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Biopharmaceutics > Pulmonary Drug Delivery > Flashcards

Pulmonary Drug Delivery Flashcards

1
Q

What are the 2 possible propellants that are in aerosols?

A
  • liquified gas

- compressed gas

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2
Q

What are the advantages of using pulmonary dose forms?

A
  • parenteral alternatives
  • fast onset of action
  • direct systemic absorption
  • noninvasiveness
  • low dose
  • minimal side effects
  • tamper proof
  • good stability
  • accurate doses
  • minimal potential for contamination
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3
Q

What are the disadvantages of pulmonary dose forms?

A
  • local action
  • administration techniques
  • patient compliance
  • limited applications
  • alternatives
  • special drug properties
  • unique production
  • explosive and flammable
  • environmental hazards
  • high unit costs
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4
Q

What are the basic requirements of a pulmonary dose forms?

A
  • non or low irritability
  • reasonable solubility
  • low therapeutic activity
  • physical/chemical compatibly
  • satisfactory permeability
  • pH range: 5.5-7.5
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5
Q

What are the medical conditions that are easily treated by inhalation devices?

A
  • asthma
  • allergy
  • inflammation
  • COPD
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6
Q

What are the properties that CFC propellants need to have to get into the lungs?

A
  • low toxicity
  • nonflammability
  • inertness
  • good boiling point
  • heavy density
  • for MDIs only
  • they are being phased out
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7
Q

What is the purpose of putting a coating inside of a glass of metal container?

A
  • prevents the leaching of the metals on the inside of the containers
  • can also coat glass on the outside- can stop the glass from breaking when the bottle is dropped
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8
Q

What is the quality control measures that need to be taken into account for pulmonary medications?

A
  • drug content
  • delivery rate and amount
  • dose uniformity
  • particle size
  • total discharge numbers
  • pressure testing
  • water content
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9
Q

What do the nomenclature names on a propellant mean? (example 114)

A

1st digit: one less than the number of carbons
2st digit: one more than the number of hydrogen atoms
3rd digit: number of fluorine atoms

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10
Q

What is the most common problem with a suspension aerosol?

A
  • suspensions may clump at the bottom- there is a challenge with the suspension
  • caking can happen in the presence of moisture, usually suspension aerosols will cake
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11
Q

What is the definition of an emulsion?

A
  • mixture of 2 immiscible liquids- milk and salad dressings are emulsions
  • need to add a surfactant to make the 2 parts come together
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12
Q

What is the particle delivery mechanism with a propellant?

A
  • actuation
  • spraying of large droplets moving at high velocity
  • evaporation of particles
  • formation of small, slow moving, individual particles, aggregates, or partially evaporated droplets
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13
Q

What is the particle delivery mechanism without a propellant?

A
  • carrier/drug static powder bed
  • carrier/drug dilated powder
  • carrier/drug on aerosol
  • carrier and stripped drug aerosol dispersion
    (drug is electrostatically bound to the carrier)
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14
Q

CFC was changed to HFA- why is this?

A
  • CFC has seen to be instrumental in depleting the ozone layer
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15
Q

How do you use an MDI?

A
  • shake the inhaler
  • breathe out
  • press the canister, inhale deeply and then slowly
  • hold breath for 10 seconds, then exhale
  • wait 30 seconds before the next dose
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16
Q

How do you use other inhalers other than an MDI?

A
  • load the drug
  • release the drug contents
  • breathe out
  • breathe in deeply
  • hold breath for 10 seconds, then exhale
  • get next dose ready
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17
Q

What is the definition of aerosols?

A
  • aerosols are products that depend on the power of a compressed or liquefied gas to expel the contents from the container
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18
Q

What are the unique advantages of aerosols?

A
  1. Drugs generally administered parenterally may be given by inhalation
    - does not need elaborate manufacturing processes
  2. Pulmonary drug delivery is able to produce a rapid onset of action, avoid drug degradation in the GI tract and circumvent 1st pass effects
  3. The use of an MDI can deliver drug doses accurately and efficiently. Lower doses are generally given through inhalation
  4. There is no danger of foreign contamination from outside environment due to complete closure of the containers. Aerosol preps are essentially tamper proof
  5. Sprays and foams can reduce drug irritation and expand drug contact to the application sites. Aerosols are also generally considered to be more efficient
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19
Q

What are some of the drug characteristics necessary for aerosol development?

