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Ceutics > Exam 1 Definitions and Concepts 1-4 > Flashcards

Exam 1 Definitions and Concepts 1-4 Flashcards

1
Q

pharmaceutics

A
  • discipline of pharmacy that deals with the science of dosage form design and the process of turning a new chemical entity into a medication that can be safely and effectively used
  • art and applied science
  • interface between drug and body
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2
Q

pharmacodynamics

A

drug action and mechanism on the body

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3
Q

pharmacokinetics

A

body acting on the drug
absorption, distribution, metabolism, excretion

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4
Q

absorption

A

variety when people have health issues, oral vs. IV injection

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5
Q

distribution

A

benign cancer local vs malignant cancer being in many sites

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6
Q

metabolism

A

all food and drugs undergo it
*liver
*prodrugs

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7
Q

excretion

A

removal from body, may want to extend time
*kidney

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8
Q

chemical

A

a substance composed of chemical elements

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9
Q

drug

A
  • substance recognzied by an official pharmacopoeia or formulary
  • substance intended for the use in diagnosis, cure, mitigation, treatment, or prevention of disease
  • intended to affect the structure or any function of the body
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10
Q

drug product

A

finished dosage form that contains a drug substance, generally, but not necessarily in association with other active or inactive ingredients

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11
Q

dosage form

A

physical form in which a drug is produced and dispensed

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12
Q

active ingredient

A
  • component intended to furnish pharmacological activity or other direct effect in the diagnosis, cure, mitigation, treatment, or prevention of disease
  • affects the structure or any function of the body
  • causes medication’s desired effect
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13
Q

inactive/inert ingredient

A

any component of a drug product other than active ingredient
*dyes, preservatives, and flavoring agents

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14
Q

brand drug

A

when the FDA approves a drug for the first time, there is only one manufacturer that makes and sells a drug

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15
Q

generic drug

A

produced after the brand name drug’s patent has expired, also must be approved by the FDA

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16
Q

over the counter drugs

A

can be dispensed without a prescription

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17
Q

prescription/legend drug

A

can only be dispensed with prescription from a licensed HCP

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18
Q

ex. estrogen

A

for: hormone replacement therapy for treatment of symptoms of menopause
molecules administered: conjugated estrogens, estradiol, estrone
dosage forms: tablets, transdermal patch, transdermal gel, vaginal ring

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19
Q

tablet

A
  • compressed contains micronized estradiol
  • micronization to improve dissolution
  • may have high first pass effect
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20
Q

transdermal patch

A
  • bypasses first-pass metabolism
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21
Q

vaginal ring

A
  • topical application for local symptoms
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22
Q

dosage forms for safe and convenient delivery of accurate dosage

A

tablet, capsule syrup

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23
Q

dosage forms that protect a drug from chemical degradation, usually due to atmospheric oxygen or humidity (increase shelf life)

A

coated tablets, sealed ampoules

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24
Q

dosage forms that provide protection of drug form influence of gastric acid and saliva after oral administration

A

enteric coated tablets

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25
Q

dosage forms that mask taste of expensive drugs

A

capsules, coated tablets, flavored syrups

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26
Q

dosage forms that provide liquid preparation, even for drugs that are either insoluble or unstable

A

syrups, suspensions

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27
Q

dosage forms that provide injectable dosage forms with the correct composition (tonicity and pH) for compatibility with surrounding tissue

A

injections
*sterility and stability

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28
Q

dosage forms that provide slow or targeted release of drug

A

implants

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29
Q

dosage forms that provide optimal topical administration

A

creams, ointments, ophthalmic, ear, nasal

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30
Q

dosage forms that provide the optimal characteristics for the insertion of a drug into one of the body’s orifices

A

rectal and vaginal suppositories

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31
Q

dosage forms that provide the requirements for inhalation of drugs to the lung

A

inhalants

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32
Q

classes of pharmaceutical dosage forms, according to the overall physical properties of dosage froms

