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Stage 3 - Case 1 (Pain) > Lecture 18, 19 & 20: Taste Masking, Quick Oral relief Formulations & Patches > Flashcards

Lecture 18, 19 & 20: Taste Masking, Quick Oral relief Formulations & Patches Flashcards

1
Q

Why is taste masking important and which formulation is hard to mask?

A
  • Many drugs have bitter taste or irritate the throat.
  • Affect acceptance and thus compliance
  • Harder to mask in liquid formualtion -> prolonged contact in mouth
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2
Q

Why is taste masking needed for paediatric formulations?

A
  • Children need different dose of API and volume of liquids. More side effects
  • Inability to take some dosage forms
  • More sensitive to bad taste
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3
Q

What are the different classes for the paediatric population?

A
  • Preterm newborn infants
  • Term newborn (0-28 days)
  • Infants and toddlers (28days-2yrs)
  • Children (2-11yrs)
  • Adolescents (12-18yrs)
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4
Q

What is the extrusion reflex?

A
  • 5-6 months
  • Solid in child, poke tongue out and push solid out. Avoid swallowing solid
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5
Q

At what age can semi solids be taken?

A
  • 5-6 months
  • Multi particulates (powders, granules, pellets, mini tablets) can be taken by sprinking on food
  • At 6 years + considered capable of swallowing conventional tablets/ capsules
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6
Q

Why is liquid formulations better for children?

A
  • Unable to swallow capsules or tablets
  • Can tailor dose better using oral syringe
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7
Q

What are the the disadvantages of liquid formulations?

A
  • Taste and smell of drugs are more difficult to mask
  • Generally, more expensive with limited shelf life
  • Usually requires more excipients (as compared to oral solids) - must be considered with great care
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8
Q

How should excipients be in paediatric populations and which are to avoid?

A
  • Should be pharmacologically inactive
  • Can cause adverse effects -> cant metabolise or eliminate excipients
  • Benzyl alcohol, ethanol - neurotoxicity and metabolic acidosis in kids
  • Polysorbate 20 & 80 - liver and kidney failure
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9
Q

What does palatability mean?

A
  • Overall appreciation of a medicine towards its smell, taste, texture and aftertaste
  • Appearance contributes to acceptability
  • Should be satisfactiory without mixing with others
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10
Q

When do children develop taste buds and what parts of the tongue can you taste sweet, salty and bitter?

A
  • Around 7-8th week of gestation. Structurally mature at 13-15 weeks
  • Sweet - front of tongue (tip), Salty - front and sides of frony, Bitter - back middle
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11
Q

What are the 3 main approaches of taste masking?

A
  • Create a barrier between taste receptors and drug (coating)
  • Make chemical or solubility modifications (controlling pH, esters of drug) - breaks down in body
  • Overcome unpleasant taste by adding flavours or sweetners
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12
Q

What is the coating technique?

A
  • Coating acts as a physical barrier to the drug particles, thereby minimising interaction between drug and taste buds
  • Either coat drug particle or compact into tablet then coat
  • Ideally, polymers selected should prevent API release in oral cavity - while allowing intended release
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13
Q

What is the adding sweetners technique in taste masking?

A
  • Simplest technique can recognise from early age and like higher levels (however can have bitter taste)
  • Highly water soluble, will dissolve in saliva and coat taste buds
  • Sucrose is most commonly used sweetner - readily hydrolysed in intestine to absorbable fructose and glucose, can cause dental caries
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14
Q

What is the alternative of adding sweetners?

A
  • Sugar free sweetners
  • Products that dont contain fructose, glucose or sucrose - sugar free
  • Contain hydrogenated glucose syrup (lycasin), maltitol, sorbitol or xylitol - sugar free
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15
Q
A
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16
Q

What are complexation techniques (Chemical or solubility modifications)?

A
  • Either decreases the amount of drug particles directly exposed to taste buds or decreases oral solubility
  • Beta cyclodextrin. Sweet, non-toxic, cyclic oligosaccharide
  • Ring has hollow space - drug sit inside and shield from taste buds. When in body it can release - can increase solubility
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17
Q

What is the taste masking pro drug technique?

A
  • Prodrugs are molecules that are initially inactive but upon administration is converted to active form
  • Pro-moeity (inactive group bound to drug by temp linkage). This changes chem structure and taste of drug
  • When in body it breaks down by pH/enzyme and active drug released
  • Pro moeity shoudnt be toxic and excreted from body
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18
Q

Why are colouring agents used and why shouldnt they be used?

