Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

OU Pharmaceutics > Final > Flashcards

Final Flashcards

1
Q

What are the different types of capsules?

A
  • Gelatin
  • Methyl cellulose (HPMC) [best to use in DPI]
  • Calcium alginate
  • DRcaps™ Gastro Resistant Capsules
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the steps for gelatin manufacturing?

A
  • Derived from skin or bone
  • Acid or alkali treatment
  • Extended treatment periods
  • Filter
  • Vacuum concentration
  • Cool to solidify
  • Air dry
  • Mill to size
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

How can capsules be closed?

A
  • welded with heated metal pin
  • bonded with molten gelatin
  • snap fit
  • coni-snap
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Properties of soft gelatin capsules

A
  • Shells of gelatin, glycerin or sorbitol added to induce plasticity
  • Oblong, elliptical or spherical shape
  • Used to encapsulate liquids, suspensions, pastes or dry powders
  • Must be prepared filled and sealed in one continuous operation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the ways in which you can manufacture soft gelatin capsules?

A
  • plate process

- die process

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What does the die process consists of?

A
  • a process which to manufacture soft gelatin capsules
  • rotary process
  • reciprocating process
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is the plate process?

A
  • a process which to manufacture soft gelatin capsules

- molds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What types of formula is suitable for soft gelatin capsules?

A
  • Water immiscible, volatile and nonvolatile liquids
  • Oily, non-volatile liquids
  • Not suitable for low molecular weight compounds that can easily pass through the capsule
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the different types of coating for coated tablets?

A
  • Sugar
  • Film (make tablet more sturdy)
  • Gelatin
  • Enteric
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the types of specialized tablets?

A
  • chewable
  • effervescent
  • CR, ER
  • sublingual
  • buccal
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the essential ingredients for tablets?

A
  • diluent
  • binder
  • lubricant
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Why would any ingredient be essential to tablets?

A

give the formula specific characteristics needed to be compressed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the ingredients to give tablets desirable characteristics?

A
  • disintegrant
  • color
  • flavor
  • sweetening agent
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the purpose of a glidant?

A
  • needed for formulations with poor flow
  • not needed if lubricant is enough for flow
  • improves flow characteristics of powder mixture
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Define diluent

A

inert substance added to increase bulk to make a tablet of practical size for compression, or to adjust its size

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are examples of diluent?

A
  • lactose
  • calcium phosphate
  • microcrystalline cellulose (Avicel®)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

There needs to be a compatibility test between diluent and active ingredient. Give an example of an incompatibility.

A

Calcium salts interfering with absorption of tetracycline in the GI tract

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

How can a diluent affect bioavailability?

A

water soluble diluents can increase bioavailability of drugs that have low solubility; can enhance dissolution

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Define binder

A

glues ingredients together and helps with compression; improves powder flow-ability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What are examples of binders?

A
  • starch (10-20% paste)
  • gelatin (10-20% solution)
  • acacia
  • CMC
  • PVP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is the purpose of a lubricant?

A

generally hydrophobic; to prevent adhesion of the powder formulation to the surfaces of the dice and punches of tableting machine; improves rate of flow of granulate; should be added after granulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are examples of lubricant?

A
  • talc (1-5%)

- magnesium stearate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Why does talc undergo testing?

A

it may contain metals

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What happens if you add too much lubricant?

A
  • your tablet may become waterproof and it will affect wetting of the tablet
  • lead to poor tablet disintegration
  • poor dissolution
  • decreased solubility
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Give an example where talc needs to be purified.

A

if talc is not pure enough, it may have a high Ca concentration and will act as a decomposing agent towards ASA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What is an example of a glidant?

A

talc

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Define disintegrant

A

substance or mixture of substances added to a tablet to facilitate its break-up or disintegration after oral ingestion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

What are examples of distinegrants?

A
  • starch

- celluloses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

How can you tell the difference between the roles that starch plays?

A
  • dilute/dissolve starch = binder
  • mixed with diluent = used as disintegrant
  • starch used as a binder usually has a lesser proportion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Why doesn’t effervescent tablets need disintegrants?

A

because the sodium bicarbonate, tartaric or citric acid effervescence will cause tablets to disintegrate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Which are the steps that we can add coloring agents and why?

A
  • wet granulation: dissolved in binding solution prior to granulation
  • dry granulation: blended in dry with other ingredients
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

What are examples of flavoring agents?

A
  • Cyclamates and saccharine (banned)

- Aspartame

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

What does it mean when you have talc and magnesium stearate in the same compound?

A

one will act as the glidant and one will act as the lubricant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

What are the purpose of tablet coating?

A
  • cover unpleasant taste, odor, color
  • physical and chemical protection
  • DR or EC
  • identification
  • ease process of blistering
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

What are the different kinds of coatings?

A
  • sugar coated
  • film coated
  • gelatin coated
  • enteric coated
  • compression coated
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

Purposes of sugar coating

A
  • protection from air and humidity

- improve taste and smell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What can be used to waterproof tablets?

A

Shellac

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

What is used to smooth tablets?

A

dibasic calcium phosphate, titanium oxide, starch

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Purposes of film coating

A
  • improve presentation
  • increase stability
  • improve taste
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

What are examples of plasticizers and how are they used in tablets?

A
  • used for film coating

- castor oil, diethyl phtalate, propylen glycol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

What are examples of enteric coating materials?

A
  • cellulose acetate phtalate
  • poly(methacrylic acid-co-methyl-methacrylate)
  • poly(vinyl acetate phtalate)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

What are some commercially available for use enteric coating solutions?

