Exam 4 Spring 2017 Flashcards

1
Q

How do you apply semi-solid preparations?

A

topically

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2
Q

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

A
  • emollient (moisturizer)

- skin protectant

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3
Q

What are the classifications of bases for semi-solids?

A
  • oleaginous
  • absorption
  • water removable
  • greaseless
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4
Q

other names for oleaginous bases

A
  • hydrocarbon bases

- hydrophobic bases

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5
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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6
Q

examples of oleaginous bases

A
  • regular and white petrolatum

- yellow and white ointment

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7
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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8
Q

examples of absorption bases

A
  • hydrophilic petrolatum

- lanolin (wool fat)

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9
Q

water removable base properties

A
  • also known as water washable

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

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10
Q

example of water removable bases

A

hydrophilic ointment

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11
Q

greaseless base properties

A
  • water soluble
  • good for incorporating solid compounds
  • soften with addition of water
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12
Q

example of greaseless bases

A

PEG ointment

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13
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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14
Q

What are the ways in which you can prepare ointments?

A
  • incorporation method

- fusion method (melt)

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15
Q

What materials can you use for the incorporation method?

A
  • pill tile
  • parchment paper
  • unguator
  • mortar and pestle
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16
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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17
Q

Define levigation

A

triturating a powder in an insoluble solvent

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18
Q

What are examples of levigating agents?

A
  • mineral oil for oil phases

- glycerin for water phases

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19
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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20
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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21
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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22
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
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23
Q

What are dosage forms of semi-solids?

A
  • ointments
  • creams
  • gels
  • pastes
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24
Q

What does the # following PEG indicate?

A

the average molecular weight

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25
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
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26
Q

What materials can you use for the fusion method?

A
  • small sacle: porcelain dish, glass beaker

- large sacle: large steam jacketed kettles

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27
Q

Common infections occur via which bacteria?

A
  • Staphylococcus aureus

- Pseudomonas aeroginosa

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28
Q

The gram +/- terms were named after who?

A

Hans Christian Gram

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29
Q

Example of USP test for semi-solids

A
  • minimum-fill
  • microbial content
  • packaging
  • storage
  • labeling
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30
Q

Properties of ophthalmic preparations

A
  • diameter should be < 50microm

- sterile

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31
Q

Examples of preservatives

A
  • paraben
  • phenols
  • benzoic acid
  • sorbic acid
  • quaternary ammonia compounds
  • benzalkonium chloride
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32
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
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33
Q

Properties of gels

A
  • aka jellies
  • thixotropic
  • must have gelling agent
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34
Q

Examples of gelling agents

A
  • cabomer 940
  • natural gums (tragacanth)
  • cellulose derivatives ex:
  • sodium carboxymethylcellulose
  • HPMC
  • carboxymethylcellulose
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35
Q

Properties of pastes

A
  • must contain at least 20% of solid content

- able to absorb serous fluid

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36
Q

What are plasters used for?

A

to remove corn

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37
Q

What can glycerogelatin be used for?

A

varicose ulcer

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38
Q

TDD

A
  • transdermal drug delivery
  • aka percutaneous absorption
  • absorb into system via skin
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39
Q

scopolamine

A
  • approved by FDA 1979

- first TDDS approved

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40
Q

nitroglycerine

A
  • aka trinitroglycerine
  • used in angina pectoris and CHF
  • releases NO (vasodilator)
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41
Q

clonidine

A

used for HTN

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42
Q

nicotine

A

used for smoking cessation

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43
Q

applications of creams

A
  • topical skin products

- rectal and vaginal

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44
Q

properties of jars

A
  • clear opaque glass

- plastic

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45
Q

properties of tubes

A
  • aluminum

- plastic

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46
Q

aluminum tubes

A

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

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47
Q

plastic tubes

A

made of high and/or low density polyethylene

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48
Q

What is a crimping clip?

