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Stage 3 Case 1 > Taste masking > Flashcards

Taste masking Flashcards

1
Q

What is taste masking

A

a perceived reduction of an undesirable taste that would otherwise exist.

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2
Q

Purpose of taste masking

A

Improve:

  • the taste of bitter APIs in drug formulations.
  • mouth feel (smooth vs. gritty).
  • the overall acceptability of medications to patients.
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3
Q

Why are APIs and issue in taste masking?

A

Most active pharmaceutical ingredients (APIs) have a bitter taste and/or irritate the throat making it unpleasant to take.

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4
Q

Solid dosage forms (like capsules or tablets) can effectively mask the unpleasant taste of pharmaceutical ingredients but…

A

but are problematic for children/geriatric to swallow.

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5
Q

Why are Taste masking techniques used for conventional solid dosage a problem?

A

Not suitable for other oral dosage forms.

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6
Q

Why is it much harder to mask taste in liquid formulation?

A

Have prolonged contact in the mouth, so more likely to perceive the APIs taste.

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7
Q

Geriatric population problems (2)

A

-often taking multiple medications and dosage forms
-have a greater degree of challenges with swallowing and handling
conventional tablets and capsules.

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8
Q

What is an alternative tablet that can be used for swallowing difficulties?

A

Chewable tablets

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9
Q

Why may Patients with neurological conditions be an issue?

A

May resist taking medications if the drug product is not easy to take.

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10
Q

What does the Paediatric population consist of?

A

Subgroups from babies to teenagers.

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11
Q

Why is the paediatric population difficult to formulate for?

A

Each subgroup has its own formulation requirements and need age-appropriate dosage forms like liquid dosage form.

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12
Q

Children have different needs from adults.

A
  • Dose of API and volume of liquids.
  • Inability to take some dosage forms
  • More sensitive to the bad taste etc.
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13
Q

Paediatric population is generally classified into five age groups which reflect the biological changes:

A

Preterm newborn infants: born before 38 weeks of pregnancy.

  • Term newborn infants: less than one month old
  • Infants and toddles: 1 month to 2 years old
  • Children: 2–11 years old
  • Adolescents: 12 to 16–18 years old
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14
Q

Swallowing capability

A

Swallowing capability is generally a factor of age and health status but there are significant inter-patient differences.

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15
Q

<5 months of age, infants display an extrusion reflex swallowing capability

A

They can only swallow liquids.

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16
Q

At 5-6 months, semi-solids can be taken

A

Multi particulates (powders, granules, pellets and minitablets <3mm) can be taken, often by sprinkling on soft food (if compatible).

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17
Q

At what age are they considered capable of swallowing conventional tablets or capsules swallowing capability

A

At 6 years+

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18
Q

Two things that make dosage forms more acceptable for children.

A
  • The smaller the solid dosage form, the easier to swallow by children.
  • Having an acceptable taste, smell and texture is important for any oral medicine.
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19
Q

Liquid formulations advantages (2)

A
  • Easier to swallow

- Offer flexible and accurate dosing using oral syringe.

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20
Q

Liquid formulations challenges (3)

A
  • Taste and smell of drugs can be more difficult to mask in liquids than solids.
  • Generally more expensive with limited shelf-life compared to solid dosage forms.
  • Usually requires more excipients (as compared to oral solids) and the selection of excipients must be considered with great care.
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21
Q

Excipients can cause significant adverse effects when used in paediatric formulations:

A
  • Physiology of neonates and infants differs considerably from that of adults.
  • They may not be able to metabolise or eliminate the pharmaceutical ingredients in the same manner as an adult.
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22
Q

Considerations of added excipients? (3)

A
  • What is the purpose of inclusion?
  • Is there a better alternative?
  • Is there a minimum amount?
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23
Q

Excipient adverse reaction in paediatrics: Benzyl alcohol (Oral, parenteral)

A
  • Neurotoxicity

- Metabolic acidosis

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24
Q

Excipient adverse reaction in paediatrics: Ethanol (Oral parenteral)

A

Neurotoxicity

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25
Q

Excipient adverse reaction in paediatrics: PEG (Parenteral)

A

Metabolic acidosis

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26
Q

Excipient adverse reaction in paediatrics: Polysorbate 20 & 80 (Parenteral)

A

Liver and kidney failure

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27
Q

Palatability definition

A

The overall appreciation of an medicine towards its smell, taste, aftertaste and texture. A major factor that determines patient acceptance of an oral medicine, paediatrics in particular.

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28
Q

Appearance also contributes to the overall acceptability

A

May even influence basic perception of the flavour.

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29
Q

Important thing about palatability

A

The palatability of a paediatric medicine should be satisfactory on its own merit (i.e. without mixing with food or beverages).

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30
Q

What can odour do to a formulation?

A

Odour can interact with taste.

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31
Q

How do taste sensations arise?

A

Taste sensations arise from stimulation of taste buds around the tongue.

32
Q

Structurally mature taste buds visible at…

A

at 13-15 weeks.

33
Q

When do the affective responses to odours appear in children?

A
  • Until the age of about 5,

- After age of 6, the adult pattern may be observed.

34
Q

What is taste?