A
  • Generally kids like brightly coloured preparations
  • However, should be avoided unless necessary as associated w/ hypersensitivity and adverse reactions
  • Azo-dyes = unacceptable
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19
Q
A
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20
Q

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What are some attributes of liquid formulations and solid formulations?

A
  • Liquid: Viscosity (pourability/thickness), smoothness, slipperiness, mouthcoating
  • Solid: Roughness, Hardness, Fracturability (force in which breaks), Cohesiveness, Tootpacking (sticks on teeth)
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21
Q

What are some excipients used for sensory attributes?

A
  • Propylene glycol: sweet/bitter (in high conc), oily and warming
  • Glycerin: Sweet
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22
Q

What are the requirements of acute pain relief medications?

A
  • Rapid onset within mins (tablets take hours)
  • Rapid drug dissolution
  • Rapid drug absorption
  • Minimal effort to take
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23
Q

What are the disadvantages of oral medicines?

A
  • Long transit time through GI tract: long distance to blood circulation, slow onset
  • First pass effects: GI degradation, first pass hepatic metabolism. Reduce bioavalability
  • Difficulty swallowing
24
Q

What are the 3 different oral quick relief formulations?

A
  • Oromucosal Absorption: Sublingual (under tongue), Buccal (inside cheek)
  • Dispersible: Disperse in water then drink
  • Orodispersible: Dissolve in saliva then swallow
25
Q

What are the advantages of Sublingual and buccal formulations?

A
  • Rapid onset
  • No swallowing
  • Mild oromucosal environment avoids drug degradation
  • No first pass metabolism -> good bioavailability
26
Q

What are the disadvantages of sublingual and buccal formulations?

A
  • Potential unpleasant taste
  • Salivary washout (drug needs to stay to get absorbed)
  • Interferes w/ eating and drinking
27
Q

What are the advantages of dispersible formulations?

A
  • Rapid onset - dissolution outside of body
  • Taken as a liquid, mitigating issues w/ swallowing and choking
  • Improved bioavailability
28
Q

What are the disadvanatges of Dispersible formulations?

A
  • Potential unpleasant taste
  • Potable water requirement
29
Q

What are the advantages of orodispersible formulations?

A
  • Rapid onset
  • Overcomes issues w/ swallowing and choking
  • No potable water requirement
  • Improved bioavalability
30
Q

What are the disadvantages of orodispersible formulations?

A
  • Potential unpleasant taste
31
Q

What are formulation considerations for oral quick relief formulations?

A
  • Rapid dissolution required: Superdisintegrant or effervescent disintegrant
  • Flavouring/ Sweetner - cant use coating (needs to be in contact w/ taste buds)
  • Moisture Sensitive - cause they dissolve in water readily
32
Q

What are the different layers of the oro mucosa and what layer does it need to reach to get absorbed?

A
  • Main keratinised barrier (oral epithelium)
  • Basement Membrane + Lamina Propia
  • Sub mucosa (contains blood vessels) - needs to reach to be dissolved
33
Q

Where are each of the salivary glands (Parotid, Sublingual, Submandibular) located?

A
  • Parotid: Cheek
  • Sublingual: Each side below tongue, on the floor of mouth
  • Submandibular: both sides, just under and deep to the jaw, towards the back of the mouth
34
Q

How does the drug from the mouth enter bloodstream?

A
  • Sublingual and Lingual Veins: The sublingual and lingual mucosa have a rich supply of capillaries and veins.
  • Drainage to the Internal Jugular Vein: Carries blood from head & neck to the heart.
  • Direct Entry into Systemic Circulation: flows into the superior vena cava, which leads directly to the heart. The heart then body.
35
Q

What are the characteristics of fentanyl?

A
  • Lipophilic and Basic Drug
  • Usually as salt (fentanyl citrate) - more water soluble so dissolved quickly
  • Suscepitible to First pass hepatic metabolism
36
Q

What are the characteristics of mucus and what is its function?

A
  • Gelatinous layer surrounding oral epithelial cells
  • Composition: Water & Mucin
  • Negatively charged at physiological pH
  • Provides lubrication, permeability barrier (Needs to cross for absorption) and anti microbial protection
  • Drug can stick and helps with retention
37
Q

What are the disintegrants in effervescent (dissolve and fizz) formulations?