A
  • Aquateric®
  • Caoteric®
  • Eudragits™
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Explain how enteric coating tablets allow the API to be released in the intestine instead of the stomach.

A
  • At low pH, carboxyl groups remain protonated (not water soluble)
  • At high pH, carboxyl group is ionized (becomes water soluble)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

Describe ingredients in sublingual tablets

A

lactose or mannitol and saccharine is massed with 60% ethanol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

What are ingredients in buccal tablets?

A
  • lactose or mannitol
  • HPMC
  • silica gel
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

With respect to the film theory, what is a stagnant film?

A

a layer of solution which is saturated with the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

Define sink condition

A

one-third times that of the maximum solubility of the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

What are factors that influence dissolution from solid dosage forms?

A
  • dosage form
  • solubility
  • dissolution media
  • partition coefficient
  • diffusivity
  • diffusional path thickness
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

What are three interaction forces that occur in powder samples?

A
  • capillary forces
  • mechanical interlocking
  • electrostatic charges
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

What are the main reasons to granulate pharmaceutical powders?

A
  • make particle size more uniform
  • improve powder flow
  • improve compression characteristics of the drug
  • densify materials
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

What are examples of plasticizers and how are they used in soft gelatin capsules?

A
  • used to soften gelatin and make it more maleable

- sorbitol, glycerin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

What are the ways in which tablets can disintegrate?

A
  • wicking: disintegrant forms pored and water enters the pores which reduces the physical bonding forces between powder particles
  • swelling: disintegrant particles swell inside tablet breaking the tablet from the inside
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

What are the advantages of a film coating over sugar coating?

A
  • simpler process
  • less ingredients in coating solution
  • can provide thinner coats
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
54
Q

Causes of capping / lamination

A
  • insufficient binder
  • undermixing of tablets ingredients
  • fast speed of compression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
55
Q

Causes of sticking / picking

A
  • insufficient amount of lubricant

- improper application of coating or insufficient drying time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
56
Q

Causes of erosion / chipping

A
  • tablets are friable
  • fast pan rotation during coating
  • poor choice of plasticizer
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
57
Q

Causes of bridging

A
  • high viscosity of solid content in coating solution
  • improper atomization pressure
  • insufficient drying time
  • slow pan rotation during coating
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
58
Q

What are different types of media for dissolution?

A
  • water
  • solution with buffer
  • simulated gastric fluid (SGF)
  • simulated intestinal fluid (SIF)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
59
Q

What does SGF consists of?

A
  • 0.2% NaCl in 0.7% HCl

- pepsin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
60
Q

What does SIF consists of?

A
  • Phosphate buffer, pH=6.8

- pancreatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
61
Q

Apparatus 1

A
  • rotating basket
  • less than 4h dissolution test
  • standard volume 900-1000mL (also 1, 2, and 4L)
    used for
  • tablets coated, IR, DR, EC
  • capsules
  • beads
  • suppositories
  • floating dosage forms
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
62
Q

Apparatus 2

A
  • paddle
  • makes up about 80% of dissolution tests performed
  • less than 4h dissolution test
  • standard volume 900-1000mL
    used for
  • tablets coated, IR, DR, EC
  • capsules
  • beads
  • floating dosage form
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
63
Q

Apparatus 3

A
  • reciprocating cylinder
  • 4-12h dissolution test
  • standard volume 200-250mL
    used for
  • controlled release tablets & beads
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
64
Q

Apparatus 4

A
  • flow-through cell
  • designed for poorly soluble compounds
  • flow rate: 10-100mL/min
    used for
  • low solubility drugs
  • microparticles
  • implants
  • suppositories
  • controlled release formulations
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
65
Q

Advantages and disadvantages to Apparatus 4

A
  • Advantages: easy to change pH, pH profile, sink conditions maintained at all times, open and closed system, can be automated
  • Disadvantages: de-aeration necessary, high volumes of media needed
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
66
Q

Apparatus 5

A
  • paddle over disk
  • standard volume = 900m L
  • used for transdermal patches
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
67
Q

What should the time period be for an IR tablet to be dissolved?

A

15 - 60 minutes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
68
Q

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

A

10-30 microm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
69
Q

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

A

5-10 microm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
70
Q

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

A

1-5 microm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
71
Q

What are local advantages of nasal drug delivery?

A
  • Ease of administration
  • Rapid absorption and onset of action
  • Reduction in systemic side effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
72
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
73
Q

Disadvantages of nasal delivery

A
  • Small site for absorption
  • Mucociliary clearance
  • Potentially short residence time
  • Efficiency of delivery is important
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
74
Q

What does formulation enhancers do to the drug?

A
  • increase absorption

- increase time spent in cavity via mucoadhesives

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
75
Q

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

A

nasal irritation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
76
Q

What are the types of dosage forms for nasal delivery?

A
  • solution: drops, spray pump
  • suspension sprays
  • gels
  • emulsions and ointments
  • DPI
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
77
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
78
Q

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

A

– Alcohol, 200 proof (2%)

– Propylene glycol (20%)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
79
Q

What are surfactants used for in nasal dosage form?

A

to reduce surface tension for drug to penetrate membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
80
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
81
Q

What is a popular bioadhesive?

A

chitosan

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
82
Q

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

A
  • rhinitis
  • nasal pruritus
  • sinusitis
  • runny nose (rhinorrhea)
  • prevent polyps
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
83
Q

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

A
  • convenient
  • more efficient dose/effect (propanolol)
  • avoid first pass metabolism
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
84
Q

What are the effects of nasal route to the brain?

