IC8: Pharmaceutical Technology I

Question 1

What are the 3 regions of the nasal cavity?

Answer 1

nasal vestibule
respiratory region
olfactory region

Question 2

Which region allows access to the CNS? Via which 3 means are drugs transported across?

Answer 2

olfactory (via paracellular, transcellular or intraneuronal transport)

Question 3

Describe the transcellular route of transport

Answer 3

through active mechanisms through the cell, slow (upwards of 13h)

Question 4

Describe the paracellular route of transport

Answer 4

rapid uptake via passive transport through gaps between cells, high turnover of olfactory sensory neurons can leave more gaps,

specific requirements for molecules (Lipinski’s rule of 5)

Question 5

What are the advantages of intranasal delivery? (4)

Answer 5

• non-invasive
• can be self-administered
• bypasses FPE
• short onset of effect (big reduction in distance)

Question 6

What are the barriers to intranasal delivery? (7)

Answer 6

• nasal epithelial layer
• nasal mucus (aqueous based, drug needs to be in solution before absorption)
• metabolic enzymes
• efflux pumps
• hair
• mucociliary clearance
• volume and concentration (concentration too high, irritation; concentration too low, not enough to cross barrier)

Question 7

What are the components of Lipinski’s rule of 5?

Answer 7

• ≤ 5 H-bond donors (H attached to electronegative atom)
• ≤ 10 H-bond acceptors (LP on electronegative atom)
• < 500 Da (<300 Da for N2B access of hydrophilic drugs, <1kDa for N2B access of lipophilic drugs)
• LogP < 5
• Unionised

Question 8

What are the advantages of using delivery systems? (7)

Answer 8

1. Make the drug phyically manageable
2. Improve solubility and absorption (using liposomes and micelles)
3. Protect the drug from degradation and excretion
4. Improve drug retention (more time to exert therapeutic effect)
5. Reduce side effects through targeting
6. Increasing dosing
7. Reducing frequency of administration (also improves compliance)

Question 9

What are some common excipients in intranasal preparations?

Answer 9

diluents/fillers,
buffer salts,
preservatives,
stabilisers/co-solvents,
permeation enhancers,
viscosity modifiers

Question 10

What are the 3 considerations for nasal sprays

Answer 10

pH (7-7.4),
tonicity (300-700 mOsm)
volume (max 200 μL)

Question 11

How is imitrex/sumatriptan packaged?

Answer 11

Single use, in blister pack

Question 12

How should nayzilam/midazolam be taken?

Answer 12

one spray with symptom onset, followed by an extra dose if symptoms persist after 10 minutes

(with no more than 2 doses per episode)