A
  1. no irritation to drug absorption
  2. be reasonably soluble in respiratory fluid
  3. Be therapeutically effective at a relatively low dose
  4. Exhibit passive drug transport mechanism through respiratory membranes
  5. Be stable and compatible with propellants and have a pH between 5.5 and 7.5
20
Q

What is ventolin?

A

beta 2 adrenergic stimulant

- for the symptomatic relief and prevention of bronchospasm due to bronchial asthma

21
Q

What is flovent?

A
  • corticosteroid

- for prophylactic management of steroid responsive bronchial asthma in adults and children over 4 years old

22
Q

What is Oxeze turbuhaler?

A
    • bronchodilator, suspension aerosol

- for long term, 2x daily administration in the maintenance treatment of asthma in patients 12 and up

23
Q

What is advair used for?

A
  • bronchodilator- corticosteroid for inhalation, for regular treatment of reversible obstructive airways disease, including asthma in patients 12 years and olders
24
Q

What is vaponefrin used for?

A
  • bronchodilator, inhalation solution, for the symptomatic relief of bronchial obstruction due to bronchial spasm and mucous secretions associated with bronchial asthma, hay fever, chronic bronchitis, etc
25
Q

Under pathological conditions where the epithelium can be damaged, there could exist ____________ present in the airways

A

enhances penetration of substances

26
Q

What is the rate of absorption of a compound in the alveolus compared to the central airway?

A
  • the rate of absorption of a compound is approximately 2 times faster in the alveolus than the central airways (there is greater permeability in the alveolus than in the trachea)
27
Q

What are the 2 components of the cardiovascular system?

A
  • the pulmonary circulation

- the systemic circulation

28
Q

What is the route of the pulmonary circulation?

A
  • carried deoxygenated blood from the right ventricle to the lungs and returns blood from the lungs to the atrium
29
Q

What is the rate of the systemic circulation?

A
  • carries oxygenated blood from the left ventricle to the tissues of the bodying returns deoxygenated blood from the body to the right atrium
30
Q

Drugs absorbed from the lungs are normally carried directly to the ______, resulting in a fast onset of action

A
  • systemic circulation
31
Q

What is the most important factor in influencing drug absorption and bioavailability in the lungs?

A
  • drug deposition
32
Q

About 80-95% of the inhaled dose form typically ends up where?

A
  • in the GI tract
33
Q

Selection of an appropriate aerosol with a uniform small particle size may permit what?

A
  • may permit drug deposition to the central or peripheral airways, benefiting drug targets for local or systemic circulation
34
Q

What is another major factors that influences drug deposition in the airways?

A
  • rate and depth of breathing (rapid inspiration promotes central deposition, where deep inspiration leads to the peripheral airway deposition)
35
Q

What is the effect of holding breath at the end of an inspiration?

A
  • facilitates drug deposition through sedimentation and difficusion
36
Q

What determines the residence time of the drug in the lungs?

A
  • the rate and volume of ventilation
37
Q

What is the positive effects of using a spacer?

A
  • can slow down aerosol cloud, evaporate volatile components, and improve pulmonary drug delivery
38
Q

What are the changes that can be made to the drug particles that can have positive effects in the lungs?

A
  • reducing particle size and size distribution
  • increasing drug density
  • controlling hygroscopic growth of particles
39
Q

What are the 3 functional components that can be used to deliver the drug content?

A
  • propellants
  • valves or actuator
  • containers
40
Q

What is the definition of a propellant?

A
  • liquified gas with a vapour pressure greater than atmospheric pressure at a temperature of 40 degrees
41
Q

What are the most common oral and nasal propellants that are used?

A
  • dichlorodifluoromethane
  • trichloromonofluoromethane
  • dichlorotetrafluoroethane
42
Q

What are the hydrocarbons that are used for topical aerosols?

A
  • butane, isobutene, pentane
43
Q

What has been used now as a replacement for CFC?

A
  • hydrocarbons
44
Q

What is the most commonly used compressed gas that is used as an aerosol propellant?

A
  • nitrogen
45
Q

What is the best container type to use for an aerosol solution?

A
  • plastic coated glass bottles

Biopharmaceutics (6 decks)

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