A
  • bypasses BBB
  • delivered via neural pathways
  • minimize systemic exposure
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
85
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
86
Q

Define aerosol

A

dispersion of particles or droplets suspended in a gas or vapor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
87
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
88
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
89
Q

What are limitations of pulmonary route?

A
  • lungs designed to prevent inhalation of exogenous compounds / particulates
  • oropharyngeal irritation, taste
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
90
Q

Define aerodynamic diameter

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
91
Q

What are the types of aerosol deposition?

A
  • for >5 microm: electrostatic attraction, interception, impaction
  • for <5 microm: gravitational settling (sedimentation), brownian diffusion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
92
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
93
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
94
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
95
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
96
Q

What can hygroscopic particles do?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
97
Q

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

A
  • cystic fibrosis

- emphysema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
98
Q

What are types of nebulizers?

A
  • air jet (makes up majority)

- ultrasonic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
99
Q

What are advantages of nebulizers?

A
  • Aqueous solutions: no environmental concerns

- Does not depend on patient inspiratory force

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
100
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
101
Q

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

A
  • volume of solution
  • surface tension
  • density and viscosity
  • nebulizer equipment
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
102
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
103
Q

Advantages of ultrasonic nebulizer

A

can created smaller particles

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
104
Q

Disadvantages of ultrasonic nebulizer

A
  • complex apparatus
  • cannot be used by particles degraded by heat
  • not easily cleaned
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
105
Q

Characteristics of solutions used for inhalation

A
  • pH close to neutral
  • iso-osmotic
  • isotonic (if not, can cause vasoconstr.)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
106
Q

What is an example of advancements in nebulizers?

A
  • AKITA JET used in Germany to treat CF

- tracks doses taken and doses missed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
107
Q

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

A

– Beta2-adrenergic agonists
– Glucocorticoids
– Mast cell stabilizer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
108
Q

Define MDI

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
109
Q

Advantages of MDI

A
  • portable
  • easy to use and convenient
  • drug is protected from light, O2, and water
  • tamper proof
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
110
Q

Disdvantages of MDI

A
  • enpensive
  • prone to incorrect use
  • pressurized contents
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
111
Q

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

A
  • formulation
  • valve design
  • actuator
  • propellant
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
112
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
113
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
114
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
115
Q

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

A
  • particle size
  • droplet evaporation
  • velocity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
116
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
117
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
118
Q

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

A

3-5 microm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
119
Q

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

A

alveolar region at <1 microm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
120
Q

What are the major components of an MDI?

A
  • canister
  • valve
  • actuator
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
121
Q

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

A
  • seasonal allergies
  • pain
  • migraine
  • smoking cessation aids
  • influenza vaccine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
122
Q

What are humectants used for in nasal products?

A

to avoid dryness of nasal cavity while using medication

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
123
Q

What are solubilizers used for in nasal products?

A

to increase the concentrations of drugs that have poor aqueous solubility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
124
Q

How do you apply semi-solid preparations?

A

topically

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
125
Q

What are examples of non-medicated semi-solid preparations?

A
  • emollient (moisturizer)

- skin protectant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
126
Q

What are the classifications of bases for semi-solids?

A
  • oleaginous
  • absorption
  • water removable
  • greaseless
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
127
Q

other names for oleaginous bases

A
  • hydrocarbon bases

- hydrophobic bases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
128
Q

oleaginous base properties

A
  • highest occlusion properties
  • most oily
  • difficult to wash off skin
  • difficult to incorporate aqueous agents
  • immiscible with water
  • used to protect skin and emollient effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
129
Q

examples of oleaginous bases

A
  • regular and white petrolatum

- yellow and white ointment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
130
Q

absorption base properties

A
  • able to absorb aqueous solutions to give w/o emulsion
  • used for emollient effects
  • difficult to wash off skin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
131
Q

examples of absorption bases

A
  • hydrophilic petrolatum

- lanolin (wool fat)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
132
Q

water removable base properties

A
  • also known as water washable

- external phase has to be water; o/w phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
133
Q

example of water removable bases

A

hydrophilic ointment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
134
Q

greaseless base properties

A
  • water soluble
  • good for incorporating solid compounds
  • soften with addition of water
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
135
Q

example of greaseless bases

A

PEG ointment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
136
Q

What does PEG stand for and what are its other names?

A
  • Polyethylene glycol
  • PEO (polyethylene oxide)
  • POE (polyoxy ethylene)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
137
Q

What are the ways in which you can prepare ointments?

A
  • incorporation method

- fusion method (melt)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
138
Q

What materials can you use for the incorporation method?

A
  • pill tile
  • parchment paper
  • unguator
  • mortar and pestle
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
139
Q

What is an unguator?

A
  • electronic mortar and pestle

- equipment that goes inside the ointment jar an into the machine consists of a shaft and a blade

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
140
Q

Define levigation

A

triturating a powder in an insoluble solvent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
141
Q

What are examples of levigating agents?

A
  • mineral oil for oil phases

- glycerin for water phases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
142
Q

What are the steps to the incorporation method?

A
  • incorporate drug into absorption base

- incorporate absorption base into oleaginous base

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
143
Q

What is one thing to note when mixing ingredients in the fusion method?

A

mix the excipients with the highest melting point first

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
144
Q

What are products that you HAVE to use fusion method for?

A
  • beeswax
  • paraffin
  • stearyl alcohol
  • PEG with high molecular weight
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
145
Q

What are things to consider when selecting the appropriate bases?

