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Pharmaceutics 2 > Quiz 1 > Flashcards

Quiz 1 Flashcards

1
Q

preformulation

A

research activities occurring between drug discovery and the filing of an IND prior to formulation/manufacturing development

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2
Q

Goals of preformulation research

A
  1. choose the correct form (solid/salt) of the drug substance
  2. evaluate its physical and chemical properties
  3. understand the stability of the drug as a material under conditions leading to successful development of a viable dosage form
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3
Q

Rule of 5

A

1st pass screen
states that acceptable systematic absorption is likely when at least 3 of the following criteria are met
molecular weight <500
c(logP) <5
H-bond donors <5
H-bond acceptors <10

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4
Q

Rule of 5 Exceptions

A
  1. certain antibiotics
  2. anti fungals (think sporonox)
  3. Vitamins
  4. Aminoglycosides
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5
Q

Biopharmaceutics Classification system

A

way of categorizing orally administered drugs according to the main factors that contribute to drug delivery by dissolution and passive drug absorption across GI epithelia

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6
Q

Class 1

A

High solubility
High permeability
poses lowest risk for development; biowaivers often granted by the FDA

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7
Q

Class 2

A

Low solubility
high permeability
dissolution rate-limited absorption; bioavailability can be improved by formulation/dosage form considerations

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8
Q

Class 3

A

High solubility
low permeability
permeability rate-limited absorption; rate and extent of absorption of API may be variable throughout GI fluid

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9
Q

Class 4

A

Low solubility
low permeability
presents significant problems for effective oral delivery

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10
Q

If systematic absorption is greater than or equal to 90% of the administered dose

A

high permeability

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11
Q

If systematic absorption is <90% the administered dose

A

low permeability

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12
Q

If volume of simulated GI fluid required to dissolve the highest dose of an API is less than 250 mL

A

high aqueous solubility

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13
Q

If volume of simulated GI fluid required to dissolve the highest dose of an API is greater than 250 mL

A

low aqueous solubility

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14
Q

What is the average of volume of GI fluid?

A

250mL

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15
Q

If delta pKa is greater than 0?

A

a salt forms

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16
Q

If pKa is less than 0

A

a salt does not form

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17
Q

What is the rate of dissolution directly proportional to?

A

the aqueous solubility

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18
Q

API salts are more water soluble in a pH that?

A

favors ionization

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19
Q

Between what two organs is there a pH jump?

A

the stomach and the duodenum

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20
Q

In general the salt with the highest what is selected?

A

Ksp

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21
Q

What are the most commonly marketed salts that go with basic API?

A

HCl salts

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22
Q

What does the common ion effect do to solubility?

A

decreases it

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23
Q

When a solution contains multiple feasible counterions for an API, the solubility of the drug is limited by?

A

the lowest solubility salt

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24
Q

How much HCl does the stomach have?

A

160mM

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25
Q

Concentrations of the drug greater than Cs adj will do what?

A

Precipitate out of the stomach and reduce bioavailability

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26
Q

How are salts selected?

A
  1. has to reproducibly form crystals for preparation of solid dosage forms
  2. crystals cannot deliquesce following adsorption of environmental water
  3. crystals must have mechanical properties conducive to solid dosage form manufacturing
  4. salt form should not be less chemically stable than the free form
  5. salt form should not be more toxic than the free form
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27
Q

powder

A

dry, bulk solid material consisting of very fine particles

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28
Q

medicated powders

A

intimate mixtures of dry, finely divided drugs and or chemical that may be intended for internal or external use

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29
Q

granule

A

any conglomeration of discrete particles; normally multi-component agglomerates consisting of API and excipient particles that have been bound together to enable manufacturing, handling, or administration

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30
Q

What are powders and granules commonly used in?

A

Tablets, hard gelatin capsules, topical, pulmonary, and suspensions

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31
Q

Powders and granules for reconstitution can’t be marketed or stored as ?

A

a liquid product

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32
Q

Degradation kinetics in solution/suspension forms are what compared to solids?

A

much faster

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33
Q

What often participates in degradation?

A

Liquid vehicle used in reconstitution

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34
Q

Who is the target populations for reconstitution?