A
  • Carbonate Salt
  • Bicarbonate Salt
  • Citric Acid
38
Q

Name some sweetners used in formulations?

A
  • Sorbitol
  • Saccharin sodium
  • Lemon flavour
  • Mannitol
  • Aspartame
39
Q

How are orodispersible tablets formulated?

A
  • Designed to be porous, pockets filled w/ air. Water gets in by capillary action. Air isnt strong in holes so less hard - easier to dissolve
  • Produced by lyophilisation
40
Q

What are superdisintegrants and name some examples?

A
  • Crosslinked polymers - can increase in vol when in contact w/ water - rapid extensive swelling
  • Crospovidone
  • Sodium starch glycolate
41
Q

What is the process of lyophilisation?

A
  • Freeze drying
  • Rapid freezing: Water freezes into ice
  • Primary drying: Ice sublimes directly into water vapour without melting
  • Secondary drying: Desorption of residual moisture
  • Dissolve quickly and leave voids and dissolves quickly
42
Q

What are the 2 ways patches deliver drugs through the skin?

A
  • Transdermal - systemic - extended release. Dermis layer than circulation
  • Transcutaneous - topical - delivers locally. Straight from skin into tissues and muscle. Shorter duration
43
Q

What are the advantages of patches?

A
  • Avoids hepatic first pass metabolism
  • Non-invasive - needle phobia (more acceptable)
  • Extended release
  • Easily applied and removable (unlike implants), can remove if ADR
44
Q

What are the disadvantages of patches?

A
  • Low deliverable doses (skin is barrier)
  • Skin irritation - non-bio plastics and adhesives can be allergic to
  • Variable absorption - sweat, wrinkle, thinner, drier, temp
45
Q

What are the main components in a patch?

A
  • Release Liner: Flap you remove before applying. Protects adhesive and contamination
  • Adhesive: Sticks to skin, contains drug (in simple)
  • Backing layer: Protects formulation, prevents occlusion (shield, covers volatile solvents from evaporating)
  • Reservoir and Matric patches (more complex) - these contain drug. Matrix controls drug release - extended release
46
Q

What are some excipients used in the drug matrix and backing layer?

A
  • Drug matrix: Dipropylene glycol, hydroxypropyl cellulose
  • Backing layer: PET film
47
Q

What are the layers of the skin?

A
  • Stratum Corneum (epidermis) - dead, metabolically active (lots of enzymes), corneocytes, most outer layer, extracellular lipid matrix
  • Dermis - Blood vessels and nerve endings
  • Hypodermis - fatty tissue
48
Q

What type of drugs are more likely to be best absorbed?

A
  • <500 Da - small
  • log P 1-4 moderately lipohilic
  • Several mg/ day
49
Q

What are the similarities and differences between different strengths of the same patch?

A
  • Release rate is greater as it increases overall.
  • However fentanyl content per patch surface area is the same. 1cm3 contains same amount as other strengths
  • Release rate per patch area is the same
50
Q

What are the different diffusion pathways?

A
  • Transcellular: Crosses straight through layers of cells
  • Paracellular: Crosses around cells
  • Appendageal : Through hair follicles and sweat glands
51
Q

What do the abbreviations Kp, D, K, h, A and J stand for?

A
  • Kp - Skin permeability coefficient
  • D - Diffusion coefficient
  • K - Skin partition coefficient
  • h - Diffusion path length
  • A - Diffusional Surface Area
  • J - Flux
52
Q

How do you test for dermal drug absorption in vitro?

A
  • Franz diffusion cell
  • Donor Chamber (drug), skin layer in between, Receptor chamber
  • Quantifies how much drug has crossed in time - absorption rate
53
Q

Why is there a lag phase in dermal drug absorption?

A
  • Can be a few hrs
  • Establishes drug diffusion path - no drug gets through
  • Takes time to get from top-bottom
54
Q

Why is there a depletion or non-sink conditions in dermal drug absorption?

A
  • Reservoir is depleted - conc gradient drops and no driving force (plateau)
  • Or drug accumulates in the skin - should keep near 0. Conc gradient drops
55
Q

What is flux?

A
  • Describes the absorption rate amount absorbed per unit time per surface area
  • Same formulation flux should be the same

Stage 3 - Case 1 (Pain) (13 decks)

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