A
  • release rate of drug from semi-solid
  • desirability of topical or percutaneous drug absorption
  • desirability of occulsion of moisture from the skin
  • stability of drug in base
  • contact time to skin
  • which part of the body it’s being applied to
146
Q

What are dosage forms of semi-solids?

A
  • ointments
  • creams
  • gels
  • pastes
147
Q

What does the # following PEG indicate?

A

the average molecular weight

148
Q

PEG physical state with respect to molecular weight

A
  • lower mw are liquid; higher mw are solids
  • 200-600 transprent liquid
  • 600-1000 semi-solid
  • > 1000 solid
149
Q

What materials can you use for the fusion method?

A
  • small sacle: porcelain dish, glass beaker

- large sacle: large steam jacketed kettles

150
Q

Example of USP test for semi-solids

A
  • minimum-fill
  • microbial content
  • packaging
  • storage
  • labeling
151
Q

Properties of ophthalmic preparations

A
  • diameter should be < 50microm

- sterile

152
Q

Examples of preservatives

A
  • paraben
  • phenols
  • benzoic acid
  • sorbic acid
  • quaternary ammonia compounds
  • benzalkonium chloride
153
Q

Properties of creams

A
  • emulsions (usually o/w but can be w/o)
  • can be easily washed off skin
  • opaque
  • once applied on skin, water evaporates and leaves behind a thin layer
154
Q

Properties of gels

A
  • aka jellies
  • thixotropic
  • must have gelling agent
155
Q

Examples of gelling agents

A
  • cabomer 940
  • natural gums (tragacanth)
  • cellulose derivatives ex:
  • sodium carboxymethylcellulose
  • HPMC
  • carboxymethylcellulose
156
Q

Properties of pastes

A
  • must contain at least 20% of solid content

- able to absorb serous fluid

157
Q

What are plasters used for?

A

to remove corn

158
Q

What can glycerogelatin be used for?

A

varicose ulcer

159
Q

TDD

A
  • transdermal drug delivery
  • aka percutaneous absorption
  • absorb into system via skin
160
Q

scopolamine

A
  • approved by FDA 1979

- first TDDS approved

161
Q

nitroglycerine

A
  • aka trinitroglycerine
  • used in angina pectoris and CHF
  • releases NO (vasodilator)
162
Q

clonidine

A

used for HTN

163
Q

nicotine

A

used for smoking cessation

164
Q

applications of creams

A
  • topical skin products

- rectal and vaginal

165
Q

properties of jars

A
  • clear opaque glass

- plastic

166
Q

properties of tubes

A
  • aluminum

- plastic

167
Q

aluminum tubes

A

coated with epoxy resin or vinyl to eliminate any interactions between tube and content

168
Q

plastic tubes

A

made of high and/or low density polyethylene

169
Q

What is a crimping clip?

A

a clip to seal off the end of a metal ointment tube

170
Q

properties of skin

A
  • in adult, covers 2m2
  • weighs 11 lbs
  • receives 1/3rd of blood circulation
  • avoid first pass metabolism
171
Q

anatomy of skin

A
  • epidermis (outer layer)

- dermis (deeper layer)

172
Q

properties of epidermis

A
  • epithelial tissue
  • semi-permeable membrane
  • contain 90% keratinocytes and 8% melanocytes
173
Q

properties of dermis

A
  • strong connective tissue

- collagen and elastic fibers

174
Q

How does drug molecule penetrate the skin?

A

via passive diffusion

175
Q

layers of epidermis

A
  • stratum corneum
  • stratum lucidum
  • stratum granulosum
  • stratum spinosum
  • stratum germinativum / basale
176
Q

Rotigotine

A
  • used in parkinson

- brand name: Neupro

177
Q

Rivastigmine

A
  • anticholinesterase
  • used for Alzhiemers
  • brand name: Exelon
178
Q

stratum corneum

A

rate limiting step for drug absorption

179
Q

subq

A
  • hypodermis; not part of the skin
180
Q

What are the properties that influence transdermal absorption?

A
  • physico-chemical properties
  • drug concentration
  • site of absorption
  • hydration status
  • time of contact
  • race
  • individual variation: disease state, genetic, age, etc.
181
Q

What are the types of physico-chemical properties?

A
  • molecular weight
  • solubility; part. coeff. of 1 preferred
  • dissociation constant
    nature of carrier
182
Q

What are the categories of enhancers for skin absorption?

A
  • chemical
  • iontophoresis
  • electroporation
  • sonophoresis
183
Q

What are other names for chemical enhancers?

A
  • absorption promoter / enhancer

- permeation promoter / enhance

184
Q

chemical enhancers

A
  • reducing resistance in s. corneum

- causes temporary opening of tight junctions

185
Q

What are things to consider when selecting a chemical enhancer?

A
  • physico-chemical properties
  • compatibility with formulation
  • toxicity to s. corneum
186
Q

Examples of chemical enhancers

A
  • dimethyl sulfoxide (DMSO)
  • azone
  • acetone
  • oleic acid
  • propylene glycol
  • sodium dodecyl sulfate
  • sodium lauryl sulfate
187
Q

iontophoresis

A
  • electric current of 12-20v applied
  • increase permeability of skin
  • creates ion-electric field interaction -> directional force drives ion through skin
  • facilitates deep penetration
188
Q

Examples of iontophoresis

A 
- lidocaine 
drugs being investigated for this kind of delivery: 
- dexamethason 
- amino acids 
- peptides 
- verapamil 
- propranolol
189
Q

What are qualities of drugs for iontophoresis?

A

any drug, as long as it’s ionizable

190
Q

What can be used to treat hyperhidrosis?