A

gaseous
liquid
semisolid
solid

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33
Q

gaseous dosage froms

A

medicinal gases
aerodispersions

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34
Q

medicinal gases

A

inhalation/volatile anesthetics (vaporized before admin by inhalation)

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35
Q

aerodispersions

A

solid particles or liquid particles

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36
Q

liquid dosage forms

A

solutions
emulsions
suspensions

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37
Q

solutions

A

prepared by dissolving one or more solutes in a solvent
*very small particle size

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38
Q

emulsions

A

a dispersion system consisting of 2 immiscible liquids
*oil in water or water in oil

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39
Q

suspensions

A

dispersion system where solid particles are dispersed in liquid phase
*larger particle size
*not intended for systemic admin of drugs with high potency

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40
Q

semi solids

A

gels
creams
ointments
pastes
*unshaped

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41
Q

gels

A

semisolid system in which a liquid phase is contained within a 3D cross-linked matrix

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42
Q

creams

A

semisolid emulsion systems (O/W, W/O), >10% of water
- O/W creams are more comfortable and cosmetically acceptable as they are less greasy and more water washable
- W/O creams accommodate and release better lipophilic API, moisturizing, cold creams

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43
Q

ointments

A

semisolid dosage forms with the oleaginous (hydrocarbon), water-soluble or emulsifying base
*oleaginous base- petrolatum (Vaseline)
*water soluble base- PEG

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44
Q

pastes

A

semisolid dispersion system, where solid particles are dispersed in ointments
*mostly oleaginous

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45
Q

shaped semi solids

A

suppositories (rectal)
*diff shapes
*melt/dissolve at body temp
*oleaginous (cacao butter, adeps neutralis) or aqueous (PEGs, glycerinated gelatine)
pessaries (vaginal)
*similar as above
*PEGs or glycerinated gelatine are often used as base

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46
Q

solid dosage forms

A

unshaped- powders
shaped- tablets, capsules, implants, transdermal patches

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47
Q

systemic admin

A

PO
sublingual and buccal
rectal
parenteral
transdermal
inhallation

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48
Q

local admin

A

topical on skin or mucosa (eye, nose, ear, mouth, vagina, rectum, bronchi, skin)
local pareneral

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49
Q

generations of dosage forms

A

1st gen- immediate release of API
2nd gen- controlled release of API (CR)
3rd gen- targeted distribution of drug delivery systems

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50
Q

1st gen dosage forms

A
  • disintegration of dosage form and dissolution of API is spontaneous
  • absorption and distribution is based only on physiochemical properties of API
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51
Q

2nd gen dosage forms

A
  • release of API is under control of drug delivery system (temporal control)
  • advantages: avoids fluctuations of plasma drug conc for safety and efficacy, decreased frequency of drug admin for better compliance, may overcome some problems with BAV, can be more economical
    -SR- release of initial API and futher prolonged release
    -CR- properly controlled release of API
  • pulsatile release- think diabetes devices
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52
Q

targeted drug delivery

A

drug delivery system provides altered PK profile, targeting drug to particular organ/tissue
*improved selectivity of action
*can overcome unfavorable PK properties
*improved efficacy
*improved tolerability/decreased toxicity

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53
Q

passive targeting

A

passive accumulation of drug at site of pathology due to the leaky vasculature and poor venous/lymphatic drainage, solid tumors draw more blood and may have larger pores

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54
Q

active targeting

A

drug delivery system with specific ligand with high affinity to receptor exposed selectively on the target cells

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55
Q

possible inert ingredients

A

anti-adherents
binders
coatings (change dissolution rates)
disintegrants
fillers/diluents
flavors and colors
glidants and lubricants (prevent aggregation)
preservatives
sorbents (so can be ok with some moisture)
sweeteners