A

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

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49
Q

properties of skin

A
  • in adult, covers 2m2
  • weighs 11 lbs
  • receives 1/3rd of blood circulation
  • avoid first pass metabolism
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50
Q

anatomy of skin

A
  • epidermis (outer layer)

- dermis (deeper layer)

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51
Q

properties of epidermis

A
  • epithelial tissue
  • semi-permeable membrane
  • contain 90% keratinocytes and 8% melanocytes
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52
Q

properties of dermis

A
  • strong connective tissue

- collagen and elastic fibers

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53
Q

How does drug molecule penetrate the skin?

A

via passive diffusion

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54
Q

layers of epidermis

A
  • stratum corneum
  • stratum lucidum
  • stratum granulosum
  • stratum spinosum
  • stratum germinativum / basale
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55
Q

Rotigotine

A
  • used in parkinson

- brand name: Neupro

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56
Q

Rivastigmine

A
  • anticholinesterase
  • used for Alzhiemers
  • brand name: Exelon
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57
Q

stratum corneum

A

rate limiting step for drug absorption

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58
Q

subq

A
  • hypodermis; not part of the skin
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59
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.
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60
Q

What are the types of physico-chemical properties?

A
  • molecular weight
  • solubility; part. coeff. of 1 preferred
  • dissociation constant
    nature of carrier
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61
Q

What are the categories of enhancers for skin absorption?

A
  • chemical
  • iontophoresis
  • electroporation
  • sonophoresis
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62
Q

What are other names for chemical enhancers?

A
  • absorption promoter / enhancer

- permeation promoter / enhance

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63
Q

chemical enhancers

A
  • reducing resistance in s. corneum

- causes temporary opening of tight junctions

64
Q

What are things to consider when selecting a chemical enhancer?

A
  • physico-chemical properties
  • compatibility with formulation
  • toxicity to s. corneum
65
Q

Examples of chemical enhancers

A
  • dimethyl sulfoxide (DMSO)
  • azone
  • acetone
  • oleic acid
  • propylene glycol
  • sodium dodecyl sulfate
  • sodium lauryl sulfate
66
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
67
Q

Examples of iontophoresis

A
- lidocaine 
drugs being investigated for this kind of delivery: 
- dexamethason 
- amino acids 
- peptides 
- verapamil 
- propranolol
68
Q

What are qualities of drugs for iontophoresis?

A

any drug, as long as it’s ionizable

69
Q

What can be used to treat hyperhidrosis?

A
  • hyperhidrosis = excessive sweating

- iontophoresis

70
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
71
Q

What is another name for electroporation?

A

electropermeability

72
Q

What is another name for sonophoresis?

A

phonophoresis

73
Q

sonophoresis

A

application of high frequency ultrasound

74
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

75
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)

76
Q

What are the components of TDDS?

A
  • adhesive
  • backing layer
  • frontal layer
77
Q

What is the backing layer made of?

A

Aluminum (but doesn’t have to be)

78
Q

monolithic system and examples

A
  • drug and polymer mixed together

- Nitro-dur, Vivelle dot, Testoderm

79
Q

membrane-controlled system and examples

A
  • drug and polymer are in separate compartments
  • can use liquid and semi-solids
  • TrasdermNitro, Transderm-Scop
80
Q

What are the barriers to ocular drug retention?

A
  • nascolacrimal duct
  • tear turnover
  • conjunctival uptake
81
Q

What is the nasolacrimal duct?

A
  • connection between eye and nose

- drugs can be cleared through this

82
Q

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

A

7-9 microL

83
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

84
Q

List categories of ocular drugs

A
  • anesthetics
  • antibiotics
  • antifungal
  • anti-inflammatory
  • antivirals
  • astringents
  • beta blockers
  • miotics
  • mydriatics
85
Q

What are astringents formulations used for in the eye?

A

constrict blood; used in conjunctivitis

86
Q

What are types of dosage ocular forms?