A
  • hyperhidrosis = excessive sweating

- iontophoresis

191
Q

electroporation

A
  • electric current of 200-1000v applied for millisecond
  • increases size of pores
  • increases permeability up to four times
  • has been used to deliver drugs with mw of several kDaltons
192
Q

What is another name for electroporation?

A

electropermeability

193
Q

What is another name for sonophoresis?

A

phonophoresis

194
Q

sonophoresis

A

application of high frequency ultrasound

195
Q

For transdermal drug delivery, what are ultrasounds used with?

A

coupling agent (gel, cream, etc) that transfers US energy from US transducer to skin

196
Q

examples of drug permeation testing systems

A
  • side-by-side diffusion cell (not used for human skin)

- Franz diffusion cell (top-to-bottom diffusion; take gravity into account)

197
Q

What are the components of TDDS?

A
  • adhesive
  • backing layer
  • frontal layer
198
Q

What is the backing layer made of?

A

Aluminum (but doesn’t have to be)

199
Q

monolithic system and examples

A
  • drug and polymer mixed together

- Nitro-dur, Vivelle dot, Testoderm

200
Q

membrane-controlled system and examples

A
  • drug and polymer are in separate compartments
  • can use liquid and semi-solids
  • TrasdermNitro, Transderm-Scop
201
Q

What are the barriers to ocular drug retention?

A
  • nascolacrimal duct
  • tear turnover
  • conjunctival uptake
202
Q

What is the nasolacrimal duct?

A
  • connection between eye and nose

- drugs can be cleared through this

203
Q

On average, how much fluid is there in the eye?

A

7-9 microL

204
Q

How much displacement of fluid can a drop of fluid give in the eye?

A
  • 50 microL

- ideal is 10-15 but there isn’t a dropper that can deliver that

205
Q

List categories of ocular drugs

A
  • anesthetics
  • antibiotics
  • antifungal
  • anti-inflammatory
  • antivirals
  • astringents
  • beta blockers
  • miotics
  • mydriatics
206
Q

What are astringents formulations used for in the eye?

A

constrict blood; used in conjunctivitis

207
Q

What are types of dosage ocular forms?

A
  • solutions
  • gel forming
  • suspensions
  • semi-solids
  • inserts
  • injections / implants
208
Q

ocular solutions

A
  • most common
  • contains buffers, emulsifiers, preservatives, etc.
  • short contact with eye
209
Q

delivery vehicles for ocular solutions

A
  • water
    aq. mixtures of:
  • lower alkanols
  • vegetable oils
  • polyalkylene glycols
  • petrolatum based jellies
210
Q

What are examples of in-vitro apparatuses?

A
  • skin cadaver
  • synthetic skin
  • synthetic polymers
  • side-by-side diffusion chain / cells
  • top-to-bottom cell
211
Q

ex-vivo

A

take organ out of body

212
Q

in-situ

A

procedure done in localized area

213
Q

What are advantages of transdermal delivery?

A
  • avoids first pass metabolism
  • decreased drug-food interaction
  • extended therapy with single application
  • increased patient compliance
214
Q

What are disadvantages of transdermal delivery?

A
  • only potent drugs can be used
  • developments of contact dermatitis
  • irritation of skin
  • expensive
215
Q

polymers (all)

A
  • cellulose derivatives (HEC, HPMC, NaCMC)
  • acrylic acid
  • PVA
  • combinations: PVP-ethylcellulose
  • gellan
  • xanthum gum
  • pluronics
216
Q

With respect to ocular solutions, how can contact time between eye and solution increase?

A

addition of polymers

217
Q

ocular gel-forming solutions

A
  • gel + polymer
  • once instilled in eye, gel is formed
  • enhanced retention
218
Q

What causes the geling formation in the eye when gel-forming solutions are applied?

A
  • pH
  • tear formation
  • ionic strength
  • temperature
  • proteins
  • components of tears
219
Q

What is the temperature for the anterior portion of the eye?

A

34°C

220
Q

What are the polymers used in gel-forming solutions?

A
  • gellan
  • xanthum gum
  • carbomer
  • pluronic
  • CAP
  • methyl cellulose
221
Q

ocular suspensions

A
  • must be > 10 microm to decrease irritation
  • longer contact time that solution
  • particles retained in cul-de-sac
222
Q

ocular semisolids

A
  • block vision - restricted to use at bedtime
  • used often in children and post-operation
  • longer contact time
223
Q

What is used as the base in ophthalmic ointments?

A

mineral oil; mixture of white and liquid petrolatum

224
Q

What polymers are used to develop ophthalmic gels?

A
  • gellan
  • xanthum gum
  • carbomer
  • pluronic
  • CAP
  • methyl cellulose
225
Q

ocular inserts

A
  • put insert in cul de sac

- designed to release drug slowly on zero order kinetics

226
Q

ocular injections

A
  • to reach posterior area
  • intravitreal
  • juxtascleral
  • subconjunctival
  • intrasclera
227
Q

ocular implant

A
  • planted in vitreous cavity
  • releases drug over a certain period
  • removed after therapy
228
Q

What are things to consider with respect to ophthalmic preparations?