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56
Q

cost to get one new medicine onto the market

A

$500-800 million

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57
Q

how many years to make a drug

A

12-15

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58
Q

how many out of 5,000 that enter preclinical testing make it to human testing

A

5

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59
Q

preclinical phase

A

research and development

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60
Q

clinical phase

A

also research and development, includes phases 1-3

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61
Q

postmarketing

A

surveillance, adverse reaction reporting, survey sampling, inspections

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62
Q

thermodynamics

A

describes the changes in the form of energy when a reaction occurs
*ex. converting chemical energy to heat
*will the reaction occur or not? feasible with stable product
*Ea (activation energy)

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63
Q

kinetics

A

describes the speed at which a reaction occurs
*rate and mechanism of action
*state functions (delta G, H, S,E)

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64
Q

first law of thermodynamics

A

energy is conserved, it can be neither created nor destroyed

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65
Q

second law

A

in an isolated system, natural processes are spontaneous when they lead to an increase in disorder, or entropy

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66
Q

third law of thermodynamics

A

the entropy of a perfect crystal is zero when the temperature of the crystal is equal to absolute zero

67
Q

steady state

A

state in which the concentration, pH, etc. do not change with time

68
Q

equilibrium

A

describes a state in which the concentrations of reactants and products do not change with time
*reactions occurring at same rate in forward and reverse

69
Q

pharmaceutical equilibrium

A

solubility, pH, complexation, protein binding, partition equilibria

70
Q

state of the system

A

can be completely described by specifying four thermodynamic variables
*composition, temperature, pressure, and volume
BUT if system is homogenous only need 3 (no composition)

71
Q

equation of state

A

relationship between P,V, and T

72
Q

open system

A

a system in which both energy and matter can leave

73
Q

closed system

A

a system in which matter is not exchanged with the surroundings

74
Q

isolated system

A

a system in which neither matter nor energy is exchanged with the surroundings

75
Q

isothermal process

A

a process that occurs with no exchange of heat

76
Q

adiabatic process

A

a process that occurs with no exchange of heat

77
Q

intensive property

A

a property of a system that does not depend on the size of the system, for example, temperature and density
*temperature, color, hardness, melting/boiling point, pressure, concentration

78
Q

extensive property

A

a property of a system that does depend on the size of the system, volume for example
*mass, volume, length

79
Q

internal energy (E)

A

the sum of the kinetic and potential energies

80
Q

kinetic molecular theory

A

temperature of an ideal gas is directly proportional to the average kinetic energy of its molecules

81
Q

internal energy of an ideal gas is directly proportional to

A

the temperature of the gas

82
Q

enthalpy

A

heat

83
Q

at constant pressure, change in Esys=

A

change in H

84
Q

the heat given off or absorbed when a reaction is run at constant volume is equal to

A

the change in the internal energy of the system
*change in Esys=qv (constant volume)

85
Q

the heat given off or absorbed when a reaction is run at constant pressure is equal to

A

the change in the enthalpy of the system
*change in Hsys=qp (constant pressure)

86
Q

the difference between delta E and delta H is _ for reactions in condensed phases (liquids and solids)

A

negligible
*because there is little if any change in the volume of the system during the reaction

87
Q

to change the internal energy of a system must be accompanied by

A

transferring either heat or work to its surroundings

88
Q

exothermic _ heat

A

gives off

89
Q

are their spontaneous reactions that absorb energy?

A

yes- water boils spontaneously even though rxn is endothermic

90
Q

change in Ssys > 0 implies that the system becomes _ disordered during the reaction

A

less

91
Q

volume changes, temperature changes, phase transitions, and mixing components all lead to

A

a change in disorder

92
Q

number of microstates

A

our ability to know exactly where each molecule is

93
Q

at a phase change _ changes abruptly

A

entropy

94
Q

standard state conditions

A

standard pressure = 1 bar
standard temperature = 25 degrees C
solutions 1 molar
1 mole of a gas
liquids and solids in pure state

