Pulmonary Delivery Flashcards
What are three characteristics of the lungs that make them good for drug delivery?
-Extensive surface area (100m2) and thin (0.1-0.3um)
-300 million alveoli which are vascularised for gas exchange
-Gives access to all parts of the body, including the brain
Why use the pulmonary route?
Potential for protein and peptide based drugs not suitable for oral route
Alternative to injectables
Expansion in non-respiratory markets (CF)
What are aerosol made of?
Dispersions/suspensions of solid material and or liquid droplets in gaseous medium
How are aerosol particles deposited in the lungs?
-gravitational sedimentation- large particles
-Inertial impaction- large particles
-Diffusion- small particles
In what way can we develop aerosols?
-provide consistent delivery
-High lung penetration
-Multiple dosing options
In the future, what changes would we make to aerosols?
-minimise device size
-Maximise patient convenience
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What was Exubra?
First inhalable insulin (2006)
Why was exubra discontinued?
-Field to gain patient and clinician acceptance
-Cost 3 1/2 times of injectable insulin
What is Affreza?
Inhaled insulin technosphere particles
When is Afrezza used?
-in 18 years old and over
-For type one and two diabetes
-Alongside a long acting insulin
What material are technoparticles made from?
FDKP micro crystal cards- large surface area for drug loading
-White solid which is highly water soluble at neutral and basic pH (due to COOH)
How is insulin loaded into technosphere particles?
-in monomer form
-It is precipitated from solution onto the surface
-has a positive charge whereas FKDP has a negative charge- promotes insulin absorption
What size of particles are used in afrezza?
2.5 µm-deep lung penetration
What inhaler is used for afrezza?
Medtone- dry powder inhaler with single use cartridges. Breath Activated
What are the differences between exubra and afrezza?
-exubra in hexomeric form: afrezza in monomeric (faster acting, no dissociation,mimics natural insulin)
-smaller device (medtone)- convenient
-exubra need manual activation: afrezza breath activated