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4200: Pharmaceutics > Solid State > Flashcards

Solid State Flashcards

1
Q

the design of a drug appropriate dosage form naturally depends on the _________ of the drug

A

physical properties

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2
Q

what are physical properties of a drug

A

the inherent characteristics of a substance that are dependent on its physical state

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3
Q

what is the primary property of a drug?

A

its physical state (solid, liquid, gas, ect)

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4
Q

is the physical state of a molecule an absolute property?

A

no, it is dependent upon the conditions under which it is placed

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5
Q

define physical change

A

when the form of a drug has changed, but the chemical properties are the same

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6
Q

what type of change is dissolution?

A

physical change

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7
Q

most pharmaceutical systems have _____ phases in _________

A

more than one phase, coexistence

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8
Q

what phases interact in suspension?

A

solid and liquid

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9
Q

what phases interact in emulsion?

A

liquid and liquid

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10
Q

what phases interact in tablets?

A

solid and solid

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11
Q

define component

A

chemically recognizable species in a system

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12
Q

what is a binary system?

A

a system that contains 2 component (ex. saline)

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13
Q

define phase

A

a homogenous, physically distinct portion of a system that is separated from the other portions by bounding surfaces; can contain one or more components

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14
Q

what is the term for a single phase system?

A

homogenous system (ex. solution)

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15
Q

what is the term for a system with 2 or more phases?

A

mixtures or heterogenous systems

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16
Q

how many phases and components do water and ethanol have?

A

1 phase

2 components

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17
Q

how many phases and components do water and ice have?

A

2 phases

1 component

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18
Q

how many phases and components do water and NaCl have?

A

1 phase

2 components

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19
Q

how many phases and components do water and oil have?

A

2 phases

2 components

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20
Q

precipitation is also known as _______

A

freezing

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21
Q

where does heat go when there is a solid to liquid phase change?

A

heat goes into the solid as it melts (phase change: melting)

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22
Q

where does heat go when there is a liquid to solid phase change

A

heat leaves the liquid as it freezes (phase change: freezing)

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23
Q

dissolving is also known as ________

A

melting

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24
Q

what type of dosage forms involve the vaporization process?

A

aerosols and inhalers

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25
Q

what process involved sublimation?

A

freeze drying (lyophilization)

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26
Q

what is the term for a phase change from gas to solids?

A

deposition

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27
Q

what is the term for a phase change from gas to liquid?

A

condensation

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28
Q

gas molecules have a _____ kinetic energy

A

high

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29
Q

gas molecules have _____ intermolecular forces

A

weak

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30
Q

what are drugs are commonly used in the gas phase?

A

volatile anesthetics; generally stored as liquids

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31
Q

liquid molecules have _____ kinetic energy than gas molecules

A

less

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32
Q

most pharmaceutical solvents exist in the ____ state

A

liquid

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33
Q

what state exhibits freezing and boiling points, vapor pressure, and surface tension?

34
Q

most drugs are ________ under ambient conditions

35
Q

what states exhibit compressibility, flow, dissolution rates, melting point, and particle size

36
Q

how does flow relate to solids

A

how to particle stick together (intermolecular forces)

37
Q

name the distinct physical properties that drugs in the solid form can impact

A
  1. bioavailability
  2. therapeutic efficacy
  3. stability of dosage form
38
Q

can a solid dosage form interconvert spontaneously?

A

yes, under certain condition (ex. bathroom) due to heat, cold, moisture, etc.

39
Q

define conformational polymorphism

A

> different crystalline forms as a result of conformation

>have different physical properties affecting bioavailability, therapeutic efficacy, and stability

40
Q

what are causes of polymorphism in the crystallization process?

A
  1. changes in equipment
  2. solvent changes
  3. temperature
  4. rate of cooling
  5. pressure
41
Q

define McCrone’s Law

A

every compound has different polymorphic forms, and in general the number of forms known for a given compound is proportional to the time and money spent in research on that compound infinite # of polymorphs)

42
Q

polymorphism can also change ________

A

crystal habit

43
Q

define monotropic

A

when only one polymorphic form is stable, and any other polymorph that is formed will eventually convert to the stable form

44
Q

metastable forms _____ to be stable for a period of time but will eventually _____

A

appear; convert to the true stable form (equilibrium)

45
Q

define enantropic

A

under different conditions, the material can reversibly transform between alternative stable forms (polymorphs)

46
Q

what properties differ between polymorphs?

