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PHRM 828 > Exam 3 > Flashcards

Exam 3 Flashcards

1
Q

Which administration routes make up about 90% of them?

A

oral, pulmonary, transdermal, parenteral

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2
Q

What are the advantages of tablets and capsules?

A
  • stability
  • accurate dose
  • patient compliance
  • low cost
  • additional functions such as taste masking or controlled release
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3
Q

What are the disadvantages for tablets and capsules?

A
  • not suitable for infants and children
  • not suitable for non-oral medications
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4
Q

What are the advantages to IV solution?

A
  • fast drug action
  • suitable for drugs that can’t tolerate GI tract environment
  • suitable for patients who are unable to swallow tablets or capsules
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5
Q

What are the disadvantages to IV solution?

A
  • expensive
  • not convenient
  • pain
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6
Q

What are transdermal patches good for?

A

local treatment

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7
Q

What kind of drug do transdermal patches require?

A

potent

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8
Q

What are the advantages to intranasal sprays?

A
  • mostly used for local treatment
  • can also be used for systemic drug delivery
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9
Q

What are the factors that dictate route of administration?

A
  • disease state treated
  • convenience to patients
  • marketing
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10
Q

List the types of solid dosage forms.

A

tablets, gelcaps, loose powders, lyophilized powders, controlled-release matrices

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11
Q

What makes liqui-gels different?

A
  • the drug is pre-dissolved
  • drug will still precipitate in stomach
  • has to re-dissolve
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12
Q

What are the two types of tablets?

A

compression, molded

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13
Q

Describe compression tablets

A
  • dominant
  • formed by compression
  • may or may not have coating
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14
Q

How are molded tablets formed?

A

melting

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15
Q

What does the multicoat of a sugar-coated tablet contain?

A

starch, calcium carbonate

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16
Q

What percent weight does a sugar-coating add?

A

50%

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17
Q

What percent weight does a film-coated tablet add?

A

2-6%

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18
Q

What are the advantages to sugar-coated tablets?

A
  • taste masking and/or identification
  • might enhance stability from oxidation
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19
Q

What are the advantages of film-coated tablets?

A
  • can avoid using moisture/water
  • put marking on tablets
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20
Q

Describe multiple compression tablets

A
  • have inner core and coating
  • inner core could be sugar tablet
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21
Q

Describe multiple layer tablets

A
  • lightly compress one layer
  • additional layers added
  • can put additional layers if needed to separate drugs
  • can be used for multiple types of release
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22
Q

Characteristics of enteric-coated tablets

A
  • resist dissolving in stomach
  • dissolve at higher pH
  • used for drugs that can irritate the stomach
  • cannot be crushed or chewed
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23
Q

What are 3 examples of enteric-coated tablets?

A

aspirin, omeprazole, sulfasalazine

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24
Q

Describe chewable tablets

A
  • large tablets designed to be chewed before being swallowed
  • may not need water
  • may help solubility
  • avoids swallowing issues
  • no disintegrant
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25
Q

What are the common fillers for chewable tablets?

A

sorbitol, mannitol

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26
Q

What is an example of a chewable tablet?

A

singulair (montelukast)

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27
Q

How are effervescent tablets administered?

A
  • dissolved in glass of water prior to administration
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28
Q

What is the benefit of effervescent tablets releasing carbon dioxide?

A
  • aids in disintegration/dissolution
  • creates a buffered solution with high pH
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29
Q

What are the benefits to the fast action of effervescent tablets?

A
  • faster bioavailability
  • less gastric irritation
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30
Q

What do effervescent tablets need to be protected from?

A

moisture

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31
Q

What type of capsule is commonly used for compounding?

A

hard gelatin

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32
Q

What are hard and soft gelatin capsules made out of?

A

collagen

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33
Q

Which kind of capsule uses two ribbons for manufacturing?

A

soft gelatin

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34
Q

What are the characteristics of solution?

A
  • faster to act
  • less stable
  • more for parenteral administration
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35
Q

What are the characteristics of solid state?

A
  • slower to act
  • more stable
  • more convenient
  • common for oral admin
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36
Q

preformulation

A

determining the physicochemical properties necessary to formulate the compound

37
Q

formulation

A

determining the route and composition of the final dosage form

38
Q

Most organics have a relatively low solubility, unless they are ________.

A

salts

39
Q

What are the three states of solubility?

A

completely soluble, supersaturated, very supersaturated (labile)

40
Q

What will high levels of supersaturation result it?

A

crystallization

41
Q

Which is more reactive: crystal lattice or amorphous?

A

amorphous

42
Q

What are reactions dictated by?

A

availability of reactant

43
Q

Why can’t you administer only the drug substance?

A
  • unstable
  • needs taste masking
  • hard to administer
44
Q

What are some of the roles of excipients?

