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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
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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
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3
Q

How can capsules be closed?

A
  • welded with heated metal pin
  • bonded with molten gelatin
  • snap fit
  • coni-snap
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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
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5
Q

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

A
  • plate process

- die process

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6
Q

What does the die process consists of?

A
  • a process which to manufacture soft gelatin capsules
  • rotary process
  • reciprocating process
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7
Q

What is the plate process?

A
  • a process which to manufacture soft gelatin capsules

- molds

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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
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9
Q

What are the different types of coating for coated tablets?

A
  • Sugar
  • Film (make tablet more sturdy)
  • Gelatin
  • Enteric
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10
Q

What are the types of specialized tablets?

A
  • chewable
  • effervescent
  • CR, ER
  • sublingual
  • buccal
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11
Q

What are the essential ingredients for tablets?

A
  • diluent
  • binder
  • lubricant
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12
Q

Why would any ingredient be essential to tablets?

A

give the formula specific characteristics needed to be compressed

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13
Q

What are the ingredients to give tablets desirable characteristics?

A
  • disintegrant
  • color
  • flavor
  • sweetening agent
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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
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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

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16
Q

What are examples of diluent?

A
  • lactose
  • calcium phosphate
  • microcrystalline cellulose (Avicel®)
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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

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18
Q

How can a diluent affect bioavailability?

A

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

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19
Q

Define binder

A

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

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20
Q

What are examples of binders?

A
  • starch (10-20% paste)
  • gelatin (10-20% solution)
  • acacia
  • CMC
  • PVP
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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

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22
Q

What are examples of lubricant?

A
  • talc (1-5%)

- magnesium stearate

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23
Q

Why does talc undergo testing?

A

it may contain metals

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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
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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

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26
Q

What is an example of a glidant?

A

talc

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27
Q

Define disintegrant

A

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

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28
Q

What are examples of distinegrants?

A
  • starch

- celluloses

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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
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30
Q

Why doesn’t effervescent tablets need disintegrants?

A

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

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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
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32
Q

What are examples of flavoring agents?

A
  • Cyclamates and saccharine (banned)

- Aspartame

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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

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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
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35
Q

What are the different kinds of coatings?

A
  • sugar coated
  • film coated
  • gelatin coated
  • enteric coated
  • compression coated
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36
Q

Purposes of sugar coating

A
  • protection from air and humidity

- improve taste and smell

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37
Q

What can be used to waterproof tablets?

A

Shellac

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38
Q

What is used to smooth tablets?

A

dibasic calcium phosphate, titanium oxide, starch

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39
Q

Purposes of film coating

A
  • improve presentation
  • increase stability
  • improve taste
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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

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41
Q

What are examples of enteric coating materials?

A
  • cellulose acetate phtalate
  • poly(methacrylic acid-co-methyl-methacrylate)
  • poly(vinyl acetate phtalate)
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42
Q

What are some commercially available for use enteric coating solutions?

A
  • Aquateric®
  • Caoteric®
  • Eudragits™
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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)
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44
Q

Describe ingredients in sublingual tablets

A

lactose or mannitol and saccharine is massed with 60% ethanol

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45
Q

What are ingredients in buccal tablets?

A
  • lactose or mannitol
  • HPMC
  • silica gel
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46
Q

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

A

a layer of solution which is saturated with the drug

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47
Q

Define sink condition

A

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

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48
Q

What are factors that influence dissolution from solid dosage forms?

A
  • dosage form
  • solubility
  • dissolution media
  • partition coefficient
  • diffusivity
  • diffusional path thickness
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49
Q

What are three interaction forces that occur in powder samples?

A
  • capillary forces
  • mechanical interlocking
  • electrostatic charges
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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
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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

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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
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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
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54
Q

Causes of capping / lamination

A
  • insufficient binder
  • undermixing of tablets ingredients
  • fast speed of compression
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55
Q

Causes of sticking / picking

A
  • insufficient amount of lubricant

- improper application of coating or insufficient drying time

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56
Q

Causes of erosion / chipping

A
  • tablets are friable
  • fast pan rotation during coating
  • poor choice of plasticizer
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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
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58
Q

What are different types of media for dissolution?

A
  • water
  • solution with buffer
  • simulated gastric fluid (SGF)
  • simulated intestinal fluid (SIF)
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59
Q

What does SGF consists of?

A
  • 0.2% NaCl in 0.7% HCl

- pepsin

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60
Q

What does SIF consists of?

