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OU Pharmaceutics > Exam 3 Spring 2017 > Flashcards

Exam 3 Spring 2017 Flashcards

1
Q

What are the sizes of particles that get stuck in to nasopharyngeal region?

A

10-30 microm

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2
Q

What are the sizes of particles that get stuck in to bronchiolar region?

A

5-10 microm

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3
Q

What are the sizes of particles that get stuck in to alveolar region?

A

1-5 microm

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4
Q

What are local advantages of nasal drug delivery?

A
  • Ease of administration
  • Rapid absorption and onset of action
  • Reduction in systemic side effects
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5
Q

What are systemic advantages of nasal drug delivery?

A
  • Rich vasculature underlining the nasal mucosa
  • does not undergo first pass metabolism
  • Rate and extent of absorption similar to IV (for some drugs)
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6
Q

Disadvantages of nasal delivery

A
  • Small site for absorption
  • Mucociliary clearance
  • Potentially short residence time
  • Efficiency of delivery is important
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7
Q

What does formulation enhancers do to the drug?

A
  • increase absorption

- increase time spent in cavity via mucoadhesives

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8
Q

What happens with chronic use of formulation enhancers for nasal routes?

A

nasal irritation

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9
Q

What are the types of dosage forms for nasal delivery?

A
  • solution: drops, spray pump
  • suspension sprays
  • gels
  • emulsions and ointments
  • DPI
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10
Q

Factors that affect drug absorption

A
  • size of drug molecule
  • partition coefficient (lipid solubility)
  • drug concentration
  • ionization state of drug
  • pH of absorption site
  • vehicle for drug delivery
  • mucosal contact time
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11
Q

What are the types of solubilizers or co-solvents for nasal dosage form?

A

– Alcohol, 200 proof (2%)

– Propylene glycol (20%)

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12
Q

What are surfactants used for in nasal dosage form?

A

to reduce surface tension for drug to penetrate membrane

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13
Q

What are tonicity agents used for in nasal dosage form?

A

so that tonicity in the nasal membrane is isotonic so it doesn’t get damaged

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14
Q

What is a popular bioadhesive?

A

chitosan

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15
Q

What are types of local action which nasal formulations can target?

A
  • rhinitis
  • nasal pruritus
  • sinusitis
  • runny nose (rhinorrhea)
  • prevent polyps
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16
Q

What are types of systemic advantages which nasal formulations can achieve?

A
  • convenient
  • more efficient dose/effect (propanolol)
  • avoid first pass metabolism
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17
Q

What are the effects of nasal route to the brain?

A
  • bypasses BBB
  • delivered via neural pathways
  • minimize systemic exposure
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18
Q

Describe the size requirements for delivery to brain from nasal route.

A

make sure the droplet sizes are on the lower side (10 micron) so that it’s more sensitive to the upper concha to go to the brain

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19
Q

Define aerosol

A

dispersion of particles or droplets suspended in a gas or vapor

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20
Q

What are advantages of local delivery with respect to pulmonary route?

A
  • can treat asthma, COPD
  • rapid onset
  • no interactions with food
  • more acceptable then injections
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21
Q

What are advantages of systemic delivery with respect to pulmonary route?

A
  • avoids first pass metabolism

- large surface area: (120 – 160 m2, ~ tennis court)

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22
Q

What are limitations of pulmonary route?

A
  • lungs designed to prevent inhalation of exogenous compounds / particulates
  • oropharyngeal irritation, taste
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23
Q

Define aerodynamic diameter

A

“How well the droplet or particle can fly in a stream of air”

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24
Q

What are the types of aerosol deposition?

A
  • for >5 microm: electrostatic attraction, interception, impaction
  • for <5 microm: gravitational settling (sedimentation), brownian diffusion
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25
Q

What is the purpose of holding your breath when inhaling an aerosol?

A
  • no air exchange to decrease air velocity going down
  • droplets fall down deeper
  • enhancing sedimentation of aerosol
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26
Q

What is the preferred value of Geometric Standard Deviation (GSD) for particle size for inhalation? And what does this mean?

A

2; means that 95.5% of particles are at the site of action

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27
Q

How do you measure diameter of particles?

A
  • individual free particle
  • aggregation will act like a larger particle
  • droplets which have free particles, particles will assume their free diameter inside the droplet
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28
Q

What is the important of density influencing deposition?