A
  • sterility
  • preservatives
  • isotonicity
  • buffer / pH
229
Q

sterilization techniques

A
  • moist heat under pressure
  • dry heat
  • filtration
  • gas sterilization
  • ionizing radiation
230
Q

moist heat sterilization

A
  • 121°C or 250°F

- 15 min

231
Q

dry heat sterilization

A
  • 160°C or 320°F

- 2 hours

232
Q

filter sterilization

A

pores of filter are 0.2-0.7 microm

233
Q

gas sterilization

A

ethylene oxide

234
Q

preservatives for ocular drugs

A
  • Quaternary ammonium compounds
  • Oxidizing agents
  • Organic mercurials
  • Para-hydroxy benzoic acid esters
  • Substituted alcohols and phenols
235
Q

body’s physiological tonicity

A
  • 0.9% NaCl
  • 290mOsm
  • 1.9% boric acid
236
Q

What type of solution is used to treat corneal edema?

A

hypertonic

237
Q

What is normal tear fluid pH?

A
  1. 4

- can tolerate pH change better than we anticipate

238
Q

What is the composition of buffers?

A

usually weak acid + conjugate base

239
Q

Besides resistance in pH change, what else does buffers do?

A

stabilize drug

240
Q

What are the types of contact lenses?

A
  • hard
  • soft
  • rigid gas permeable
241
Q

hard contact lenses

A
  • not permeable
  • offer clarity and crisp vision
  • only cover cornea
  • diameter of 7-10microm
  • made of PMMA
242
Q

soft contact lenses

A
  • not permeable
  • softer and pliable
  • not as clear
  • diameter of 13-15microm
  • made of HEMA
243
Q

rigid glass permeable (RGP)

A
  • permeable

- provide visual clarity

244
Q

What are the types of care products for contact lenses?

A
  • wetting solutions
  • cleaning solutions
  • disinfectants
  • soaking and storage solutions
245
Q

wetting solutions: contact lenses

A
  • cellulose derivatives
  • polyvinyl pyrrolidone
  • polyvinyl alcohol
246
Q

cleaning solutions: contact lenses

A
  • surfactants

- enzymes

247
Q

disinfectants: contact lenses

A
  • hydrogen peroxide

- polyquad

248
Q

soaking and storage solutions: contact lenses

A
  • chlorhexidine

- benzalkonium chloride

249
Q

What are the types of suppositories?

A
  • rectal
  • vaginal
  • urethral (less common)
250
Q

What kind of effects are suppositories used for?

A
  • local

- systemic (less common)

251
Q

properties of rectal suppositories

A
  • adults weigh 2g, pediatrics weigh 1g
  • 1.5 in long
  • cylindrical
252
Q

What are the systemic drug uses for rectal suppositories?

A
  • sedatives
  • tranquilizers
  • nausea
  • analgesics
253
Q

What is another name for vaginal suppositories?

A

pessaries

254
Q

properties of vaginal suppositories

A
  • weigh 5g
  • oviform of globular shaped
  • sometimes needs applicator
  • mostly used for local effects
255
Q

properties of vaginal inserts

A
  • ovoid shaped tablets
  • must be administered with inserter
  • disintegrated inside the vagina
256
Q

What is another name for urethral suppositories?

A

bougies

257
Q

properties of urethral suppositories

A
  • cylindrical slender shape
  • males: 5mm diam, 125mm length
  • females: 5mm diam, 50mm length
  • need applicator
258
Q

What are urethral suppositories usually used for?

A

local anesthetic for examination

259
Q

What are the types of suppository bases?

A
  • cocoa butter and other fatty bases
  • water-soluble or water-dispersible bases
  • hydrogels
260
Q

What are ideal properties of a suppository base?

A
  • non-irritating to mucous membranes
  • compatible with a variety of drugs
  • melts, dissolves, or swells in rectal/vaginal fluids
  • should not interfere with release or absorption of drug substances
261
Q

cocoa butter and other fatty bases properties

A
  • naturally occurring triglyceride
  • melts at body temperature
  • smooth; lubricant not needed
  • exhibits polymorphism
262
Q

What are substitutes to cocoa butter?

A
  • hydrated fat
  • hydrogenated regular oil
  • suffer polymorph but have potential for lower rancidity
263
Q

What are the polymorphs for cocoa butter?

A
  • α melt at 18°C
  • β melt at 37°C
  • γ melt at 22°C
  • melting temp. should not exceed 60°C or it will polymorph from β to α
264
Q

What is another name for cocoa butter?

A

theobroma oil

265
Q

water-soluble or water-dispersible bases properties

A
  • dissolves / solubulizes
  • offer prolonged release of drug
  • can be stored at room temperature
  • contain PEG or glycerinated gelatin
266
Q

hydrogels properties

A
  • swelling mechanism (via polymer)

- drug comes out of polymer

267
Q

examples of hydrogel polymers

A
  • polyvinyl alcohol (PVA)
  • hydroxyethyl methacrylate
  • polyacrylic acid
  • polyoxyethylene
268
Q

What are the ways in which you can prepare suppositories?

A
  • rolling (hand-shaping)
  • compression
  • molding (fusion)
269
Q

How should glycerinated gelatin suppositories be stored?

A

packaged tightly closed in screw-capped containers and stored at room temperature

270
Q

What are the uses for otic drug preparations?

A
  • ear infections
  • inflammation
  • pain
  • removal of cerumen
  • local only; no systemic
271
Q

What makes up the outer ear?

A
  • pinna
  • external auditory canal
  • tympanic membrane
272
Q

What makes up the middle ear?

A
  • auditory ossicles

- air-filled cavity in ear drum

273
Q

What makes up the inner ear?

A
  • chochlea

- vestibule and semi-circular canals

274
Q

What are formulations of otic drugs?

A
  • solutions
  • suspensions
  • semi-solids
275
Q

What is used as the traditional method to soften cerumen for removal?