A
  • Phosphate buffer, pH=6.8

- pancreatin

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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
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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
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63
Q

Apparatus 3

A
  • reciprocating cylinder
  • 4-12h dissolution test
  • standard volume 200-250mL
    used for
  • controlled release tablets & beads
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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
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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
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66
Q

Apparatus 5

A
  • paddle over disk
  • standard volume = 900m L
  • used for transdermal patches
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67
Q

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

A

15 - 60 minutes

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68
Q

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

A

10-30 microm

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69
Q

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

A

5-10 microm

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70
Q

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

A

1-5 microm

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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
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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)
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73
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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74
Q

What does formulation enhancers do to the drug?

A
  • increase absorption

- increase time spent in cavity via mucoadhesives

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75
Q

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

A

nasal irritation

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76
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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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
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78
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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79
Q

What are surfactants used for in nasal dosage form?

A

to reduce surface tension for drug to penetrate membrane

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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

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81
Q

What is a popular bioadhesive?

A

chitosan

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82
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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83
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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84
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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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

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86
Q

Define aerosol

A

dispersion of particles or droplets suspended in a gas or vapor

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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
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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)

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89
Q

What are limitations of pulmonary route?

A
  • lungs designed to prevent inhalation of exogenous compounds / particulates
  • oropharyngeal irritation, taste
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90
Q

Define aerodynamic diameter

A

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

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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
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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
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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

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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
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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

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96
Q

What can hygroscopic particles do?

A

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

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97
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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98
Q

What are types of nebulizers?

A
  • air jet (makes up majority)

- ultrasonic

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99
Q

What are advantages of nebulizers?

A
  • Aqueous solutions: no environmental concerns

- Does not depend on patient inspiratory force

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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
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101
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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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
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103
Q

Advantages of ultrasonic nebulizer

A

can created smaller particles

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104
Q

Disadvantages of ultrasonic nebulizer

A
  • complex apparatus
  • cannot be used by particles degraded by heat
  • not easily cleaned
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105
Q

Characteristics of solutions used for inhalation

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

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107
Q

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

A

– Beta2-adrenergic agonists
– Glucocorticoids
– Mast cell stabilizer

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108
Q

Define MDI

A

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

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109
Q

Advantages of MDI

A
  • portable
  • easy to use and convenient
  • drug is protected from light, O2, and water
  • tamper proof
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110
Q

Disdvantages of MDI

A
  • enpensive
  • prone to incorrect use
  • pressurized contents
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111
Q

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

A
  • formulation
  • valve design
  • actuator
  • propellant
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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

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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

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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
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115
Q

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

A
  • particle size
  • droplet evaporation
  • velocity
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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
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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
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118
Q

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

A

3-5 microm

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119
Q

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

A

alveolar region at <1 microm

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120
Q

What are the major components of an MDI?

A
  • canister
  • valve
  • actuator
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121
Q

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

A
  • seasonal allergies
  • pain
  • migraine
  • smoking cessation aids
  • influenza vaccine
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122
Q

What are humectants used for in nasal products?

A

to avoid dryness of nasal cavity while using medication

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123
Q

What are solubilizers used for in nasal products?

A

to increase the concentrations of drugs that have poor aqueous solubility

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124
Q

How do you apply semi-solid preparations?

A

topically

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125
Q

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

A
  • emollient (moisturizer)

- skin protectant

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126
Q

What are the classifications of bases for semi-solids?

A
  • oleaginous
  • absorption
  • water removable
  • greaseless
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127
Q

other names for oleaginous bases

A
  • hydrocarbon bases

- hydrophobic bases

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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
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129
Q

examples of oleaginous bases

A
  • regular and white petrolatum

- yellow and white ointment

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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
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131
Q

examples of absorption bases

A
  • hydrophilic petrolatum

- lanolin (wool fat)

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132
Q

water removable base properties

A
  • also known as water washable

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

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133
Q

example of water removable bases

A

hydrophilic ointment

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134
Q

greaseless base properties

A
  • water soluble
  • good for incorporating solid compounds
  • soften with addition of water
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135
Q

example of greaseless bases

A

PEG ointment

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136
Q

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

A
  • Polyethylene glycol
  • PEO (polyethylene oxide)
  • POE (polyoxy ethylene)
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137
Q

What are the ways in which you can prepare ointments?

A
  • incorporation method

- fusion method (melt)

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138
Q

What materials can you use for the incorporation method?

A
  • pill tile
  • parchment paper
  • unguator
  • mortar and pestle
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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

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140
Q

Define levigation

A

triturating a powder in an insoluble solvent

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141
Q

What are examples of levigating agents?

A
  • mineral oil for oil phases

- glycerin for water phases

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142
Q

What are the steps to the incorporation method?

A
  • incorporate drug into absorption base

- incorporate absorption base into oleaginous base

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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

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144
Q

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

A
  • beeswax
  • paraffin
  • stearyl alcohol
  • PEG with high molecular weight
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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?

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?

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?

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

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)

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