95
Q

standard-state entropy of reaction

A

when change in entropy is measured under standard-state conditions

96
Q

enthalpy

A

H, heat gained by the system

97
Q

entropy

A

S, change in the disorder of a system

98
Q

spontaneous reactions must _ or _

A

give off energy in the form of heat, lead to an increase in disorder

99
Q

Gibbs’s free energy

A

combines contributions of enthalpy and entropy to define the spontaneity of a process
*state function (in terms of thermodynamic properties that are state functions)

100
Q

magnitude of delta G standard tells us

A

how far standard state is from equilibrium

101
Q

equilibrium constants change with

A

temperature
&Van’t Hoff

102
Q

solubility

A

amount of solute that can be completely dissolved in solvent at a well defined temperature

103
Q

driving forces of solubility

A

Van der Waals
ionic bonds
covalent bonds
H bonds
dipole dipole interactions

104
Q

2 types of H bonds

A

intramolecular- H bonds within itself
intermolecular- H bonds between separate molecules

105
Q

to increase solubility

A

increase temperature
increase surface area (crush)
increase pressure
change pH
add cosolvent
agitation of solution

106
Q

alcohols

A

always ethyl alcohol

107
Q

alcohol content allowed

A

peds (<6 years)- 0.5% w/v
6-12- 5% w/v
12+- 10% w/v

108
Q

alcohol content allowed

A

<6 years- 0.5% w/v
6-12 years- 5% w/v
12+- 10% w/v

109
Q

diluted alcohols

A

alcohol with 50% water and 50% ethanol
*100mL combines becomes 97mL because of H bonding

110
Q

rubbing alcohols

A

70% of ethyl alcohol w/v

111
Q

pharmaceutical waters

A

purified by distillation, ion exchange
*removing ions for higher purity
but if for injectables and ophthalmic formulations must be purified and sterile (no ions or bacteria)

112
Q

cosolvents

A

solvent systems besides water

113
Q

semi-aqueous solvents

A

syrups
tinctures
elixirs

114
Q

syrups

A

Syrup NF 85% (w/v) sucrose

115
Q

tinctures

A

higher alcoholic content than elixirs
used to extract natural products

116
Q

elixirs

A

slightly lower alcoholic content than tinctures
for making medicated syrups

117
Q

weight concentration

A

weight of solute in weight of solution

118
Q

molarity

A

moles / liter of solution
*can be used for non-ionic compounds that don’t dissociate

119
Q

normality

A

equivalents / liter of solution
*can be used for ionic compounds defined by dissociated ions used a lot for acids

120
Q

molality

A

moles / kg solvent

121
Q

mole fraction

A

moles of solute / total # moles

122
Q

solution properties are _ than the pure solvent or the solute

A

different

123
Q

colligative properties

A

properties of a liquid that may be altered by the presence of a solute
*depend only on the amount of solute in solution
*does not depend on the identify of the solute
*vapor pressure lowering, boiling point elevation, freezing point depression, osmotic pressure

124
Q

non-colligative properties

A

depends on the identity of the dissolved solute and the solvent
*taste, color, viscosity, surface tension, solubility

125
Q

osmotic pressure determines

A

the physiological acceptability of parenteral, ophthalmic, and nasal solutions

126
Q

vapor pressor of solution _ pure solvent

A

<

127
Q

effect on solute on vapor pressure

A

when a nonvolatile solute is dissolved in solvent, the vapor pressure of the resulting solution is lower than that of the pure solvent
*amount of vapor pressure lowering is proportional to the amount of solute and not its identity

128
Q

boiling point elevation

A

colligative property related to vapor pressure lowering, solution requires higher temp to reach its boiling point

129
Q

freezing point depression

A

disruption in the freezing process results in a depression of the freezing point for the solution relative to the pure solvent
*solute molecules disrupt the formation of crystals of the solvent
*colligative

130
Q

osmotic pressure

A

pressure caused by solutes

131
Q

isotonic

A

equal osmotic pressure

132
Q

crenation

A

shrinkage of RBCs in hypertonic solution

133
Q

hemolysis

A

burst of RBCs in hypotonic solutions

134
Q

Raoult’s law

A

vapor pressure of a solution equals the mole fraction of the solvent multiplied by the vapor pressure of the pure solvent
P1 = P0 x X1

