combination of?

A

Taste, smell, touch, and sight

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2
Q

Where do taste sensations come from?

A

Taste buds located on all regions of the tongue

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3
Q

Does the tongue have specific zones for each flavour?

A

No

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4
Q

Where can taste occur?

A

On any part of the tongue and the mouth

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5
Q

What are the structures called that recognize taste?

A

Papille, located under the mucous membrane of the tongue

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6
Q

What happens when a chemical substance of a certain taste comes into contact with a sensory cell on the tongue?

A

It activates the sensory cell to transmit messenger substances, which in turn activate further nerve cells, which send impulses for a particular perception of flavour on to the brain

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7
Q

Which flavours are G protein-coupled receptors?

A

Sweet, bitter, and umami

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8
Q

What is the receptor for salty?

A

Sodium channel

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9
Q

What is the receptor for sour?

A

Unknown

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10
Q

What are the 5 basic tastes?

A
  • Sweet
  • Sour
  • Salty
  • Bitter
  • Savoury
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11
Q

Flavour acceptance may be affected by ___

A

Age

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12
Q

What flavour do children typically like?

A

Fruit

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13
Q

What flavour do adults typically prefer?

A

Acidic

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14
Q

What flavour do the elderly typically prefer?

A

Mint

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15
Q

Which functional group is sweet taste associated with?

A

Hydroxyl

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16
Q

Which ion is associated with sour taste?

A

Hydrogen ions resulting from the dissociation of acids like citric acid

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17
Q

What is salty taste associated with?

A

Many inorganic salts

- Ex: sodium and potassium chloride, magnesium chloride, sulfate

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18
Q

Which functional groups are associated with bitterness?

A

Amine functional groups

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19
Q

Which molecules are associated with umami taste?

A
  • Glutamic acid

- Aspartic acid

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20
Q

Is spicy a taste?

A

No, it is a pain signal sent via temperature and touch receptors on the tongue

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21
Q

Which flavours are effective in disguising dephenhydramine in a expectorant formulation?

A

Orange-mint

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22
Q

Which flavour is effective in disguising phenylephrine and chlorpheniramine?

A

Vanilla

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23
Q

Which flavour is effective in disguising adsorbents like kaolin and pectin?

A

Butterscotch

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24
Q

Which flavour is preferred in antacid preparation?

A

Mint

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25
Q

What are important characteristics for flavours used in formulation?

A
  • Non-toxic
  • Soluble
  • Stable
  • Compatible with the preparation
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26
Q

Is it better for a solution to be more or less viscous and why?

A

More b/c viscous materials give a better mouth-feel

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27
Q

What are 2 antibiotics that cause a metallic taste?

A
  • Metronidazole

- Clarithromycin

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28
Q

What kind of taste can ACE inhibitors cause and why?

A
  • Metallic, sweet, or salty
  • Taste buds need zinc as a cofactor and ACE inhibitors can chelate zinc and prevent it from interacting w/ the taste bud receptors
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29
Q

Why do calcium channel blockers alter taste?

A

Inhibition of calcium channels right at the taste receptors

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30
Q

What happens to the number of taste buds as a person ages?

A

They decrease

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31
Q

Are flavouring agents potent?

A

Yes

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32
Q

What can be used to flavour water-containing solutions and suspensions?

A
  • Water-soluble artificial flavours (1-4%)

- Concentrates (1-3%)

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33
Q

What can be used to help mask a bitter aftertaste?

A

Artificial marshmallow and vanilla flavourings

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34
Q

What is a flavour that can mask many bitter-tasting medications?

A

Chocolate

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35
Q

What is important to note about powdered flavours?

A

Usually require a higher concentration up to 5%

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36
Q

What are the normal concentrations of oil flavours?

A

0.1-1%

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37
Q

What are 2 common oil flavours used?

A

Peppermint and spearmint

38
Q

What are commonly used artificial sweeting agents?

A

Stevia, aspartame, acesulfame, and saccharin

39
Q

What is the normal concentration for stevia?

A

0.1-0.5%

40
Q

What is the normal concentration for aspartame?

A

0.1%

41
Q

What is the normal concentration for acesulfame?

A

0.1-0.5%

42
Q

What is the normal concentration for saccharin?

A

0.1%

43
Q

What is sodium chloride used for with respect to flavouring?

A

To reduce sourness and/or bitterness

44
Q

What does citric acid do with respect to flavouring and what is the typical concentration that is used?

A
  • Enhance fruit flavours

- 0.1%

45
Q

What is sodium chloride used for with respect to flavouring and what is the typical concentration that is used?

A
  • Adding salty tastes to medication for cats and dogs

- 1%

46
Q

Which 2 flavourings should not be given to dogs and why?

A
  • Chocolate and xylitol

- Toxicity

47
Q

How can parents or caregivers help a child take a medication that tastes bad?