A

Pediatrics

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35
Q

When is reconstitution prepared by pharmacists?

A

Rx medications
parenteral and peroral medication
multi-dose solutions or suspensions

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36
Q

When reconstitution is performed by patients?

A

non Rx medications
per oral medications
single dose suspensions/solutions

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37
Q

Dispensing

A

defined masses of API and excipients are weighed according to formulation

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38
Q

Comminution

A

homogenization of particle size and particle size distribution to improve flow and mixing properties

compounding scale: trituration
industrial scale: milling

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39
Q

Blending

A

dry powders blended to homogeneity; content uniformity measured to ensure reproducible dosing

compounding scale: blending/co-trituration

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40
Q

Glidants

A

improve flow properties of poorly flowing powders, to help enable homogenous mixing

tends to consist of colloidal or ultra fine particles

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41
Q

What do glidants reduce?

A

adhesion and friction between blend components

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42
Q

Colloidal Silicon Dioxide

A

Cab-o-sil, Aerosil, colloidal silica
colloidal, spherical particles
diameter < 1 um
hydrophobic
glidant

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43
Q

Talc

A

Altalc, Luzenac Pharma, hydrous magnesium silicate
ultra fine/very fine, regularly shaped particles
diameter 10-70 um
hydrophobic
glidant

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44
Q

Corn Starch

A

ultra fine, spherical particles
diameter 2-20um
hygroscopic
glidant

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45
Q

Granulation

A

powder blends are agglomerated into aggregate particles usually consisting of API & excipients
aggregates are held together by binders

compounding scale: wet massing
industrial scale: wet granulation

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46
Q

Drying

A

granulating liquid is evaporated; binder dries and hardens resulting in coarse dry particles

compounding scale: tray drying
industrial scale: fluid bed drying

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47
Q

Sizing

A

dried particles are passed through a screen to break any clumps that may have formed during drying

compounding scale: sieving

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48
Q

Wet Granulation

A

powder blend mixed by high RPM blades
granulating solution added until wet mass reaches desired consistency

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49
Q

Fluid bed drying

A

wet mass transferred to dryer
warm air blown through wet mass; granultating liquid evaporated and removed

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50
Q

Binders

A

polymeric materials as part of the powder blend or introduced via granulation solution
becomes viscous when introduced to water

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51
Q

Hydroxypropylmethylcellulose

A

Hypromellose, HPMC
can be used as a binder in either wet granulation or dry granulation
used as a film-coating polymer and an extended release polymer

52
Q

polyvinylpyrolidone

A

povidone, kollidon, plasdone, PVP
introduced as a binder solution during wet granulation

53
Q

hydroxypropylcellulose

A

Klucel, HPC
used as a binder in wet granulation
commonly used as film polymer

54
Q

Acacia

A

acacia gum, gum arabic
used as a binder in wet granulation
used as an extended release polymer

55
Q

pregelatinized starch

A

prejel, pharma-gel, lycatab PGS
used as a binder in wet granulation
introduced as a dry component, activated when granulated with water

56
Q

solid oral dosage forms

A

contain single discrete dose of API, allowing accurate convenient dosing
most common type of dosage form dispensed in pharmacies

57
Q

Advantages of solid oral dosage forms

A

inexpensive cost to patients/manufacturers
patient compliance/adherence is great
no medical/professional intervention
simple to take correctly
taste/smell/odor masking
fewer special storage instructions
more chemically and physically stable
stop effects of medication by inducing vomiting
sometimes crush/chew or open/empty to aid swallowing
formulate specific delivery profiles

58
Q

Disadvantages of solid oral dosage forms

A

sometimes crush/chew or open/empty
slower onset of action (especially relative to parenterals)
swallowing may be difficult/impossible for certain populations/circumstances
could be variable absorption, 1st pass metabolism
compression properties of API may be limiting
manufacturing process is less conducive to compounding

59
Q

Aesthetic coating

A

dissolve on contact with GI fluid; product identification and branding

60
Q

Barrier Coating

A

dissolve on contact with GI fluid; protects tablet core contents from de-stabilizing influence

61
Q

Functional coating

A

prolongs drug release from core in some controlled fashion; may dissolve, partially dissolve, gel or remain intact

62
Q

Coating solutions/suspensions are xxx components of a tablet

A

formulated

63
Q

How are film coats applied?