A

The perception produced or stimulated when a substance in the mouth reacts chemically with taste receptors on the taste buds in the oral cavity mostly found on the tongue.

35
Q

5 tastes the tongue can sense

A 
Sweet
 Salty
 Sour
 Bitter
 Umami
36
Q

Why do children have greater difficulties to recognise tastes in mixtures

A

Due to limited analytical skills in perceptual tasks.

37
Q

Their ability to recognize a flavour may also be affected by…

A

The concentration of the flavour in the formulation and the appearance of the medication itself.

38
Q

To increase the probability that a formulation will be accepted by children it is best to avoid…

A

Unusual flavours and complex taste mixtures

39
Q

What 2 things can affect children’s attitude and preferences towards flavour.

A

-Social factors and cultural influences
-A bubble-gum or cherry flavour in combination with a high intensity sweetener may suit the US paediatric market, while
a less intense sweetness may be more appropriate for South East market.

40
Q

What might be a child’s response to effervescence or peppermint.

A

Children may find irritating sensations in the mouth unpleasant

41
Q

There are three broad approaches Taste masking techniques

A
  • To create a barrier between taste receptors and drug.
  • To make chemical or solubility modifications (controlling pH, esters of drug)
  • To overcome the unpleasant taste by adding flavours and sweeteners.
42
Q

What is one of the best methods of taste masking for solid dosage forms?

A

For solid dosage form, coating is one of the best methods of taste masking.

43
Q

How does coating technique mask tastes?

A

The coating acts as a physical barrier to the drug particles, thereby minimizing interaction between the drug and taste buds.

44
Q

Coating technique

A

It can involve coating of a tablet containing bitter API or coating of the bitter API particles themselves.

45
Q

What should polymers selected in costing do?

A

Prevent API release in oral cavity and allow its release in the absorption window of the API.

46
Q

What is the simplest from of taste making in liquids?

A

Sweeteners

47
Q

How do sweeteners mask tastes?

A

Being highly water soluble, will dissolve in saliva and coat the taste buds, thus retarding the interaction of API with taste buds.

48
Q

What is a commonly used sweetener?

A

Sucrose

49
Q

What does sucrose hydrolyse to?

A

Readily hydrolysed the intestine to the absorbable mono-saccharides fructose and glucose.

50
Q

When should sucrose be avoided?

A

Those suffering from hereditary fructose intolerance.

51
Q

What can blending different sweeteners with other ingredients like flavourants and texture enhancers do?

A

Could optimise the sensory characteristics of the drug formulation.

52
Q

Issues with sweeteners like sucrose?

A

Can cause dental caries.

53
Q

Sugar-free sweeteners

A

Increasingly used in liquid formulations to replace sugars that contribute to dental caries.

54
Q

What products are considered sugar-free?

A
  • Do not contain fructose, glucose or sucrose.

- Containing hydrogenated glucose syrup (lycasin), maltitol, sorbitol or xylitol.

55
Q

Three products that make a product ‘sugared’

A

fructose, glucose or sucrose.

56
Q

High concentrations of intense sweeteners such as sodium saccharine or aspartame may be unsuccessful in masking bitter taste in paediatric formulations.

A

Develop a bitter aftertaste at high concentrations.

57
Q

How do Complexation techniques mask tastes?

A

Decreases the amount of drug particles directly exposed to taste buds
Or decreases its oral solubility on ingestion thereby reducing the perception of bitter taste.

58
Q

β‐cyclodextrin is the most widely used complexing agent

A

It is a sweet, nontoxic, cyclic oligosaccharide obtained from starch.

59
Q

How does the API and complexing agent work?

A

The less hydrophilic API fits into the non-polar cavity of a complexing agent forming a stable complex that is hydrophilic.

60
Q

What are Pro-drugs?

A

Molecules that are initially inactive but, upon administration, are converted to active forms.

61
Q

How do pro-drugs mask tastes?

A

Prodrug formation leads to physicochemical modification of bitter loci and thereby inhibits/retards their interaction with taste receptors.

62
Q

Why are colouring agents avoided?

A

Associated with hypersensitivity and other adverse reactions in paediatrics.

63
Q

Can Azo-dyes be used in paediatric formulations?

A

No

64
Q

Can pH affect the taste?

A

Yes

65
Q

What is done with pH and flavours?

A

Used flavours associated with the different pH to help mask.

66
Q

Viscosity

A

The force required to draw a liquid from a spoon into the mouth

67
Q

Smoothness

A

Measure of the presence of particulates in a solution or suspension

68
Q

Slipperiness

A

The extent to which the product coasts the tongue and palate

69
Q

Mouthcoating

A

The extent to which the product coasts the tongue and palate

70
Q

Roughness

A

The amount of particles in the surface of a product

71
Q

Hardness

A

The force to attain deformation between the molars

72
Q

Fracturability

A

The force with which the sample breaks

73
Q

Cohesiveness

A

The degree which a sample deforms rather than crumbles, cracks or breaks.

74
Q

Denseness

A

The compactness of the cross section of the products.

75
Q

Tooth packing

A

The degree to which product sticks on the surface of the teeth.

Stage 3 Case 1 (12 decks)

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