Oral quick relief formulations

Question 1

advantages of taking medicines by mouth

Answer 1

Convenience

Onset time—fast drug release and absorption.

Question 2

disadvantages of taking medicines by mouth

Answer 2

absorption barriers—e.g. mucus, vascularity. • Residence time.

Question 3

advantages of oromucosal drug delivery:

Answer 3

– Rapid absorption and onset—suited for emergencies. – Mild environment—avoids drug degradation.
– No first-pass hepatic metabolism—excellent bioavailability. – Non-invasive and discreet—well accepted by patients. – No swallowing needed—can be used by dysphagic patients. • Disadvantages: – Need to avoid eating or drinking

Question 4

disadvantage of oromucosal drug delivery

Answer 4

• Disadvantages: – Need to avoid eating or drinking

Question 5

how much of the mucosal surface area is available for drug absorption

Answer 5

60%

Question 6

what is keratinised sublibgual or buccal

Answer 6

none

Question 7

does sublingual or buccal have very good permeability

Answer 7

sublingual

Question 8

what is the thickness of sublingual

Answer 8

100-200

Question 9

what is the thickness of buccal

Answer 9

500-600

Question 10

what is the surface area of sublingual

Answer 10

25

Question 11

what is the surface area of buccal

Answer 11

50

Question 12

what is the turnover time in days of sublingual

Answer 12

20

Question 13

what is the turnover time in days of sublingual

Answer 13

20

Question 14

what is the blood flow of sublingual

Answer 14

12

Question 15

what is the blood flow of buccal

Answer 15

0.2

Question 16

what is the residence time of sublingual

Answer 16

poor

Question 17

what is the residence time of buccal

Answer 17

intermediate

Question 18

give the flow of oromucosal drug absorption

Answer 18

Oral mucosa

Submucosal capillaries

Jugular veins

Seuperior vena cava

Arterial circulation

Question 19

challenges of oromucosal drug absorption

Answer 19

Permeability • pH • Dissolution – limited fluid volume • Enzyme activity • Retention time – salivary washout • Taste

Question 20

saliva key facts:
pH
how much we make
resting value

Answer 20

Ph is 5.5-7

We make 0.5-2L daily

Resting value is 1mL

Question 21

what is mucus important for

Answer 21

mucoadhesion of dosage forms

Question 22

thickness of mucus

Answer 22

40–300 µm

Question 23

what characteristics do you want in the formulation

Answer 23

Low effective dose. – Good stability in saliva. – Acceptable taste. – Rapid dissolution and absorption across oral mucosa.

Question 24

is fentanyl lipophillic

Answer 24

yes

Question 25

is fentanyl basic

Answer 25

yes

Question 26

is fentanyl through first pass

Answer 26

yes

Question 27

actiq buccal lozenges are in what form

Answer 27

It is in ionised form so its absorbed more rapidly than the non-ionised form in the mouth

Question 28

citric acid acidifies what

Answer 28

acidifies saliva to enhance dissolution of basic drugs

Question 29

orally dispersible tablets have what

Answer 29

Disintegrate rapidly in mouth. • Low hardness. • Porous. • Uncoated. • Rapid disintegration activated by water: – Superdisintegrant. – Effervescent system.

Question 30

what does super disintegrate mean

Answer 30

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