A
  • light mineral oil
  • vegetable oil
  • hydrogen peroxide
276
Q

What is the active ingredient for products to soften cerumen?

A

cabamide peroxide which releases oxygen to disrupt integrity of impacted wax

277
Q

What dosage forms are the only ones that you can use with controlled drug delivery (CDD)?

A
  • tablets

- capsules

278
Q

What are the types of controlled drug delivery (CDD)?

A

XL, SR, ER, CR, PA, PL, SA, TR

279
Q

What are CDD useful for?

A

to treat chronic diseases

280
Q

What is dose dumping?

A

when the CDD fails and delivers the amount of drug in the tablet all at once

281
Q

Define CDD

A

drug system that is capable of spatial placement and temporal release of a drug

282
Q

What does spatial placement pertain to?

A

release of drug in a particular location

283
Q

What does temporal placement pertain to?

A

time release of the drug

284
Q

What are the ways in which you can maintain sustained plasma levels of the drug?

A
  • multiple dosing
  • intermittent infusion
  • constant infusion
285
Q

After how many half lives can we assume that the drug is out of the body?

A
  • four

- some literature use 3.3 because that equals 90%

286
Q

intermittent infusion

A

drug is given continually but not continuously

287
Q

multiple dosing

A
  • requires strict adherence
  • cannot tolerate missed doses
  • if doses are missed, plasma levels not sustained and may fall below MEC
288
Q

What is the assumption for CDD?

A

kinetics of drug release governs drug availability

289
Q

What are the types of CDD systems?

A
  • osmotically controlled
  • swelling controlled
  • diffusion controlled
  • dissolution controlled
  • ion-exchange resin
  • complex formation
  • magnetically controlled
  • electrically controlled
290
Q

osmotically controlled system

A
  • has a hole in the tablet
  • polymer is semi-permeable
  • pH independent
291
Q

With respect to osmotically controlled systems, what does it mean that the polymer is semi-permeable?

A

water and GI fluids can enter tablet but not permeable to substances coming out of tablet

292
Q

example(s) of osmotic agents

A
  • mannitol

- xylitol

293
Q

What is osmotically controlled systems dependent on?

A
  • size of hole
  • type of polymer
  • type of osmotic agent / osmotic pressure
  • saturated solubility of drug
294
Q

Example(s) of semi-permeable membranes used to regulate osmotic permeation of water

A
  • cellulose derivatives
  • polyvinyl chloride
  • polyvinyl alcohol
295
Q

How does the osmotic agent play a role in osmotically controlled systems?

A
  • osmotic agent creates a high osmotic pressure gradient inside the tablet
  • fluid enters the tablet (osmosis)
  • increase in volume -> drug gets pushed out of hole
296
Q

swelling controlled system

A
  • polymer and drug tightly packed

- once in GIT, polymer swells to release drug

297
Q

In a swelling controlled system, what is the release of drug dependent on?

A

rate of water sorption in polymer

298
Q

Example(s) of polymers used in swelling controlled systems

A
  • poly acrylic acid
  • sodium alginate
  • cellulose derivatives
299
Q

diffusion controlled system

A

polymer is physical barrier to drug release

300
Q

In a diffusion controlled system, what is the release of drug dependent on?

A
  • nature of polymer

- thickness of polymer

301
Q

What are the categories of diffusion controlled systems?

A
  • reservoir

- matrix

302
Q

describe the reservoir diffusion controlled systems

A
  • drug is coated with water-insoluble polymer
  • water penetrate through polymer to reach drug
  • drug dissolved to produce saturated solution
  • saturated solution diffuses through polymer to outside
303
Q

If the polymer for reservoir diffusion controlled system is water-insoluble, how does the drug diffuse through it to the outside?

A

osmotic movement through polyemeric mesh (space between macromolecular chains)

304
Q

For reservoir diffusion controlled systems, how can release of drug remain constant?

A

if concentration of drug in the core remains at saturation

305
Q

describe the matrix diffusion controlled systems

A
  • aka monolithic

- drug dispersed in polymeric matrix

306
Q

Polymers for diffusion controlled systems

A
  • reservoir’s polymers are water-INsoluble

- matrix’s can be both

307
Q

fate of polymers for matrix diffusion controlled systems

A
  • erode with tiem
  • dissolve
  • stay intact as ghost matrix
308
Q

dissolution controlled system

A

dissolution of drug is the major role in drug release

309
Q

ion exchange resin system

A

drug is resinated and then formulated in it’s respective dosage form

310
Q

What does it mean for a drug to be resinated?

A
  • cationic / anionic drug passed through ion exchange resin
  • cations replace H atoms
  • anions replace OH atoms
  • drug-resin complex = resinated
311
Q

complex formation systems

A
  • drug complexes which are slowly soluble in GI fluid; pH dependent
  • salts of tannic acid used for this purpose
312
Q

Characteristics of controlled release systems

A
  • not for all drugs
  • not all medical conditions need it
  • dissolution and absorption release of drug should be predictable
  • rate of drug release is controlled
  • rate of drug release = rate of drug elimination
313
Q

Ideal drug candidates for controlled release systems

A
  • Absorption/elimination rate shoud not be too fast or slow
  • Uniformly absorbed form the GI tract
  • Effective dose should be small
  • Possess good margin of safety
  • Used for chronic conditions
314
Q

Limitations of controlled release systems

A
  • Dose dumping
  • Termination of therapy is not easy
  • Variable release of drug
  • Absorption of released drug may not be constant
  • Delayed release = delayed immediate effect of drug
315
Q

What does modified release refer to?

