Buccal + Sublingual Application Flashcards

1
Q

What is buccal delivery through?

A

Cheek lining

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2
Q

What is buccal delivery generally used in?

A

Treatment of chronic disorders when a prolonged release is required

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3
Q

What is sublingual delivery through?

A

Under the tongue

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4
Q

What is sublingual delivery used for?

A

Treatment of acute disorders for fast actions

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5
Q

What is the oral cavity lined with?

A

Uninterrupted mucosal membrane

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6
Q

What does the mucosal lining consist of?

A

Epithelial membrane
Basement membrane
Lamina propria + submucosa

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7
Q

Describe the non-keratinised oral epithelium

A

Flexible
Found in soft palate, buccal region

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8
Q

Describe keratinised oral epithelium

A

Dehydrated
Mechanically tough + chemically resistant
Barrier to drug absorption
Found in gums + hard palate (roof of mouth)

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9
Q

What is the transcellular route?

A

Crossing the polar + lipid domain of the cell membrane
For lipophilic drugs

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10
Q

What is the paracellular route?

A

Through intercellular aqueous space between cells
For hydrophilic drugs

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11
Q

What are factors affecting drug absorption?

A

Lipophilicity
Solubility in saliva
Ionisation
Binding to oral mucosa
Thickness of oral epithelium

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12
Q

Why are conventional oral dosage forms not suitable for buccal drug formulation?

A

Washing effect of saliva + mechanical stress

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13
Q

What are the most common buccal formulations?

A

Tablets + patches

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14
Q

What is used in buccal formulation to improve mucosal contact?

A

Mucoadhesive agents
Penetration enhancers
Enzyme inhibitors
Backing membrane

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15
Q

What are mucoadhesive agents?

A

Materials that bind to mucus layer of membrane

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16
Q

What do mucoadhesive agents do?

A

Maintain an intimate + prolonged contact of the formulation with thew absorption site

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17
Q

What are examples of mucoadhesive agents?

A

Mucoadhesive polymers
PAA
PVA

18
Q

How do mucoadhesive polymers work?

A

Polymer hydrates
Swells = flexible chain allows interpenetration between polymer + mucin chain

19
Q

When are penetration enhancers added?

A

For systemic effect

20
Q

What must penetration enhancers be?

A

Non-irritant
Reversible effects

21
Q

What are examples of penetration enhancers?

A

Fatty acids
Surfactants
Bile salts

22
Q

How do enzyme inhibitors work?

A

By affecting enzyme activities

23
Q

Why are enzyme inhibitors used?

A

To improve buccal absorption of drugs, particularly peptides

24
Q

What does a backing membrane do?

A

Prevent drug loss + offers better patient compliance

25
Q

What are examples of backing membranes?

A

Carbopol
Magnesium stearate

26
Q

What is the ideal molecular size for buccal delivery?

A

Less than 500 Da

27
Q

What is the ideal log P for buccal delivery?

A

1.6-3.3

28
Q

What should the drug be stable for?

A

Buccal pH 6.4-7.2

29
Q

Describe buccal tablets

A

Small, flat, oval shape
Monolithic + 2-layered matrix

30
Q

What is the limitation of buccal tablets?

A

Small contact surface
Extended contact = cause irritation

31
Q

Describe buccal monolithic tablets

A

Mix of drug with swelling bioadhesive release polymer with bidirectional release

32
Q

What can buccal monolithic tablets be coated?

A

On outer or three sides with H2O impermeable hydrophobic substance

33
Q

Describe buccal 2-layered matrix, local action

A

Inner layer based on a bioadhesive polymer + outer non-bioadhesive layer containing drug for bi-directional release

34
Q

Describe buccal 2-layered matrix, systemic action

A

Drug loaded into inner bioadhesive layer
Outer layer is inert + acts as protective layer

35
Q

Describe buccal patches/films

A

Long, flat, thin film with high SA

36
Q

Why do buccal patches have higher patient compliance?

A

Physical flexibility + softness

37
Q

What does buccal patches consist of?

A

Impermeable backing layer + drug-containing layer that has mucoadhesive properties

38
Q

Describe the drug absorption of sublingual

A

Rapid due to relatively thin + high permeable sublingual mucosa + profuse blood supply

39
Q

What is the sublingual route effected by?

A

Constantly washed by saliva + movements of the tongue

40
Q

What is critical in sublingual formulation because there is rapid disintegration + dissolution?

A

Small tablet size
Low hardness
High porosity

41
Q

Because sublingual tablets have a high porosity + low hardness, what does it mean?

A

More friable
= need to be careful with packaging

42
Q

What do you advise the patient with sublingual tablets?

A

Avoid chewing or swallowing the tablets
Avoid eating/drinking during administration