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a. SL12102: The science of medicines > L32 - Absorption: Sublingual, Buccal And Rectal Drug Delivery > Flashcards

L32 - Absorption: Sublingual, Buccal And Rectal Drug Delivery Flashcards

1
Q

What is topical drug delivery to the mouth used to treat? (3)

A
  • ulcers
  • fungal infections
  • periodontal disease
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2
Q

What are the different transmucosal delivery? (2)

A
  • sublingual
  • buccal
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3
Q

What has a signigicant effect on drug absorption?

A

They physiology of the mouth

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4
Q

What is the lining of the mouth?

A

Oral mucosa
(Buccal, sublingual, gingival, labial, palatal mucosae)
200cm2 (buccal + sublingual)

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5
Q

What is the structure of the oral mucosa? (4)

A
  • epithelium (membrane coating granules from prickle cells)
  • basement membrane
  • lamina propria
  • sub-mucosa
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6
Q

What are the different mucosal types? (3)

A
  • masticatory (gingival, palatal tissue)
  • lining (buccal, sublingual tissue)
  • specialsied (dorsal tongue)
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7
Q

What is the structure, thickness (mcm), permeability, residence time and % area of masticatory gingival tissue? (5)

A
  • K
  • 200mcm
  • poor
  • intermediate
  • 50%
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8
Q

What is the structure, thickness (mcm), permeability, residence time and % area of masticatory palatal tissue? (5)

A
  • K
  • 250mcm
  • poor
  • very good
  • 50%
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9
Q

What is the structure, thickness (mcm), permeability, residence time and % area of lining buccal tissue? (5)

A
  • NK
  • 500-600
  • intermediate
  • intermediate
  • 30&
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10
Q

What is the structure, thickness (mcm), permeability, residence time and % area of lining sublingual tissue?

A
  • NK
  • 100-200
  • very good
  • poor
  • 30%
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11
Q

What is the structure, thickness (mcm), permeability, residence time and % area of specialised dorsal tongue tissue?

A
  • K/NK
  • n/a
  • n/a
  • 20%
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12
Q

What goes through transcellularly?

A

Small lipophilic drugs
- passive diffusion, epithelial thickness affects flux

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13
Q

What goes through paracellularly?

A

Small hydrophilic drugs
- epithelial thickness affects flux
- intracellular lipids (MCGs)

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14
Q

What is the pH of oral cavity?

A

Approx 5.6-7.6
Log P values generally 1-5

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15
Q

What is saliva composed of?

A

Water + mucus, electrolytes and enzymes
- 0.5-2.0 L per day, 1.1 mL present

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16
Q

What are degraders in the saliva? (5)

A
  • Aminopeptidases,
  • carboxypeptidases
  • esterases
  • carbohydrases
  • lysosymes
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17
Q

What is saliva wash out?

A

Aid or hinder drug asborption

18
Q

What type of barrier is mucus? (2)

A
  • physical (30.400mcm)
  • chemical (-ve charge)
19
Q

What is blood supply like in the mouth? (2)

A
  • good blood fow (Buccal = 2.4 ml min-1 cm-2, Sub-lingual = 0.97 ml min-1 cm-2)
  • Avoids hepatic first-pass metabolism
20
Q

What are other factors that affect oral delivery? (4)

A
  • residence time
  • taste
  • irritation
  • compliance
21
Q

What is the bioavailability of subingual nitroglycerin?

A

38%
- rapidly absorbed sublingually

22
Q

What happens to sublingual nitroglycerin?

