Buccal + Sublingual Application

Question 1

What is buccal delivery through?

Answer 1

Cheek lining

Question 2

What is buccal delivery generally used in?

Answer 2

Treatment of chronic disorders when a prolonged release is required

Question 3

What is sublingual delivery through?

Answer 3

Under the tongue

Question 4

What is sublingual delivery used for?

Answer 4

Treatment of acute disorders for fast actions

Question 5

What is the oral cavity lined with?

Answer 5

Uninterrupted mucosal membrane

Question 6

What does the mucosal lining consist of?

Answer 6

Epithelial membrane
Basement membrane
Lamina propria + submucosa

Question 7

Describe the non-keratinised oral epithelium

Answer 7

Flexible
Found in soft palate, buccal region

Question 8

Describe keratinised oral epithelium

Answer 8

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

Question 9

What is the transcellular route?

Answer 9

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

Question 10

What is the paracellular route?

Answer 10

Through intercellular aqueous space between cells
For hydrophilic drugs

Question 11

What are factors affecting drug absorption?

Answer 11

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

Question 12

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

Answer 12

Washing effect of saliva + mechanical stress

Question 13

What are the most common buccal formulations?

Answer 13

Tablets + patches

Question 14

What is used in buccal formulation to improve mucosal contact?

Answer 14

Mucoadhesive agents
Penetration enhancers
Enzyme inhibitors
Backing membrane

Question 15

What are mucoadhesive agents?

Answer 15

Materials that bind to mucus layer of membrane

Question 16

What do mucoadhesive agents do?

Answer 16

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

Question 17

What are examples of mucoadhesive agents?

Answer 17

Mucoadhesive polymers
PAA
PVA

Question 18

How do mucoadhesive polymers work?

Answer 18

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

Question 19

When are penetration enhancers added?

Answer 19

For systemic effect

Question 20

What must penetration enhancers be?

Answer 20

Non-irritant
Reversible effects

Question 21

What are examples of penetration enhancers?

Answer 21

Fatty acids
Surfactants
Bile salts

Question 22

How do enzyme inhibitors work?

Answer 22

By affecting enzyme activities

Question 23

Why are enzyme inhibitors used?

Answer 23

To improve buccal absorption of drugs, particularly peptides

Question 24

What does a backing membrane do?

Answer 24

Prevent drug loss + offers better patient compliance

Question 25

What are examples of backing membranes?

Answer 25

Carbopol Magnesium stearate

Question 26

What is the ideal molecular size for buccal delivery?

Answer 26

Less than 500 Da

Question 27

What is the ideal log P for buccal delivery?

Answer 27

1.6-3.3

Question 28

What should the drug be stable for?

Answer 28

Buccal pH 6.4-7.2

Question 29

Describe buccal tablets

Answer 29

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

Question 30

What is the limitation of buccal tablets?

Answer 30

Small contact surface Extended contact = cause irritation

Question 31

Describe buccal monolithic tablets

Answer 31

Mix of drug with swelling bioadhesive release polymer with bidirectional release

Question 32

What can buccal monolithic tablets be coated?

Answer 32

On outer or three sides with H2O impermeable hydrophobic substance

Question 33

Describe buccal 2-layered matrix, local action

Answer 33

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

Question 34

Describe buccal 2-layered matrix, systemic action

Answer 34

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

Question 35

Describe buccal patches/films

Answer 35

Long, flat, thin film with high SA

Question 36

Why do buccal patches have higher patient compliance?

Answer 36

Physical flexibility + softness

Question 37

What does buccal patches consist of?

Answer 37

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

Question 38

Describe the drug absorption of sublingual

Answer 38

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

Question 39

What is the sublingual route effected by?

Answer 39

Constantly washed by saliva + movements of the tongue

Question 40

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

Answer 40

Small tablet size Low hardness High porosity

Question 41

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

Answer 41

More friable = need to be careful with packaging

Question 42

What do you advise the patient with sublingual tablets?

Answer 42

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