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Stage 3 Case 1 > Quick oral relief formulations > Flashcards

Quick oral relief formulations Flashcards

1
Q

Disadvantages of oral formulations? (5)

A

Not good for acuteness and severity—e.g. angina pectoris, breakthrough cancer pain.

  1. Onset time—slow drug release and absorption.
  2. Absorption barriers—e.g. mucus, vascularity.
  3. Residence time?
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2
Q

Advantages of oral formulations? (5)

A
  1. Portable
  2. Solid dosage forms are stable
  3. Not invasive or intrusive
  4. Do not need to measure or use other equipment.
  5. Not embarrassing or stressful.
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3
Q

Oromucosal drug advantages (5)

A
  1. Rapid absorption and onset
  2. Mild environment
  3. No first-pass hepatic metabolism
  4. Non-invasive and discreet
  5. No swallowing needed
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4
Q

Oromucosal drug disadvantages (1)

A

Need to avoid eating or drinking.

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5
Q

Oromucosal drug advantages: Rapid absorption and onset

A

suited for emergencies.

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6
Q

Oromucosal drug advantages: Mild environment

A

avoids drug degradation.

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7
Q

Oromucosal drug advantages: No first-pass hepatic metabolism

A

excellent bioavailability.

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8
Q

Oromucosal drug advantages: Non-invasive and discreet

A

well accepted by patients.

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9
Q

Oromucosal drug advantages: No swallowing needed

A

can be used by dysphagic patients.

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10
Q

How much of the oral mucosa is available for frug absorption?

A

Oromucosa provides a large surface area where 60% is available for drug absorption.

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11
Q

Sublingual Placement

A

Under tongue

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12
Q

Sublingual Absorption

A

Ventral surface of tongue; floor of mouth

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13
Q

Buccal Placement

A

Between cheek and gum

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14
Q

Buccal Absorption

A

Mucosa inside cheeks

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15
Q

Drug delivery via the oral mucosa (5)

A
  1. Oral mucosa
  2. Submucosal capillaries
  3. Jugular veins
  4. Superior vena cava
  5. Arterial circulation
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16
Q

Challenges of oromucosal drug delivery (6)

A
  • Permeability
  • pH
  • Dissolution -limited fluid volume
  • Enzyme activity
  • Retention time -salivary washout
  • Taste
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17
Q

How is permeability a problem in oromucosal drug delivery?

A

Needs to go through the mucosal barrier.

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18
Q

How is pH a problem in oromucosal drug delivery?

A

pH in the mouth is neutral so not that harsh on the drug stability. May affect solubility so can affect the dissolution and absorption rate of the drug.

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19
Q

How is dissolution a problem in oromucosal drug delivery?

A

Due to the limited fluid volume in oral cavity. Relates to the saliva in the mouth.

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20
Q

How is enzyme activity a problem in oromucosal drug delivery?

A

May degrade the drug but relatively mild compared to the GI tract.

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21
Q

How is retention time a problem in oromucosal drug delivery?

A

Saliva washout presents a challenge as the drug could be swallowed with saliva.

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22
Q

How is taste a problem in oromucosal drug delivery?

A

Interacts with tastebuds so needs to taste nice.

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23
Q

3 main Salivary glands

A

G1-Parotid
G2-Sublingual
G3-Submandibular

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24
Q

How is saliva secreted from the glands?

A

Through the salivary ducts.

25
Q

Saliva

A
  • Involuntary reflex
  • pH 5.5–7.0
  • 0.5–2 L daily
  • Resting volume ~1 mL
26
Q

How does thickness of oral epithelium affect the drug absorption?

A

The thicker the slower the drug absorption and slower the onset

27
Q

How does lipids of oral epithelium affect the drug absorption?

A

The amount of lipids will dictate the permeability?

28
Q

How does keratinisation of oral epithelium affect the drug absorption?

A

More keratinised = less permeable the barrier is.

29
Q

Oral epithelium

A
  • Found on the outside
  • The main barrier
  • Highly keratinised
  • Lipid component severe as gatekeepers to diffusion.
30
Q

Basement membrane

A

Responsible for the regeneration and renewal of the oral epithelium.

