Buccal/ Sublingual Drug Delivery

Question 1

What is the most typical and successful example of buccal/ SL drug delivery for systemic effect?

Answer 1

Nitroglycerin

Question 2

What is the benefit of administering to the oral cavity?

Answer 2

Absorbed directly into systemic circulation and achieves fast onset

Question 3

Where is sublingual administration restricted ?

Answer 3

Ventral surface of the tongue and floor of the mouth, limited area with faster absorption

Question 4

What is the area of main focus in buccal administration?

Answer 4

Lining of the cheek, large area

Question 5

What are the 5 characteristics of SL and Buccal application?

Answer 5

First systemic absorption
Fast onset of action and easily ended administration 
Convenient application
Limited absorption
Special formulation

Question 6

When is Buccal/SL administration appropriate?

Answer 6

Emergency use
To replace injections
Candidates with extensive a first pass metabolism
Uncooperative/unconscious patients

Question 7

What is the major difference between the oral mucosa and the GI mucosa?

Answer 7

The thickness. There are multiple, stratified epithelial layers in the oral mucosa and only a single layer in the GI.

Question 8

What are the three types of oral mucosa in the mouth?

Answer 8

Masticatory, lining and special.

Question 9

What component of the oral cavity has the thickest epithelium/epidermis and what has the thinnest?

Answer 9

Buccal (Mean thickness of 580 mcm)

Epidermis (Mean thickness of 120mcm)

Question 10

The epithelial cell membrane is ________ and the intracellular space is relatively ___________

Answer 10

Lipophilic

Hydrophilic

Question 11

The mosaic of hydrophilic and lipophilic regions allow for two mechanisms of drug transport:

Answer 11

Transcellular (Lipophilic drug, directly trough cells)

Paracellular (Hydrophilic drug, longer)

Question 12

The fast blood flow in the oral mucosa allows for what type of transfer and what are the critical factors involved?

Answer 12

Passive diffusion

Initial concentration and Membrane thickness

Question 13

Name the 3 major glands that supply saliva.

Answer 13

Parotid, Sublingual and Submandibular

Question 14

What pH range in the saliva creates the optimal environment for absorptive, nonionized drugs?

Answer 14

5.8- 7.4

Question 15

What are the functions of saliva?

Answer 15

Digest, mineralized, lubricate

Question 16

What are the three factors that effect drug penetration?

Answer 16

Drug Candidates
In vivo Conditions
Formulations

Question 17

Solubility, partition coefficient, permeability, taste, good diffusion (small MW) and stability/irritability are all factors determining what?

Answer 17

Drug Candidates

Question 18

What are the three main in vivo conditions?

Answer 18

Mucosa conditions, pH and saliva flow.

Question 19

What characteristics in the drug formulation are necessary to consider?

Answer 19

Drug release, retention, taste, shape, size, texture and irritability.

Question 20

The ________ the drug concentration in the saliva, the better the chance for drug concentration across the mucosa.

Answer 20

Higher

Question 21

Do we want a smaller or larger molecular weight in our drug candidates?

Answer 21

Smaller; easier to penetrate

Question 22

What are the 4 In vivo requirements, not including taste and low irritability?

Answer 22

Small molecules (200-300MW)
Small dosing (10-20mg)
Low therapeutic concentration
Short half life

Question 23

What are the 5 formulation requirements?

Answer 23

Fast disintegration; fast drug availability; few excipients present; appropriate shape, size and texture; no interference with normal oral function.

Question 24

What are the traditional formulations?

Answer 24

Solutions, tablets, sprays, film strips

Question 25

This formulation allows a prolonged drug release but can also have a high drug loss from swallowing into the stomach.

Answer 25

Chewing gum

Question 26

What are some ways to increase drug release in chewing gum?

Answer 26

Buffer, coating, solubilizing agents, solid dispersion and chewing vigor

Question 27

What are some drug candidates for chewing gum?

Answer 27

Local: chlorohexidine, sulfonamides, fluoride Systemic: Nicotine

Question 28

This formulation is immobile, with prolonged drug release and less functional interference than most.

Answer 28

Bioadhesive tablet

Question 29

What are in bioadhesive tablets that allow them to stick to the surface?

Answer 29

Hydrogels. They swell, stick and release drug

Question 30

This formulation is an immobile system with prolonged release and is a unidirectional drug release.

Answer 30

Oral patch

Question 31

What are the two types of oral patches?

Answer 31

Matrix | Reservoir

Question 32

Release is constant in which formulation?

Answer 32

Oral patch

Question 33

True Or False? The more excipients in the oral patch, the better.

Answer 33

False. Excipient selection is very important.

Question 34

What are the 3 methods of quality control?

Answer 34

Content uniformity Package conditions Disintegration testing *dissolution testing is unnecessary

Question 35

Substances to facilitate drug absorption by having temporary, reversible effects on membrane, but have no active pharmacological agents.

Answer 35

Permeation Enhancers

Question 36

What are four enhancement mechanisms?

Answer 36

Disruption of cell structure Extraction of intracellular lipids Formation of micelles Inhibition of enzyme activity