A
  • solutions
  • gel forming
  • suspensions
  • semi-solids
  • inserts
  • injections / implants
87
Q

ocular solutions

A
  • most common
  • contains buffers, emulsifiers, preservatives, etc.
  • short contact with eye
88
Q

delivery vehicles for ocular solutions

A
  • water
    aq. mixtures of:
  • lower alkanols
  • vegetable oils
  • polyalkylene glycols
  • petrolatum based jellies
89
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
90
Q

ex-vivo

A

take organ out of body

91
Q

in-situ

A

procedure done in localized area

92
Q

What are advantages of transdermal delivery?

A
  • avoids first pass metabolism
  • decreased drug-food interaction
  • extended therapy with single application
  • increased patient compliance
93
Q

What are disadvantages of transdermal delivery?

A
  • only potent drugs can be used
  • developments of contact dermatitis
  • irritation of skin
  • expensive
94
Q

polymers (all)

A
  • cellulose derivatives (HEC, HPMC, NaCMC)
  • acrylic acid
  • PVA
  • combinations: PVP-ethylcellulose
  • gellan
  • xanthum gum
  • pluronics
95
Q

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

A

addition of polymers

96
Q

ocular gel-forming solutions

A
  • gel + polymer
  • once instilled in eye, gel is formed
  • enhanced retention
97
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
98
Q

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

A

34°C

99
Q

What are the polymers used in gel-forming solutions?

A
  • gellan
  • xanthum gum
  • carbomer
  • pluronic
  • CAP
  • methyl cellulose
100
Q

ocular suspensions

A
  • must be > 10 microm to decrease irritation
  • longer contact time that solution
  • particles retained in cul-de-sac
101
Q

ocular semisolids

A
  • block vision - restricted to use at bedtime
  • used often in children and post-operation
  • longer contact time
102
Q

What is used as the base in ophthalmic ointments?

A

mineral oil; mixture of white and liquid petrolatum

103
Q

What polymers are used to develop ophthalmic gels?

A
  • gellan
  • xanthum gum
  • carbomer
  • pluronic
  • CAP
  • methyl cellulose
104
Q

ocular inserts

A
  • put insert in cul de sac

- designed to release drug slowly on zero order kinetics

105
Q

ocular injections

A
  • to reach posterior area
  • intravitreal
  • juxtascleral
  • subconjunctival
  • intrasclera
106
Q

ocular implant

A
  • planted in vitreous cavity
  • releases drug over a certain period
  • removed after therapy
107
Q

What are things to consider with respect to ophthalmic preparations?

A
  • sterility
  • preservatives
  • isotonicity
  • buffer / pH
108
Q

sterilization techniques

A
  • moist heat under pressure
  • dry heat
  • filtration
  • gas sterilization
  • ionizing radiation
109
Q

moist heat sterilization

A
  • 121°C or 250°F

- 15 min

110
Q

dry heat sterilization

A
  • 160°C or 320°F

- 2 hours

111
Q

filter sterilization

A

pores of filter are 0.2-0.7 microm

112
Q

gas sterilization

A

ethylene oxide

113
Q

preservatives for ocular drugs

A
  • Quaternary ammonium compounds
  • Oxidizing agents
  • Organic mercurials
  • Para-hydroxy benzoic acid esters
  • Substituted alcohols and phenols
114
Q

body’s physiological tonicity

A
  • 0.9% NaCl
  • 290mOsm
  • 1.9% boric acid
115
Q

What type of solution is used to treat corneal edema?

A

hypertonic

116
Q

What is normal tear fluid pH?

A
  1. 4

- can tolerate pH change better than we anticipate

117
Q

What is the composition of buffers?

A

usually weak acid + conjugate base

118
Q

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

A

stabilize drug

119
Q

What are the types of contact lenses?

A
  • hard
  • soft
  • rigid gas permeable
120
Q

hard contact lenses

A
  • not permeable
  • offer clarity and crisp vision
  • only cover cornea
  • diameter of 7-10microm
  • made of PMMA
121
Q

soft contact lenses

A
  • not permeable
  • softer and pliable
  • not as clear
  • diameter of 13-15microm
  • made of HEMA
122
Q

rigid glass permeable (RGP)

A
  • permeable

- provide visual clarity

123
Q

What are the types of care products for contact lenses?