A

by spraying a solution or suspension onto core surfaces, which dries to form solid film layer

64
Q

Water soluble film-forming polymers

A

Hypromellose, Methylcellulose, Povidone, hydroxyethyl cellulose, gelatin

65
Q

water insoluble film forming polymer

A

ethylcellulose, methacrylic polymers

66
Q

enteric film forming polymer

A

hydroxypropylmethylcellulose phthalate, cellulose acetate phthalate, polyvinyl acetate phthalate, methacrylic polymers

67
Q

Titatnium dioxide is an

A

opacifier

68
Q

Propylene glycol, polyethylene glycol, glycerol are all examples of

A

plasticizers

69
Q

FD&C pigments/dyes are

A

colorants

70
Q

What are some examples of tablet classification?

A

Route of Admin
Manufacturing Method
Delivery Technology
Coating type
dimensions

71
Q

Hard gelatin capsules anatomy

A

cap
tapered rim
body
locking grove

72
Q

tablet anatomy

A

face
band
land
film coating

73
Q

Hard gelatin capsules enclosure formulation

A

gelatin (animal collagen-derived)
hydroxypropylmethylcellulose

74
Q

Soft gelatin capsule enclosure formulation

A

gelatin (animal collagen-derived)
hydroxypropylated starch, l-carrageenan

75
Q

shell material has a sol-gel temperature of approximately?

A

37 degrees C

76
Q

At room temperature, the shell polymer is

A

a solid

77
Q

At body temperature, the shell polymer quickly

A

liquifies, dissolves into GI fluid

78
Q

Hard gelatin capsules contain how much additional plasticizer?

A

13-16%

79
Q

soft gelatin capsules contain how much additional plasticizer?

A

5-8%

80
Q

Hard gelatin capsule fill types

A

powder/granulate - typically IR
pellet mixture - typically XR
paste
capsule
tablet

81
Q

soft gelatin capsule fill types

A

solution
suspension
powder

82
Q

The larger the hard gelatin capsule the smaller the?

A

volume

83
Q

Shapes of soft gelatin capsules

A

ovoid, ovule
capsule, barrel, elongated
spheroid, spherule

84
Q

antioxidant

A

used to minimize/slow api/excipient degradation by oxidation

85
Q

surfactant/wetting agent

A

used in solid oral dosage forms where API/excipients are hydrophobic; helps dosage form interact with aqueous fluids

86
Q

antimicrobial preservative

A

used in solid oral dosage forms when microbial growth is problematic

87
Q

diluent

A

provides bulk weight to core/fill materials; should be free-flowing powder
examples: sucrose and mannitol

88
Q

Lactose

A

lactose monohydrate, lactose anhydrous, spray-dried lactose
diluent
water soluble
very compressible

89
Q

Microcrystalline Cellulose

A

MCC, Avicenna
diluent
very compressible
absorbs water and swells

90
Q

Calcium phosphate

A

Di-Tab, A-Tab, Tri-Tab, emcompress
diluent
very compressible
inorganic excipient

91
Q

disintegrant

A

imbibes water from GI fluid and swells
swelling disrupts mechanical bonds
examples: potato starch and starch

92
Q

Sodium starch glycolate

A

explotab, explosol, primojel, carboxymethyl starch
disintegrant

93
Q

Crospovidone

A

cross-linked polyvinylpyrroloidone, polypasdone
disintegrant

94
Q

Croscarmellose Sodium

A

Ac-Di-Sol, carboxymethylcellulose sodium
disintegrant

95
Q

Tablet making process

A
  1. specified weight of powders/granules filled into a die
  2. tons of applied pressure deforms particles in die
  3. table core ejected from die, maintains shape imposed during compression
96
Q

Why does the tablet core maintain shape after it is ejected?

A

the formation of inter-particulate non bonded interactions

97
Q

What does tooling determine?