A

apparent solubility, melting point, spectroscopic properties, dissolution rate, stability, hardness, compressibility, and density

47
Q

most stable polymorph is equal to ____ melting points is equal to _____ is equal to _____ dissolution rate

A

highest; strong; low

48
Q

due to polymorphism, drugs may require ______

A

special storage to prevent conversion

49
Q

in suspension, the interconversion of a ______ form to the ______ form can cause caking

A

metastable to stable

50
Q

the difference in concentration from the metastable form to the stable form acts as a driving force towards ________

A

crystallization of the stable form (apparent solubility)

51
Q

explain how cocoa butter relates to polymorphism

A

different heating and cooling temperatures and rates can create different polymorphs

52
Q

define solvate

A

when a stoichiometric amount of crystallization solvent molecules incorporate into the drug crystal lattice, satisfying all valence forces

53
Q

hydrate

A

same definition, but the solvent is water

54
Q

solvates ______ polymorphic forms of anhydrates

55
Q

polymorphs have _______ chemical composition

56
Q

define anhydrate

A

crystal that has had water of crystallization removed via heating

57
Q

how does the loss of water from a hydrate affect the crystal?

A

> formation of different crystal lattices (collapse and reform)
crystal lattice is unchanged (become void and unstable)
formation of amorphous material (collapses and never reforms)

58
Q

physical properties of a hydrate can differ from anhydrous form in an _______ as polymorphs

A 
analogous manner (NOT polymorphs)
>habit, hardness, density, melting point, stability, apparent solubility, dissolution rate
>ultimately impacts bioavailability
59
Q

define pseudo-polymorphic solvates

A

> solvent is trapped in the voids of the crystal lattice as an impurity (not a part of the crystal lattice)
greater apparent solubility and dissolution rate due to water molecules pushing the lattice apart (causes strain)

60
Q

how do psuedo-polymorphic solvates increase the apparent solubility?

A

solvent distorts the plane as an interstitial substitution, leading to stress on the crystal lattice

61
Q

define hygroscopicity

A

the uptake of water from the atmosphere

62
Q

define the 2 types of hygroscopicity

A
  1. absorption to form a hydrate (re-crystallization)

2. absorption without a major change in the lattice (surface water)

63
Q

define deliquescence

A

the uptake of sufficient water from the atmosphere to form a solutions

64
Q

define efflorescence

A

spontaneous loss of water molecules to form a lower hydrate or an anhydrate

65
Q

what is a possible cause of efflorescence

A

drastic drop in humidity (ex. moving from GA to AZ)

66
Q

define exsiccation

A

dehydration or partial dehydration produced by heat

67
Q

water adds ______ to a dosage form

68
Q

what are the concerns when dispensing moisture sensitive drugs

A

storage, vials, desiccants

69
Q

hygroscopic excipients

A

may absorb water and alter the physical state of the drug (starch)

70
Q

gelatin capsules contain ______ moisture

71
Q

describe a concern with granulation

A

water is added

72
Q

define co-crystal

A

> crystal composed of drug and other molecules (substitutional defect) (mixed crystal)
a solid where one solid is dissolved/dispersed in another solid

73
Q

what type of defect do co-crystals have?

A

substitutional defects

74
Q

what is considered a “solid solution”

A

co-crystal

75
Q

how many phases and components does a co-crystal have

A

1 phase

2 components

76
Q

define contact melting

A

mixtures of pharmaceutical solids will liquefy at a given temperature and composition

77
Q

define eutectics

A

contact melting; 2 solids interacting together to form a liquid

78
Q

define eutectic point

A

the lowest temperature in which a liquid phase can exist in a binary system

79
Q

explain what happen below the eutectic point

A

solid A and B crystallize out, forming a microcrystalline mixture that is distinct from crystalline A or B (intimate crystalline mixture)
>see slide

80
Q

define intimate crystalline mixture

A

structure below the eutectic point that is distinct from crystal A or B

81
Q

list the types of chemicals that form eutectics

A
  1. urea
  2. succinic acid
  3. aromatics (salon, thymol, camphor, menthol)
82
Q

physical state must be controlled if physical differences between forms have _________

A

biological significance

4200: Pharmaceutics (4 decks)

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