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Pharmaceutics 2 - Winter > 3 - Buccal/Sublingual > Flashcards

3 - Buccal/Sublingual Flashcards

1
Q

How can nitroglycerin be administered?

A
  • Sublingual
  • Buccal
  • Transdermal
  • Oral
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2
Q

Oral mucosa is similar to ____ in terms of drug absorption characteristics

A

Skin

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3
Q

What composes the lining of the stomach and intestines? What does it do?

A
  • Simple epithelium, w/ single layer of cells

- Allows passage/absorption of nutrients, water, and other components

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4
Q

What covers the oral mucosa? Why?

A

Stratified epithelium composed of multiple layers of cells b/c of the functional demands of the tongue and mouth (speech, food digestion)

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5
Q

What are the 3 types of oral mucosa in the mouth?

A

1) Masticatory mucosa
2) Lining mucosa
3) Specialized mucosa

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6
Q

Is blood flow through the oral mucosa a rate-limiting factor in buccal or sublingual drug absorption?

A

No

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7
Q

What does a high drug concentration in saliva mean?

A

Greater chance for drug penetration across oral mucosa

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8
Q

Where does buccal absorption occur?

A

Cheek lining

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9
Q

Where does sublingual absorption occur?

A

Tongue and mouth floor

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10
Q

Does the buccal or sublingual area have a thinner mucosa? Which has a greater blood flow? Which has faster absorption?

A
  • Thinner mucosa in sublingual
  • Greater blood flow in buccal
  • Faster absorption in sublingual
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11
Q

What are characteristics of buccal and sublingual absorption?

A
  • Direct systemic absorption
  • Fast onset (b/c drugs are absorbed directly into circulation)
  • Convenient application
  • Limited absorption
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12
Q

Are buccal and sublingual considered primary or alternative administration methods?

A

Alternative, so only used when absolutely necessary

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13
Q

When are buccal/sublingual drugs used?

A
  • Emergencies
  • Replacement of injection
  • Drugs w/ extensive first-pass metabolism
  • Uncooperative/unconscious px
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14
Q

Why are sublingual and buccal administrations used in emergency situations?

A

B/c drug can reach max blood concentration is a short period of time

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15
Q

What are the excipients found in lorazepam?

A
  • Cornstarch
  • Lactose
  • Microcrystalline cellulose
  • Magnesium stearate
  • Colorants
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16
Q

Is there a difference btwn oral and buccal/sublingual absorption?

A

No

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17
Q

Will ionized or un-ionized drug molecules penetrate oral mucosa more easily?

A

Un-ionized

18
Q

What is the difference between transcellular and paracellular transfer?

A
  • Transcellular = lipophilic compounds, direct and short

- Paracellular = hydrophilic compounds, long b/c travelling btwn cells as opposed to right through

19
Q

What determines the rate of drug diffusion for buccal/sublingual drugs?

A

Diffusion coefficient of drug molecule w/in epithelium

20
Q

Do larger molecules have lower or higher diffusivity and why?

A

Lower b/c more difficult to move about

21
Q

How much saliva is secreted per day?

A

0.6-1.5 L

22
Q

What is the pH of saliva?

A

5-7

23
Q

What in vivo conditions affect drug absorption buccally and sublingually?

A
  • Mucosa condition
  • pH
  • Saliva flow
24
Q

What are the in vivo requirements for a drug to be appropriate for buccal/sublingual absorption?

A
  • Small molecule
  • Small dose (10-20 mg)
  • Low therapeutic concentrations
  • Short half-life
  • Low irritability/allergenicity
  • Favourable taste
25
Q

What is the total amount of drug that can be systemically delivered across the buccal and sublingual mucosa in 1 day?

A

10-20 mg

26
Q

What are the formulation requirements for a drug to be appropriate for buccal/sublingual absorption?

A
  • Fast disintegration
  • Fast drug availability
  • Few excipients present
  • Appropriate size, shape, texture
  • Favourable taste, odour
  • No interference w/ normal oral functions
27
Q

What are the traditional formulations of buccal and sublingual products?

A
  • Solutions
  • Molded tablets
  • Tablets
  • Sprays
  • Film strips
28
Q

What are some common excipients in buccal and sublingual products?

A
  • Sucrose
  • Lactose
  • Dextrose
  • Sorbitol
  • Mannitol
  • Starch, cellulose
  • Disintegrants
29
Q

Chewing gum provides a ____ drug release

A

Prolonged

30
Q

Bioadhesive tablets provides a ____ drug release

A

Prolonged

31
Q

What are some shortcomings of the bioadhesive tablet?

A
  • Less functional interference
  • Physical inflexibility, may induce irritation or allergy
  • Slow drug release
32
Q

What are some factors that affect drug release from bioadhesive preparations?

A
  • Nature of polymer used
  • Drug/polymer ratio in dosage
  • Swelling kinetics of preparation
33
Q

What are some polymers used in a hydrogel?

A
  • Hydroxypropyl cellulose
  • Hydroxyethyl cellulose
  • Hydroxypropylmethyl cellulose
  • Sodium carboxymethyl cellulose
  • Polyacrylic acid
34
Q

What is a major concern w/ the oral patch?

A

Very slow drug release b/c drug molecules have to diffuse through adhesive layer before reaching saliva

35
Q

What is tested during quality control of buccal/sublingual products?

A
  • Content uniformity
  • Disintegration testing
  • Packaging conditions
  • Dissolution testing in modified release preparations
36
Q

Do permeation enhancers have any pharmacological effects?

A

No

37
Q

What are permeation enhancers used for?

A
  • Facilitate drug permeation or absorption

- Increase bioavailability of drug substances that possess normally poor membrane penetration

38
Q

Do permeation enhancers have an effect on biological membranes?

A

Yes, but temporary and reversible

39
Q

What are the mechanisms of permeation enhancers?

A
  • Disrupt cell structure
  • Extract intercellular lipids
  • Form micelles
  • Inhibit enzyme activity
40
Q

What is a concern w/ permeation enhancers?

A

Adverse effects and toxicity

Pharmaceutics 2 - Winter (4 decks)

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