A

The size and shape of the tablet

98
Q

Rectification

A

on compounding scale
empty shells placed in a frame; oriented so that caps and bodies are all in the same direction

99
Q

Separation

A

on the compounding scale
oriented caps and bodies are separated from one another

100
Q

Filling

A

on the compounding scale
fill material spread over feed-frame; consistent volume of powder/granulate added to each individual body

101
Q

Repositioning

A

on compounding scale
caps secured on filled bodies; filled capsules ejected from frame

102
Q

Capsule outputs

A

compounding scale: 100-1000s of capsules per hour
industrial scale: 40,000-175,000 capsules per hour

103
Q

Which is the more efficient process: tablets or capsules?

A

tablets

104
Q

lubricant (boundary)

A

reduces friction between formulation components and manufacturing equipment; prevents materials from sticking to equipment

105
Q

Magnesium sterate

A

lubricant
water insoluble
very small colloidal particles coat larger formulation particles
molecular structure of aliphatic tails helps absorb mechanical energy

106
Q

What are some examples of insoluble lubricants?

A

magnesium stearate
stearic acid
glyceryl behenate

107
Q

What is an example of a soluble lubricant?

A

Polyethylene glycol

108
Q

Powder consolidation occurs during tableting and powder xxx occurs during encapsulation

A

tamping

109
Q

Drug delivery

A

dissolution of api molecules into a physiological fluid

110
Q

In conventional PO admin products are swallowed whole and the drug dissolves?

A

in the stomach

111
Q

PO formulations may dissolve in the small intestines following?

A

rapid gastric emptying or gastric bypass surgery

112
Q

immediate release

A

solid oral dosage forms designed to release the majority of API via dissolution into the GI fluid within 30 minutes

113
Q

Immediate release tablets

A

may not have film coat layer
if film coated its dissolution is rapid
aims to dissolve the majority of API into solution in <30 min

114
Q

IR tablet delivery

A
  1. rapid dissolution of water soluble film coating
  2. consolidate composite disintegrates into aggregate particles
  3. de-aggregation occurs, results in primary particles
  4. dissolution occurs
  5. ADME processes
115
Q

IR delivery from hard gelatin capsules

A
  1. Dissolution of gelatin

2a. Slug or granules/pellets disintegrate into aggregate particles
2b primary particles dissolve and ADME processes occur

3a. Deaggregation occurs and primary particles dissolve, ADME processes occur

116
Q

IR Soft gelatin capsule solution fill delivery

A

miscible base mixes with GI fluid and ADME processes occur

117
Q

IR soft gelatin capsule suspension fill

A
  1. miscible base mixes with GI fluid
  2. primary particles dissolve
  3. ADME processes occur
118
Q

Dissolution

A

kinetic process by which API molecules dissolve out of solid particles at a rate initially proportional to their saturation solubility in the aqueous GI fluid

119
Q

(dC/dt) = (DACs)/(Vh)

A

Noyes-Whitney equation
attempt to model initial dissolution rate; how fast molecules dissolve out of a particle
C = concentration delivered
D = diffusivity in water
A = surface are of particles
Cs = saturation solubility in GI fluid
V = volume of GI fluid (250mL)
h = width of static diffusion layer

120
Q

h is inversely proportional to ?

A

the dissolution rate

121
Q

(dWs/dt)= - (DA/h)(Cs-(Wd/V))

A

Nernst-Bruner Equation
initial dissolution rate
Ws = mass remaining in solid
Wd= mass delivered over time
D = diffusivity in water
A = surface area of particles
Cs = saturation solubility in GI fluid
V = volume of GI fluid
h = width of static diffusion layer

122
Q

Initial dissolution rate assumes that change in particle radius is ?

A

negligible

123
Q

Trituration affects the initial surface area of particles, so therefore it will influence?

A

dC/dt

124
Q

When the number of particles remains constant, dissolution causes ?

A

a decrease in surface area

125
Q

(Ws/W0)^(1/3) = 1 - (DCst/phr0)

A

Hixson-Crowell Cube Root Dissolution model
delivery from monodisperse spherical particles whose radius changes over time

Ws = mass remaining in solid at time t
W0 = initial mass in the solid at time t=0
D = diffusivity in water
Cs = saturation solubility in GI fluid
p = density of the solid
h = width of static diffusion layer
r0 = particle radius

Pharmaceutics 2 (6 decks)

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