A

drug release based on time, course, or location not offered by conventional dosage forms

316
Q

What are the categories of modified release?

A
  • extended release

- delayed release

317
Q

extended release

A

allows a reduction in dosing frequency

318
Q

delayed release

A

releases drug at a time other than promptly after administration

319
Q

What are repeat action tablets?

A

two layer tablet; one layer is IR and second layer is DR

320
Q

What are targeted release tablets/capsules?

A

directed towards a target location in the GI tract

321
Q

Can CNS drug targeting be viewed as advanced drug delivery?

A

Yes; needs to pass BBB

322
Q

What are categories of nanoparticulate systems?

A
  • nanocapsule (encapsulated drug, reservoir)

- nanospheres (drug-polymer matrix)

323
Q

T/F; Polymeric nanoparticles can only carry low MW substances.

A

False

  • can deliver both low and high MW substances
  • ex. genes, proteins
324
Q

What are the advantages of nanoparticles?

A
  • increased bioavailability
  • protection from degradation
  • specific targets
325
Q

characteristics of tumor vasculature

A
  • heterogeneous distribution
  • larger in size
  • high vascular density
  • more permeable
  • more leaky
326
Q

What factor allows retention of NP in solid tumors?

A
  • high vasculature

- production of vascular mediators

327
Q

F

A
  • bioavailability

- dose / AUC

328
Q

How can you actively target a tumor?

A
  • ligand-receptor

- antibody-antigen

329
Q

How are NPs utilized in targeting cancer cells?

A

NP conjugated with tissue or cell-specific ligand

330
Q

examples of ligands

A
  • lectins
  • carbohydrates
  • transferrin
  • folate
331
Q

passive targeting

A

delivering drug at local site

332
Q

What are vectors?

A

gene carrier used in gene therapy

333
Q

Steps in gene therapy

A
  • genetic material packaged in vector to be transferred
  • vector enters cytoplasm
  • gene from vector to nucleus
  • gene integrated into cellular DNA (if need be)
  • gene expressed
334
Q

What are the categories used in gene therapy?

A
  • viral

- non-viral

335
Q

viral vectors

A
  • part of viral genome replaced by therapeutic gene

- this gene taken up by target cells and expressed

336
Q

examples that viral vectors were used for

A
  • retrovirus
  • adenovirus
  • adeno-associated virus
  • herpes simplex virus (HSV)
337
Q

risks of viral vectors

A
  • inflammation

- cellular / humoral immune response

338
Q

What are the components of a non-viral vector?

A
  • therapeutic gene
  • gene expression system
  • gene delivery system
339
Q

plasmid-based vectors

A

non-viral

340
Q

size of plasmid DNA

A
  • huge polyanion

- 100-200 nm

341
Q

Plasmid potency can be reduced by which factors?

A
  • chemical instability
  • enzymatic instability
  • colloidal instability
  • sequestered by immune system
  • uptake / adsorption of non-target cells
342
Q

What are the most commonly used synthetic gene carrier?

A
  • cationic polymers

- lipids

343
Q

What are advantages of using cationic polymers / lipids as a gene carrier?

A

they condense plasmids into small particles and protect them from degradation

344
Q

Lipid-based gene delivery

A
  • low efficiency
  • pH sensitive
  • fusogenic at acidic pH
  • facilitate release of plasmid in endosome
345
Q

Peptide-based gene delivery

A

linked macromolecules complexed into plasmids via electrostatic interaction

346
Q

Polymer-based gene delivery

A
  • made to interact at a more cellular / protein level

- high specificity

347
Q

ideal features of gene delivery system

A
  • reach appropriate cellular target
  • penetrate into target cells
  • gene integrate with cell’s DNA
  • avoid destruction by body
348
Q

ex-vivo: gene therapy

A
  • take cells out of body
  • cells treated in lab
  • cell inserted back in body
349
Q

in-vivo: gene therapy

A
  • administration of vector in body

- low integration / efficacy

350
Q

What are the transport mechanisms for the brain endothelium to take up nutrients into CNS?

A
  • passive diffusion
  • carrier mediated
  • receptor-mediated transcytosis (RMT)
351
Q

What are substrates for RMT?

A

polypeptide

352
Q

Give an example of RMT

A

cerebral insulin reaching the brain from circulation

353
Q

What are the invasive CNS delivery techniques?

A
  • intracerebroventricular drug infusion
  • implants
  • reversible BBB disruption
354
Q

intracerebroventricular drug infusion

A

direct injection of drug into brain ventricles and large cavities in middle of the brain

355
Q

implants( CNS delivery

A

implant genetically engineered cells that secrete a drug or polymeric matrix or reservoir containing drug in the brain

356
Q

Gliadel

A

commercial product that is used in polymeric implant for CNS delivery

357
Q

Reversible BBB disruption

A

disruption of BBB by intracarotid injection of hyperosmolar (2M) solutions of mannitolr, vasoactice substances like leukotrienes and bradykinins

358
Q

What are the non-invasive CNS delivery techniques?

A
  • lipidization

- exploitation of carrier mediated system

359
Q

lipidization

A
  • non-invasive CNS delivery
  • blocking H bond functional groups to increase lipophilicity
  • binding drug to lipid moieties
  • convert drug to more lipophilic prodrug
360
Q

exploitation of carrier mediated system

A
  • non-invasive CNS delivery

- drug with similar molecular structure to molecules that get carried into brain via carrier

361
Q

examples of drug that uses exploitation of carrier mediated system to get into CNS

A
  • methyldopa
  • methylparatyrosine
  • phenylalanine mustard

OU Pharmaceutics (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions