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Medicine Pharmaceutics > Inhalation drug delivery > Flashcards

Inhalation drug delivery Flashcards

1
Q

benefits of inhaled medication

A 
rapid 
avoids GIT 
avoids first pass
lower doses needed
accurate dose measurement 
small volumes 
tamperproof- child safety 
protection
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2
Q

inhaled drug delivery provides and alternate route of administration for:

A

For acute and breakthrough pain treatment
Where physical and/or chemical interactions with other medications must be avoided
When the drug exhibits variable or erratic pharmacokinetics when given orally
When critical to avoid gi degradation of the therapeutic agent, e.g., biologics, insulin

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3
Q

components of the upper respiratory tract?

A 
buccal 
sublingual 
nasal 
pharynx
upper larynx
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4
Q

point of the nasal cavity?

A

moisten and warm air

filter out large particles >15mm

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5
Q

nasal cavity filters particles..

A

> 15mm

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6
Q

epiglottis role?

A

covers entrance to airways when swallowing

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7
Q

components of the lower respiratory tract?

A

trachea
bronchi
bronchioles
alveoli

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8
Q

how big are alveoli?

A

<1mm

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9
Q

how many alveoli in the lungs?

A

30 million per lung

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10
Q

surface area of alveoli?

A

70m2

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11
Q

where can particles deposit in the respiratory tract?

A

anywhere

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12
Q

extent and loci of particle disposition is controlled by?

A

product characteristics
dry powder
liquid aerosol

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13
Q

what affects the extent and loci of particle distribution in dry powder inhalers?

A 
particle diameter 
shape 
density 
charge 
surface chemistry
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14
Q

what affects the extent and loci of particle distribution in liquid aerosols?

A

droplet size
velocity
nature of propellant

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15
Q

anatomical and physiological characteristics that affectextent and loci of particle distribution molecules?

A

lung capacity
breathing patterns
geometry of respiratory tract

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16
Q

there’s _____ disposition in the peripheral regions of the lungs

A

less

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17
Q

why could you see some drug in the stomach with inhaled drugs?

A

some deposited in mouth which will be swallowed

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18
Q

explain inertial impaction?

A

momentum of particle renders it unable to follow the airflow in a curved airway so that it impacts on the wall-travels too fast so just hit the walls. Significant forward momentum.

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19
Q

explain gravitational sedimentation?

A

related to the residence time in an airway & terminal settling velocity, increased by holding breath. In the time between inhalation and exhalation.

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20
Q

explain brownian diffusion?

A

random collision of particle with airway wall; significant only for particles < 0.1 mm- smaller they are, the more likely they are to be deposited

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21
Q

brownian diffusion is only significant for particles _____

A

<0.1

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22
Q

for brownian diffusion, the smaller they are the …..

A

more likely they are to be deposited

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23
Q

explain electrostatic attraction

A

charge on particle induces opposite charge on airway wall and accelerates particle into wall by attraction. Need to be travelling travelling quite slowly and close to the wall. By the time this happens, usually one of the other has happened

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24
Q

what are the circumstances for electrostatic attraction?

A

needs to be travelling quicte slowly

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25
Q

why is electrostatic attraction rarer than the others

A

as its slow so by the time it could happen, one of the other dispositions have occurred

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26
Q

explain interception

A

particle size approaches airway diameter. Only for very asymmetric and needle like particles. Can be tangled up like straw and get trapped

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27
Q

what disposition is most likely to happen to particles of an asymmetric and needle like structure?

A

interception

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28
Q

disposition by impaction and sedimentation are directly proportional to?

A

particle size

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29
Q

disposition by impaction and sedimentation are most significant for particles > than

A

1mm

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30
Q

in disposition by impact and sedimentation, the bigger the particle the….

A

more likely it will impact as it will be going quicker (impaction) and will sediment faster (gravitational)

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31
Q

desposition by infusion is ______ proportional to particle size. this means?

A

inversely

the smaller the size, the more diffusion

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32
Q

in traditional delivery devices, desposition is achieved primarily through which 2 methods?

A

impaction

sedimentation

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33
Q

for particles <10mm ____% of dose is not deposited. meaning?

A

80-90%

breathed out or swallowed

34
Q

how can you improve disposition of inhalers with small molecules?

A

emit at lower velocities

35
Q

emitting small particles at lower velocities achieves >___% disposition in the airways

A

30

36
Q

what inhalation devices are good for the upper respiratory tract?

A

sprays

37
Q

prssurised metered dose inhales use ______ based propellants

A

solvent- no longer cfcs

38
Q

superfine particle inhalers are used for….

what do they produce

A

small airway disease

produce very small aerosol particles

39
Q

what do superfine particle inhalers use as a propellant

A

hfas

40
Q

explain nebulisers

A

drug dispersed in polar solvent- usually water

41
Q

dry powder inhalers are replacing? why?

A

pressurised metered dose inhalers

no solvent propellant so no environmental issues

42
Q

dry powder inhaler mechanism of drug delivery?

A

dry powder fluidises when patient inhales

drug shears from larger particles and penetrates deeper into the lungs

43
Q

how does drug penetrate deeper into the lungs with dry powder inhalers?

A

drug shears from larger particles

44
Q

3 uses for nasal sprays?

A

hay fever
sinusitis- steroids
decongestents

45
Q

what do some sprays use now- more modern

A

metered dose pump

46
Q

how do metered dose sprays work- from pressing the actuator?

A

releases the drug

when it returns to normal position, more drug is drawn up to replenish the supplies

47
Q

vianase uses ______ technology. how does it give controlled particle dispersion

A

kurve
uses electronic atomiser to give controlled particle dispersion (with narrow size range: 10 – 30 mm); minimises pulmonary and gi deposition

48
Q

what is vianase size range?

A

10-30mm

49
Q

options uses _____ flow.

A

bidirectional flow

50
Q

how does optinose work?

A

exploiting the blow reflex
to ensure large particles go to the nasal mucosa and prevent smaller particles going down into the lungs
blow into the mouth piece, the soft pallet closes which shuts the nasal cavity off to the airway

51
Q

pMDI’s use a _____ propellent

A

liquid

52
Q

what type of thing do pMDIs create?

A

fast moving micro-fine suspensions

53
Q

how do the valves operate in pMDIs?

A

simultaneously to inhalation

manually operated or breath actuated

54
Q

excipients in pMDIs?

A

: co-solvent (ethanol), inverse micelles, or liposomes to enhance solubility of surfactant propellants; surfactants (e.g., lecithin, oleic acid),
to adsorb to particles & prevent agglomeration (shake before use); menthol, flavouring; ascorbic acid, antioxidant; phenylethanol, preservative

55
Q

patient advice with pMDIs?

A

shake before use

56
Q

why are small airway diseases inadequately treated using traditional inhalers?

A

as the airways are smaller

airflow limitation

57
Q

most particles generated in traditional pMDIs and DPIs deposit in …

A

the upper airways by sedimentation and impaction

58
Q

small particle aerosols can be used to treat?

A

COPD

asthma

59
Q

small particle aerosols can decrease the dose of?

A

corticosteroids needed

60
Q

nebulisers only delivery ___% of nebuliser drug

A

13

61
Q

how do traditional (air jet) nebulisers work?

A

compressed air or oxygen exits a narrow orifice at high velocity, creating negative pressure which draws liquid to top of tube, where it is aerosolised, giving droplets > 40 mm; very large droplets removed through impaction on bends in the equipment

62
Q

what sized particles are produced by traditional air jet nebulisers

A

> 40mm

very large

63
Q

issue with the equipment of traditional air jet nebulisers?

A

40mm very large droplets

removed by impaction on beds of the equipment

64
Q

how do ultrasonic nebulisers work?

A

piezoelectric transducers used to focus (1- 3 mhz) ultrasound waves in liquid, with intense agitation at the focus to disperse the liquid and form aerosol

65
Q

how do vibrating mesh ultrasonic nebulisers work?

A

alternating current causes piezo crystal to expand and contract rapidly, pulling mesh into liquid and then thrusting forward to create a monodisperse aerosol of superfine droplets (virtually all of which is appropriate for inhalation) these are much smaller and better for use

66
Q

DPIs are _____ ______ _______ devices

A

passive breath dispersing

67
Q

what type of inhalation is needed with DPIs?

A

quick
strong
deep

68
Q

how are the drug particles delivered in DPIs?

A

small drug particles adhered to larger carrier particles – separated by sheer with large particles then being deposited in the oropharynx, and the smaller (drug) particles going down to the lower airways

69
Q

how would active DPIs work?
examples?
- not commercial use yet

A

use an internal power source to aerosolize the powder; spirostm, uses a battery-powered motor, oriel, uses a piezoelectric polymer

70
Q

carriers in DPI?

A

lactose or drug crystals

71
Q

examples where drug crystals are used in DPI?

A

pulmicort (budenoside)

turbuhaler (az)

72
Q

how are DPIs micronised?

A

by jet, pin or ball milling
or
spray drying or use of supercritical fluid

73
Q

drug particles still attached to carrier in DPIs will be deposited?
smaller drug particles?

A

in the oropharyngeal area

into the lungs

74
Q

efficient alveolar delivery of particles with aerodynamic diameters of?

A

1-5mm

75
Q

what does aerodynamic diameter describe?

A

the dynamic behaviour of a particle relating to gravitational settling and inertial impaction

76
Q

aerodynamic diameter determines what?

A

where the particles deposit

77
Q

aerodynamic diameter can be increased by?

A

decreasing size
decreasing density
increasing shape factor

78
Q

TF: a more assymetric/ needle like particle is more aerodynamic

A

true

79
Q

if X>1 the aerodynamic diameter is?

A

less

elongated

80
Q

if X=1 then what are the particles like?

A

more spiracle

81
Q

if density is less then the D(ae) becomes ____

A

lower

82
Q

aerodynamic diameter equation?

A

D(ae)= D(eq) (square root of:)Pp/ PpX

D(ae)= Aerodynamic diameter 
D(eq)= GEOMETRIC SIZE
P(p)= density 
X= shape factor

Medicine Pharmaceutics (6 decks)

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