A

trinitroglycerine to dinitroglycerin to monoglycerine to glycerine

23
Q

What are alternative administration routes of the buccal testosterone delivery? (4)

A
  • oral
  • IM
  • SC implant
  • dermal (patches or gel)

Controlled drug delivery system

24
Q

What is buccal testosterone delivery like? (2)

A
  • well tolerated for long-terms use
  • common adverse events are local irritation and dysgeusia
25
Q

What are traditional treatment of BCP of opioid delivery? (2)

A
  • background analgesia
  • typical breakthrough pain episode before treatment with normal release opioid
26
Q

What are treatment with quick onset and short duration of BCP of opioid delivery? (2)

A
  • background analgesia
  • treat with ideal rescue medicine during typical breakthrough pain episode
27
Q

What is the opiod delivery of buprenorphine? (3)

A
  • outpatient treatment of opiod addiction
  • as effective as methadone, generally safe and well-tolerated
  • once daily sublingual tablet
28
Q

What is the oral transmucosal insulin delivery composed of? (6)

A
  • insulin
  • surfactant
  • solubiliser
  • micelle-creating agent
  • emulsifying agent
  • [all exceipient found on the FDA GRAS list]
29
Q

What are features of transmucosal insulin delivery? (8)

A
  • Needle-free
  • Rapid onset of action
  • No lung deposition (absorption in the buccal mucosa)
  • Established safety profile (FDA approved excipients)
  • Precise dose control (meets USP guideline)
  • Expected Improvement in Compliance
  • Easy self-administration
  • Convenient to carry and handle
30
Q

What are advantages of sublingual/buccal delivery? (8)

A
  • access and ease
  • large SA
  • rich blood supply
  • low metabolism
  • avoids hepatic first pass
  • low variability
  • prolonged contact
  • alternative to oral delivery
31
Q

What are disadvantages of sublingual/buccal delivery? (5)

A
  • high MW drugs must be potent
  • adverse reactoins
  • saliva & mucus
  • acceptance
  • development cost
32
Q

What is the rectal drug administration an excellent route of drug delivery for? (6)

A
  • Unconscious patients
  • Children
  • Patients that are nauseous/vomiting
  • Patients with upper GI tract disease
  • Drugs with an objectionable taste
  • Drugs extensively degraded via oral delivery
33
Q

What are rectal dosage forms? (5)

A
  • suppositories
  • capsules
  • tablets
  • ointments, creams & gels
  • solution, emulsions & suspensions
34
Q

What is the rectal anatomy? (6)

A
  • Last 15-20 cm of the colon
  • Upper and lower regions
  • ~300 cm2 (no villi)
  • Normally empty
  • ~3 ml mucus
  • pH ~7.5 - little buffering capacity
35
Q

What is transcellular and paracellular absorption dependent on? (4)

A
  • size
  • lipophilicity
  • ionisation
  • simple epithelium
36
Q

What is rectal delivery like? (3)

A
  • sustained release and absorption possible
  • metabolism of some drugs by bacteria
  • no esterase/peptidase activity - possible route for protein delivery
37
Q

What is the rectal blood supply like? (4)

A
  • highly vascularised
  • venous drainage (inferior & middle veins, lower) (superior vein, upper)
  • avoids hepatic first pass
  • complicated by anastomoses
38
Q

What is the first pass avoidance of diazepam gel?

A
  • metabolised to desmethyldiazepam (major metabolite; active) by CYP2C19 and CYP3A4 in liver (two minor active metabolites)
39
Q

What is diazepam gel who for and what for? (2)

A
  • management of selected, refractory epileptic patients
  • used to control bouts of increased seizure activity
40
Q

What are advantages of diazepam gel? (5)

A
  • Very low incidence of respiratory depression
  • Low potential for abuse
  • Does not require trained healthcare professional to administer injection
  • Serious consequences from overdose of rectal gel are rare
  • However, under-administration may be an issue (failure to control seizures)
41
Q

What are advantages of rectal delivery? (7)

A
  • safe and painless
  • avoids degradation in GI tract
  • avoids hepatic first pass
  • good range of dosages possible
  • potential extended absorption
  • good alt in certain patient groups
  • potential for protein delivery
42
Q

What are disadvantages of rectal delivery? (5)

A
  • acceptability (long term)
  • upwards movement leads to hepatic first pass
  • insertion issues
  • slow absorption (compared to oral and iv)
  • leakage

a. SL12102: The science of medicines (33 decks)

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