Pharmaceutical Technology Flashcards
Types of transport
- Transcellular
- Paracellular
- Intraneuron
Properties of transcellular transport
- Active mechanisms
- Slow (>13 hours)
Properties of paracellular transport
- Passive transport through gaps
- Rapid
- High turnover of olfactory sensory neurons can leave more gaps
Advantages of intranasal delivery
- Non-invasive
- Can be self administered
- Bypass hepatic 1st pass effect
- Short onset of action
Name the 7 barriers in intranasal delivery
- Nasal epithelial layer
- Nasal mucus (~5um)
- Metabolic enzymes
- Efflux pump
- Hair
- Mucociliary clearance
- Volume
Lipinski’s rule of 5: ≤ 5 __________
Hydrogen bonds donors
Lipinski’s rule of 5: ≤ 10 ___________
Hydrogen bond acceptors
Lipinski’s rule of 5: size
<500 Da
- < 300 Da for N2B access of hydrophilic drugs
- <1 kDa for N2B access of lipophilic drugs
Lipinski’s rule of 5: logP
<5
Lipinski’s rule of 5: ionised or unionised?
unionised
What is the excipient function of edetate disodium?
Metal chelator/preservative enhancer
What is the excipient function of chlorobutanol?
Preservative
What is the excipient function of ethanol?
Solvent
What is the excipient function of glycerin/glycerol?
Solvent/tonicity adjustment
What is the excipient function of glycine?
Solvent/tonicity adjustment
What is the excipient function of PEG?
Solvent
What is the excipient function of PG?
Solvent
What is the excipient function of saccharin sodium?
Sweetener
What is the excipient function of lecithin?
Surfactant
What is the excipient function of polysorbate 20&80?
Surfactant
What is the excipient function of tyloxapol?
Surfactant
What is the excipient function of Na CMC?
Viscosity adjustment
What is the excipient function of benzyl alcohol?
Preservative
Containers should not have _________.
Chemical or physical interactions with drug and excipient
Containers should ___________.
Protect formulation from contamination and degradation
Requirements of nasal spray delivery device
- Stability with formulated product
- User friendly design for patient compliance
- Reliability in use
Considerations for device design (6)
- Droplet size distribution
- Viscosity
- Spray pattern
- Plume geometry
- Dose volume
- Velocity
Advantages of powder
- Blowing through mouth avoids negative pressure and traps powder in nasal cavity
- Less loss of drug
Disadvantage of powder
- May cause irritation
How are in situ gels activated?
By stimulus such as change in
- pH
- temperature
- salt concentrations