A
  • wetting solutions
  • cleaning solutions
  • disinfectants
  • soaking and storage solutions
124
Q

wetting solutions: contact lenses

A
  • cellulose derivatives
  • polyvinyl pyrrolidone
  • polyvinyl alcohol
125
Q

cleaning solutions: contact lenses

A
  • surfactants

- enzymes

126
Q

disinfectants: contact lenses

A
  • hydrogen peroxide

- polyquad

127
Q

soaking and storage solutions: contact lenses

A
  • chlorhexidine

- benzalkonium chloride

128
Q

What are the types of suppositories?

A
  • rectal
  • vaginal
  • urethral (less common)
129
Q

What kind of effects are suppositories used for?

A
  • local

- systemic (less common)

130
Q

properties of rectal suppositories

A
  • adults weigh 2g, pediatrics weigh 1g
  • 1.5 in long
  • cylindrical
131
Q

What are the systemic drug uses for rectal suppositories?

A
  • sedatives
  • tranquilizers
  • nausea
  • analgesics
132
Q

What is another name for vaginal suppositories?

A

pessaries

133
Q

properties of vaginal suppositories

A
  • weigh 5g
  • oviform of globular shaped
  • sometimes needs applicator
  • mostly used for local effects
134
Q

What are the most common pathogens to the vaginal tracts?

A
  • Trichomonas vaginalis
  • Candida albicans
  • Gardnerella vaginalis
135
Q

properties of vaginal inserts

A
  • ovoid shaped tablets
  • must be administered with inserter
  • disintegrated inside the vagina
136
Q

What is another name for urethral suppositories?

A

bougies

137
Q

properties of urethral suppositories

A
  • cylindrical slender shape
  • males: 5mm diam, 125mm length
  • females: 5mm diam, 50mm length
  • ## need applicator
138
Q

What are urethral suppositories usually used for?

A

local anesthetic for examination

139
Q

What are the types of suppository bases?

A
  • cocoa butter and other fatty bases
  • water-soluble or water-dispersible bases
  • hydrogels
140
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
141
Q

cocoa butter and other fatty bases properties

A
  • naturally occurring triglyceride
  • melts at body temperature
  • smooth; lubricant not needed
  • exhibits polymorphism
142
Q

What are substitutes to cocoa butter?

A
  • hydrated fat
  • hydrogenated regular oil
  • suffer polymorph but have potential for lower rancidity
143
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
144
Q

What is another name for cocoa butter?

A

theobroma oil

145
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
146
Q

hydrogels properties

A
  • swelling mechanism (via polymer)

- drug comes out of polymer

147
Q

examples of hydrogel polymers

A
  • polyvinyl alcohol (PVA)
  • hydroxyethyl methacrylate
  • polyacrylic acid
  • polyoxyethylene
148
Q

What are the ways in which you can prepare suppositories?

A
  • rolling (hand-shaping)
  • compression
  • molding (fusion)
149
Q

How should glycerinated gelatin suppositories be stored?

A

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

150
Q

What are the uses for otic drug preparations?

A
  • ear infections
  • inflammation
  • pain
  • removal of cerumen
  • local only; no systemic
151
Q

What makes up the outer ear?

A
  • pinna
  • external auditory canal
  • tympanic membrane
152
Q

What makes up the middle ear?

A
  • auditory ossicles

- air-filled cavity in ear drum

153
Q

What makes up the inner ear?

A
  • chochlea

- vestibule and semi-circular canals

154
Q

What are formulations of otic drugs?

A
  • solutions
  • suspensions
  • semi-solids
155
Q

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

A
  • light mineral oil
  • vegetable oil
  • hydrogen peroxide
156
Q

What is the active ingredient for products to soften cerumen?

A

cabamide peroxide which releases oxygen to disrupt integrity of impacted wax