A

if a particle is larger in diameter but less in density, it can still act as if it is a small particle

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29
Q

What can hygroscopic particles do?

A

can absorb humidity in resp. tract and assume a larger diameter than intended

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30
Q

What are two conditions (that we talked about in class) that can be treated by nebulization?

A
  • cystic fibrosis

- emphysema

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31
Q

What are types of nebulizers?

A
  • air jet (makes up majority)

- ultrasonic

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32
Q

What are advantages of nebulizers?

A
  • Aqueous solutions: no environmental concerns

- Does not depend on patient inspiratory force

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33
Q

What are disadvantages of nebulizers?

A
  • Bulky / Not portable
  • Equipment is not cheap
  • Device designed independent of drugs; can lead to waste
  • Contamination of device
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34
Q

With respect to nebulizers, what does droplet size depend on?

A
  • volume of solution
  • surface tension
  • density and viscosity
  • nebulizer equipment
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35
Q

Describe the events that take place in an ultrasonic nebulizer

A
  • Energy generated to piezoelectric transducer
  • Shakes to coupling fluid which goes to drug solution
  • Droplets are formed
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36
Q

Advantages of ultrasonic nebulizer

A

can created smaller particles

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37
Q

Disadvantages of ultrasonic nebulizer

A
  • complex apparatus
  • cannot be used by particles degraded by heat
  • not easily cleaned
38
Q

Characteristics of solutions used for inhalation

A
  • pH close to neutral
  • iso-osmotic
  • isotonic (if not, can cause vasoconstr.)
39
Q

What is an example of advancements in nebulizers?

A
  • AKITA JET used in Germany to treat CF

- tracks doses taken and doses missed

40
Q

What are classes of drugs that can be used to treat asthma?

A

– Beta2-adrenergic agonists
– Glucocorticoids
– Mast cell stabilizer

41
Q

Define MDI

A

Devices that contain a pressurized formulation that is aerosolized through an atomization nozzle; doses are metered

42
Q

Advantages of MDI

A
  • portable
  • easy to use and convenient
  • drug is protected from light, O2, and water
  • tamper proof
43
Q

Disdvantages of MDI

A
  • enpensive
  • prone to incorrect use
  • pressurized contents
44
Q

Specific to MDI, particle size released from MDI depends on what?

A
  • formulation
  • valve design
  • actuator
  • propellant
45
Q

What are the uses for propellants in MDI’s?

A

– Provide pressure to expel product
– Also act as dispersion medium
– Occasionally exhibit solvent properties

46
Q

What are the uses for solvents in MDI’s?

A

– Bring active ingredient into solution
– Co-solvent for immiscible liquids
– influence particle size
– reduce vapor pressure

47
Q

What is the Montreal Protocol?

A
  • CFC [Chlorofluorocarbons] were killing the ozone layer; mandate to stop using it
  • HFA [Hydrofluoroalkanes] used in its place and transition all to HFA by 2005
48
Q

What effect does vapor pressure have on formulation performance in MDI’s?

A
  • particle size
  • droplet evaporation
  • velocity
49
Q

Advantages of DPI

A
  • does not require coordination with actuation (but do breathe in with full force)
  • don’t have to worry about solubility
  • less likely that microbe will grow in powder
  • can deliver higher doses
  • tamper proof
50
Q

Disadvantages of DPI

A
  • breathe in with full force (not recommended for children or elderly)
  • strength of pt’s airflow determines dose administered
  • active DPI may be expensive
51
Q

Sedimentation that occurs between bronchiolar and alveolar region has to be what size?

A

3-5 microm

52
Q

Diffusion occurs where and what size does it have to be?

A

alveolar region at <1 microm

53
Q

Define complexation

A

interaction between two or more compounds to form a complex

54
Q

What is the center of a complex called?

A
  • central atom / ion
  • substrate
  • acceptor atom
55
Q

What is the name of the molecules attached to the central atom?

A

ligand

56
Q

What is a coordination number of a complex?

A

it denotes the number of attachments to the central atom

57
Q

What are pharmaceutical relevance to complexation?

A
  • increased solubility
  • increased drug stability
  • aids in drug delivery system
  • increase excretion of compound in urine
58
Q

What are disadvantages to complexation?

