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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
Excipient adverse reaction in paediatrics: PEG (Parenteral)
Metabolic acidosis
26
Excipient adverse reaction in paediatrics: Polysorbate 20 & 80 (Parenteral)
Liver and kidney failure
27
Palatability definition
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.
28
Appearance also contributes to the overall acceptability
May even influence basic perception of the flavour.
29
Important thing about palatability
The palatability of a paediatric medicine should be satisfactory on its own merit (i.e. without mixing with food or beverages).
30
What can odour do to a formulation?
Odour can interact with taste.
31
How do taste sensations arise?
Taste sensations arise from stimulation of taste buds around the tongue.
32
Structurally mature taste buds visible at…
at 13-15 weeks.
33
When do the affective responses to odours appear in children?
- Until the age of about 5, | - After age of 6, the adult pattern may be observed.
34
What is taste?
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
5 tastes the tongue can sense
``` Sweet Salty Sour Bitter Umami ```
36
Why do children have greater difficulties to recognise tastes in mixtures
Due to limited analytical skills in perceptual tasks.
37
Their ability to recognize a flavour may also be affected by…
The concentration of the flavour in the formulation and the appearance of the medication itself.
38
To increase the probability that a formulation will be accepted by children it is best to avoid…
Unusual flavours and complex taste mixtures
39
What 2 things can affect children’s attitude and preferences towards flavour.
-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
What might be a child’s response to effervescence or peppermint.
Children may find irritating sensations in the mouth unpleasant
41
There are three broad approaches Taste masking techniques
- 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
What is one of the best methods of taste masking for solid dosage forms?
For solid dosage form, coating is one of the best methods of taste masking.
43
How does coating technique mask tastes?
The coating acts as a physical barrier to the drug particles, thereby minimizing interaction between the drug and taste buds.
44
Coating technique
It can involve coating of a tablet containing bitter API or coating of the bitter API particles themselves.
45
What should polymers selected in costing do?
Prevent API release in oral cavity and allow its release in the absorption window of the API.
46
What is the simplest from of taste making in liquids?
Sweeteners
47
How do sweeteners mask tastes?
Being highly water soluble, will dissolve in saliva and coat the taste buds, thus retarding the interaction of API with taste buds.
48
What is a commonly used sweetener?
Sucrose
49
What does sucrose hydrolyse to?
Readily hydrolysed the intestine to the absorbable mono-saccharides fructose and glucose.
50
When should sucrose be avoided?
Those suffering from hereditary fructose intolerance.
51
What can blending different sweeteners with other ingredients like flavourants and texture enhancers do?
Could optimise the sensory characteristics of the drug formulation.
52
Issues with sweeteners like sucrose?
Can cause dental caries.
53
Sugar-free sweeteners
Increasingly used in liquid formulations to replace sugars that contribute to dental caries.
54
What products are considered sugar-free?
- Do not contain fructose, glucose or sucrose. | - Containing hydrogenated glucose syrup (lycasin), maltitol, sorbitol or xylitol.
55
Three products that make a product ‘sugared’
fructose, glucose or sucrose.
56
High concentrations of intense sweeteners such as sodium saccharine or aspartame may be unsuccessful in masking bitter taste in paediatric formulations.
Develop a bitter aftertaste at high concentrations.
57
How do Complexation techniques mask tastes?
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
β‐cyclodextrin is the most widely used complexing agent
It is a sweet, nontoxic, cyclic oligosaccharide obtained from starch.
59
How does the API and complexing agent work?
The less hydrophilic API fits into the non-polar cavity of a complexing agent forming a stable complex that is hydrophilic.
60
What are Pro-drugs?
Molecules that are initially inactive but, upon administration, are converted to active forms.
61
How do pro-drugs mask tastes?
Prodrug formation leads to physicochemical modification of bitter loci and thereby inhibits/retards their interaction with taste receptors.
62
Why are colouring agents avoided?
Associated with hypersensitivity and other adverse reactions in paediatrics.
63
Can Azo-dyes be used in paediatric formulations?
No
64
Can pH affect the taste?
Yes
65
What is done with pH and flavours?
Used flavours associated with the different pH to help mask.
66
Viscosity
The force required to draw a liquid from a spoon into the mouth
67
Smoothness
Measure of the presence of particulates in a solution or suspension
68
Slipperiness
The extent to which the product coasts the tongue and palate
69
Mouthcoating
The extent to which the product coasts the tongue and palate
70
Roughness
The amount of particles in the surface of a product
71
Hardness
The force to attain deformation between the molars
72
Fracturability
The force with which the sample breaks
73
Cohesiveness
The degree which a sample deforms rather than crumbles, cracks or breaks.
74
Denseness
The compactness of the cross section of the products.
75
Tooth packing
The degree to which product sticks on the surface of the teeth.

Stage 3 Case 1 (12 decks)

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