31
Q

Lamina propria

A

Enriched with immune cells that protect the mucosa from invading pathogens.

32
Q

Sub-mucosa

A

Contains blood vessels and nerves. It contains the vasculature further down in the submucosa.

33
Q

Sublingual keratinisation

A

Non-keratinised

34
Q

Sublingual permeability

A

Very good

35
Q

Sublingual thickness

A

100-200um

36
Q

Sublingual surface area

A

25cm2

37
Q

Sublingual turnover time

A

20 days

38
Q

Sublingual blood flow

A

0.12 mL/min/g

39
Q

Sublingual residence time

A

Poor (as it is more washed out by saliva)

40
Q

Buccal keratinisation

A

Non-keratinised

41
Q

Buccal permeability

A

Intermediate

42
Q

Buccal thickness

A

500-600um

43
Q

Buccal surface area

A

50cm2

44
Q

Buccal turnover time

A

5-7days

45
Q

Buccal blood flow

A

0.2 mL/min/g

46
Q

Buccal residence time

A

Intermediate

47
Q

What is the mucus?

A
  • Gelatinous layer surrounding oral epithelial cells. Provides lubrication, permeability barrier, antimicrobial protection, intercellular adhesion.
  • Important for mucoadhesion of dosage forms.
48
Q

3 Properties of mucus

A
  • Thickness: 40–300 μm.
  • Composition: water and mucin (1–5%).
  • Negatively charged at physiological pH.
49
Q

Where is mucus secreted?

A

In the saliva

50
Q

Formulation characteristics Basic features:

A
  • Low effective dose.
  • Good stability in saliva.
  • Acceptable taste.
  • Rapid dissolution and absorption across oral mucosa.
51
Q

Formulation characteristics desired feature

A

Mucoadhesion (e.g. chitosan) to prolong retention time.

52
Q

Fentanyl

A 
Lipophilic.
 Basic.
 As fentanyl citrate.
 Better absorbed through oral mucosa than GI mucosa.
 First-pass metabolism.
53
Q

Actiq buccal lozenges

A 
To be sucked.
 Applicator to move lozenge around mouth.
 Composition:
 -Fentanyl citrate.
 -Dextrates hydrated (containing glucose).
 -Citric acid.
 -Disodium phosphate.
 -Artificial berry flavour.
 -Magnesium stearate.
54
Q

Citric acid

A
  • Sour taste.
  • Stimulates salivation.
  • Acidifies saliva to enhance dissolution of basic drugs.
55
Q

Abstral sublingual tablets

A 
Analgesia within 15–30 minutes.
 Tmax 22.5–240 minutes.
 Composition:
 -Fentanyl citrate.
 -Mannitol.
 -Silicified microcrystalline cellulose.
 -Croscarmellose sodium.
 -Magnesium stearate.
56
Q

Orally dispersible tablets

A 
Disintegrate rapidly in mouth 
 Low hardness.
 Porous.
 Uncoated.
 Rapid disintegration activated by water:
 -Superdisintegrant.
 -Effervescent system.
57
Q

Superdisintegrant

A 
Crosslinked polymers.
 Hygroscopic.
 Rapid 3D swelling.
 High swelling capacity.
 Typically used at 2–5%.
58
Q

Effentora buccal tablet

A 
Analgesia within 30 minutes.
 Tmax ~1 hour.
 Composition:
 -Fentanyl citrate.
 -Mannitol.
 -Sodium starch glycolate.
 -Sodium hydrogen carbonate.
 -Sodium carbonate anhydrous.
 -Citric acid anhydrous.
 -Magnesium stearate.
59
Q

Effentora buccal tablet

A
  • Remove from blister pack immediately before use.
  • Do not push tablet from blister pack.
  • Do not return to package after opening.
  • Disintegration within 14–25 minutes.
  • Remnants can be swallowed with water after 30 minutes.
  • Can also be administered subligually.

Stage 3 Case 1 (12 decks)

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