A
  • modify pharmacologic activity of drug

- decreased solubility

59
Q

Classes of antacids

A
  • neutralize acids
  • H2 antagonist (block secretion of acids from parietal cells)
  • proton pump inhibitor
60
Q

Which drugs can antacids cannot be used with? (specific examples discussed in class)

A
  • digoxin
  • phenytoin
  • chlorpromazine
61
Q

Characteristics of transition metals

A
  • open d orbital
  • usually more than one oxidation state
  • show characteristic colors
62
Q

T/F; Metal ion complexes must always have a metal as the central atom.

A

False; it usually is metal but doesn’t have to be

63
Q

Define capacity of binding

A

number of ligand binding sites in the protein molecule

64
Q

What are properties that might change after formation of a complex?

A
  • solubility
  • stability
  • partitioning
  • energy absorption
  • emission
  • conductance of complex
65
Q

Characteristics of inorganic complex

A

coordinate covalent link between ligand and central atom

66
Q

Characteristics of chelated complex

A
  • one or more ligand combine with central atom to form many bonds
  • ligands are polydentated
67
Q

Examples of inorganic complexes

A

silver-ammonia complex, [Ag(NH3)2]+

68
Q

Examples of chelates

A

Chlorophyll, hemoglobin, myoglobin and cytochrome c

69
Q

Characteristics of organic molecular complex

A
  • substrate-ligand held together by weak forces

- small + small or small + large molecules

70
Q

Examples of organic molecular complexes

A

theophylline to form aminophylline; polymer complex

71
Q

Examples of polymer complexes

A

PEG, polystyrene, carboxymethylcellulose

72
Q

Characteristics of cyclodextrin complex

A
  • donut-shaped cyclic structure of glucose moeities
73
Q

What is the diameter of the cyclodextrin cavity?

A

5 to 8 Å

74
Q

Characteristics of channel lattices

A
  • crystals of deoxycholic acid (DCA) are arranged to form a channel
  • camphor and terpinol bind within the lattice structure of DCA to produce an inclusion complex
75
Q

What can channel lattices form complexes with?

A
  • paraffins
  • organic acids
  • aromatic compounds
76
Q

Examples of layer type complex

A

bentonite can trap hydrocarbons and glycols between the layers of their lattices

77
Q

Characteristics of clathrates

A

cage like lattic

78
Q

Examples of clathrates

A

warfarin sodium USP, is a clathrate of water, isopropyl alcohol, and sodium warfarin in the form of crystalline powder

79
Q

Characteristics of albumin

A
  • most important plasma protein
  • MW of ~65 KDa
  • bind to acidic (anionic) drugs
  • synthesized in liver
80
Q

What are the causes of hypoalbuminemia?

A
  • cirrhosis of the liver
  • viral hepatitis
  • renal failure
  • surgery
  • burns
81
Q

What are the causes of hyperalbuminemia?

A
  • dehydration

- certain neurological disorders

82
Q

What can affect the affinity of a drug towards albumin, AAG, and lipoprotein?

A
  • presence of another drug

- disease condition

83
Q

Characteristics of AAG

A
  • α1 -Acid Glycoprotein
  • lower concentration than albumin
  • MW of ~44 KDa
  • binds to basic (cationic) and neutral drugs
  • synthesized in liver
84
Q

Examples of acidic (anionic) drugs

A
  • phenytoin
  • tolbutamide
  • warfarin
  • naproxane
  • ibuprofen
85
Q

Examples of basic (cationic) drugs

A
  • propranolol
  • imipramine
  • lidocaine
86
Q

Characteristics of lipoproteins

A
  • less than 0.5% concentration
  • bind to basic and neutral drugs
  • synthesized in liver AND intestinal mucosa
87
Q

What are solubilizers used for in nasal products?

A

to increase the concentrations of drugs that have poor aqueous solubility

88
Q

What are humectants used for in nasal products?

A

to avoid dryness of nasal cavity while using medication

89
Q

What are five symptoms / diseases that nasal formulations can be used for?

A
  • seasonal allergies
  • pain
  • migraine
  • smoking cessation aids
  • influenza vaccine
90
Q

What are the major components of an MDI?

A
  • canister
  • valve
  • actuator

OU Pharmaceutics (9 decks)

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