A
  • Give a cold treat (slushy, ice pop, or ice chips) before or after the medication to numb the taste buds and minimize aftertaste
  • Add sweeteners (chocolate or strawberry syrup) to the dose of liquid medication
  • Give the child a lollipop after medication
48
Q

What should be done to medications that are mixed with a food or flavouring agent AT HOME by the caregiver?

A

Must be given right away so that the effectiveness of the medication is not reduced

49
Q

What is preformulation?

A

Gathering info regarding drug properties which may have a bearing on product formulation

50
Q

What is the object of the first step of development of dosage forms?

A

Developing a stable, bioavailable product with good patient acceptance

51
Q

What are organoleptic properties?

A

Description of drug substance including colour, odour, and taste

52
Q

What can be done to fix an objectionable colour?

A
  • Colouring agent

- Tablets may be coated

53
Q

What can be done to fix an objectionable odour?

A

Coating or inclusion of an aromatic excipient

54
Q

What can be done to fix an objectionable taste?

A
  • Flavouring agent
  • Coating
  • Use of an insoluble salt form
55
Q

What can be affected by the presence of trace amounts of metals?

A

Stability

56
Q

What is micromeretics?

A

Particle size, shape, and surface area of drug material

57
Q

What can micromeretics affect?

A

Physical and biopharmaceutical properties of finished dose form

58
Q

___ plays a role in homogeneity of tablets

A

Particle size

59
Q

____ and ____ will influence the flow and mixing efficiency of powders and granules

A

Size and shape

60
Q

What effect does decreasing particle size have?

A

Will increase surface area which will be in contact with excipient and atmospheric moisture and oxygen

61
Q

What problems can milling generate?

A
  • Static electricity
  • Agglomeration
  • Polymorph formation
62
Q

Product must dissolve in _______ prior to ______

A
  • Gastrointestinal fluids

- Absorption

63
Q

What effect does dissolution have on bioavailability?

A

Better dissolution means better bioavailability

64
Q

What does it mean if a drug shows acid instability?

A

An oral dose form may not be possible unless a way can be found to protect the drug from gastric acidity

65
Q

For HCl salts of oral products, what must you assess and why?

A

Assess common ion effect with chloride b/c gastric fluid has a high content of chloride ions

66
Q

What happens if Kd is slower than Ka?

A

Absorption is rate-limited by dissolution and a change in Kd will affect absorption rate

67
Q

What does a larger partition coefficient (logP) mean?

A

More affinity for organic phase

68
Q

What can you conclude when logP = 1?

A

10 parts in organic to 1 part in water

69
Q

What can you conclude when logP = 0?

A

1:1 organic:aqueous

70
Q

Is a crystalline or amorphous structure more soluble?

A

Generally amorphous

71
Q

Is a crystalline or amorphous structure more stable?

A

Crystalline

72
Q

Does a crystalline or amorphous structure show better bioavailability?

A

Amorphous

73
Q

For polymorphs, are all of the forms stable?

A

No, only one form is (generally in the solid state)

74
Q

Can you decipher the forms of a polymorph once in solution?

A

No

75
Q

What must a metastable polymorph exhibit to justify its use in a product?

A

Sufficient chemical and physical stability

76
Q

What must you ensure when using a drug that is capable of forming polymorphs?

A

That processing does not cause a transition

77
Q

What processes can cause polymorph transformation?

A
  • Milling
  • Granulation
  • Drying
  • Compression
78
Q

What can granulation cause?

A
  • Polymorph transformation

- Formation of solvates or hydrates

79
Q

What can drying cause?

A
  • Polymorph transformation

- Transformation to anhydrous crystalline or amorphous forms

80
Q

Knowledge of _____ is needed to know which excipients may be needed and which are most effective

A

Stability

81
Q

What are some stability studies for a tablet dose form?

A
  • Solid state stability of drug alone (chemical and physical stability)
  • Stability in the presence of potential excipients
  • Stability of the drug in solution
82
Q

What is the objective of stability studies at the preformulation stage?

A

To identify and therefore control or avoid situations where the stability of the active component may be compromised

83
Q

Which properties of a drug influence stability?

A
  • pKa
  • Solubility
  • Melting point
  • Crystal habit and form
  • Eq’m moisture content
84
Q

What are the most common factors for instability?

A
  • Light
  • Heat
  • Oxygen
  • Moisture
85
Q

What is the criteria for a stability prognosis to be good?

A

No change at 60 C after 30 days

86
Q

Why are samples tested under increasing humidity at a constant temperature?

A

In the presence of moisture many drugs hydrolyze, react with excipients, or oxidize

87
Q

What does density affect?

A
  • Flow properties

- Blending of a drug if excipients have quite different densities (segregation may occur)

88
Q

What is good flow essential for?

A
  • Blending
  • Granulation
  • Compression
89
Q

Should an excipient that increases or decreases flow properties be used?

A

Increases

90
Q

What is the preferred angle of repose?

A

25-45

91
Q

What type of compressibility is ideal?

A
  • A powder which forms a hard uniform compact under moderate pressure
  • Capping or chipping shouldn’t occur

Pharmaceutics Year 2 (17 decks)

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