A
  • preservative
  • solubility enhancer
  • stability enhancer
  • taste masking
45
Q

List the types of excipients

A

diluents, disintegrants, binders, lubricants, glidants, controlled release

46
Q

diluents

A
  • referred to as bulking agents
  • needed to make practical weight for tablet
  • compression aid
  • enhances powder flow for manufacturing
47
Q

Examples of diluents

A
  • microcrystalline cellulose, lactose, calcium phosphate dibasic dihydrate, starch, compressible sugar
48
Q

Disintegrants

A
  • breaks up solid dosage forms, enhancing dissolution
  • works by either water uptake and/or swelling
49
Q

disintegrant examples

A

sodium starch glycolate, croscarmellose sodium, crospovidone, starch

50
Q

binders

A
  • give tablets mechanical strength, creates granules in wet milling
  • works by either water uptake and/or swelling
51
Q

binder examples

A

polyvinylpyrrolidone, starch, mircrocrystalline cellulose, polymers

52
Q

lubricants

A
  • prevents adherence of tablet to the die after compaction
  • overlubrication can affect dissolution
  • used at levels of 0.5% - 2%
53
Q

lubricant examples

A

magnesium stearate (most common), stearic acid, lubritab, talc

54
Q

glidants

A
  • improves powder flow
  • stops inter-particle friction
  • used at levels of <0.2%
  • low bulk density – fluffy
  • can have problems with asbestos (talc)
55
Q

gildants examples

A

fumed silica, talc

56
Q

controlled release

A

used to extend the release of drug from a matrix

57
Q

controlled release example

A

HPMC, hyromellose, xantham gum

58
Q

Roles of coloring agents

A
  • improves esthetics
  • identification to user
  • control product
  • help in case of poisoning
59
Q

What properties do we need to know while formulating a dosage form?

A
  • physical and chemical properties
  • mechanical properties
  • biopharmaceutical properties
60
Q

A drug needs to be _________

A

stable, bioavailable, deliverable

61
Q

Aqueous solubility

A
  • concentration at which the solution is in equilibrium with the solid phase
  • depends on temp, pressure
  • key to bioavailability
62
Q

dissolution rate

A
  • determines how quickly it goes into solution
  • might be enhanced by fast-dissolving tablets
  • important for in vivo- in vitro correlation
  • measured using simulated gastric fluid
63
Q

ionization constant

A
  • affects dissolution, membrane partition, complexation, chemical stability, absorption
  • protonated or non-protonated
64
Q

polymorphism

A
  • molecules may have multiple crystalline forms
65
Q

amorphous

A
  • lack of long-range order
  • usually has higher solubility than crystalline form of drug
  • unstable - wants to crystallize
  • enhanced bioavailability – good for poorly-soluble drugs
66
Q

hydroscopicity

A
  • amount of water taken up by solid
  • significantly affects stability and manufacturability
  • water uptake can be used to measure surface area and disordered/high energy sites
67
Q

types of deformation

A

elastic, plastic, brittle fracture

68
Q

elastic

A

material deforms and then returns to equilibrium – reversible

69
Q

plastic

A

material deforms beyond elastic deformation – irreversible

70
Q

brittle fracture

A

material breaks into smaller fragments

71
Q

Goal of manufacturing

A

take API and turn it into a dosage form that is stable, soluble, and easy to administer

72
Q

unit operations

A

weighing, blending/mixing, milling, granulation, drying, compaction (tableting), coating, packaging

73
Q

modified release

A

one in which the time course, location of drug release, or both, are altered to accomplish therapeutic objectives not achieved by conventional dosage forms

74
Q

zero-order

A

releases drug at a constant and known rate

75
Q

variable release

A

releases drug at a variable rates so as to match circadian rhythms

  • useful when changes in blood concentrations are necessary
76
Q

bio-responsive

A

drug release triggered by a change in biological stimulus such as pH, temperature, or concentration of some disease marker

77
Q

Which modified release systems are practical?

A

delayed-release, extended-release

78
Q

delayed-release delivery system

A

one that releases a drug all at once but at a time other than promptly after administration – often bioresponsive

79
Q

extended-release delivery system

A

achieves slow release over extended period of time

80
Q

What are two reasons to employ delayed-release?

A
  • avoid release in stomach
  • chronotherapy
81
Q

chronotherapy

A

timing of drug release to be in harmony with biological rhythm of a disease

82
Q

What strategies can be used to avoid stomach pH?

A
  • change the pH
  • avoid dissolution in stomach
83
Q

What size of doses have greater variation in peaks and valleys?

A

high dose

84
Q

How do you achieve constant blood level?

A

zero order

85
Q

reservoir device

A

core of drug surrounded by a poorly water-soluble polymeric membrane

  • diffusion of drug through membrane is rate-limiting step.
86
Q

matrix device

A

dissolved or dispersed drug is uniformly throughout a polymer matrix

  • diffusion through the matrix is rate-limiting step
87
Q

flux

A

mass of drug that moves through a membrane per unit time

  • Fick’s law
88
Q

How are zero-order release kinetics attained?

A
  • excess solid encapsulated makes this possible
  • C1 high and constant
  • C2 low and constant
  • all other factors constant, so Flux must be constant

PHRM 828 (2 decks)

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