135
Q

ideal solution

A

a solution that obeys Raoult’s law
* Ptotal = XaPa0 + XbPb0

136
Q

calculating mole fraction

A

A = nA / (nA + nB)

137
Q

Avogadro’s number

A

6.023 x 10^23

138
Q

non-ideal / real solutions

A

solutions that show a deviation from Raoult’s law
*may be positive or negative
*negative if solute is strongly held by solvent
*positive if solute and solvent are not tightly bound

139
Q

change in boiling point

A

boiling point of a solution made of a liquid solvent with a nonvolatile solute is greater than the boiling point of the pure solvent
*higher temp required

140
Q

van’t Hoff factor

A

i
number of dissociated moles of particles per mole of solute
*i=1 for non electrolytes, i= number of ions released for electrolytes
*as solution concentration increases the multiplier effect diminishes
*ion pairs begin to form, 2 oppositely charged ions stick together and act as a single particle

141
Q

change in freezing point

A

if there are impurities in a liquid, it is inherently less ordered
*a solution is more difficult to freeze than the pure solvent

142
Q

osmotic tablets

A

have a semipermeable membrane with laser-drilled hole, osmotically active core containing drug

143
Q

extensive effects on chemical potential

A

volume, enthalpy, free energy, entropy

144
Q

intensive effects on chemical potential

A

temperature, density, refractive index

145
Q

partial molar quantity

A

quantity denoting the rate of increase in the magnitude of an extensive property with an increase in the number of moles of a substance added to the system at constant temp and pressure

146
Q

chemical potential of a component

A

contribution of each mole of that component to the free energy of the system containing it (at constant T and P)

147
Q

when solid and liquid water exists in equilibrium, temperature is

A

0 degrees C

148
Q

the chemical potential of water in the liquid _ the chemical potential of ice

A

equals
*same with ointment on skin, solid in aqueous solution

149
Q

chemical potential relation to mole fraction

A

difference between chemical potential of a drug in solution and chemical potential of drug at standard state is a function of mole fraction
*u2 = u2o + RT lnx2 or lna2

150
Q

activity of a solute

A

a2
effective concentration that reflects not only the concentration, but also any interactions that cause deviations from ideality
*ratio of asolution/areference

151
Q

reference state

A

activity is 1
*for solvent it is pure liquid, if solid it is pure substance

152
Q

for saturated solutions, the chemical potential of drug in solution equals

A

the chemical potential of drug in the solid
*activities are equal

153
Q

Debye-Huckel theory

A

-logy = |z+||z-| x A sqrt(I)
*higher ionic strength reduces activity of electrolytes
*I = ionic strength
*activity coefficient of higher valence ions is affected more by addition ions

154
Q

solubility

A

the maximum amount of solute dissolved in a solvent at equilibrium

155
Q

supersaturated

A

a solution that contains more solute than the solvent can dissolve
* solid particles of solute may be present and solution phase will be in equilibrium with the solid

156
Q

dissolution rate

A

rate at which drug dissolves from its solid state
*higher solubility = more rapid rate of dissolution

157
Q

hydration

A

binding of water to solvent molecules
*solvation refers to solvent in general

158
Q

increasing chain length _ solubility, branching _ solubility

A

decreases, increases

159
Q

factors affecting solubility

A

nature of drug molecule
hydrophobicity
shape
surface area
state of ionization
influence of pH
pKa

160
Q

intrinsic solubility

A

concentration of unionized drug in equilibrium with solid drug

161
Q

measured/total solubility

A

total concentration of drug in all forms in equilibrium with solid drugs

162
Q

solubility depends on

A

-the lattice energy of the drug crystal (higher lattice energy, lower solubility)
-hydrophobicity of the drug molecule (higher log P = more hydrophobic)
and more

163
Q

miscibility

A

analogous to solubility for liquids in liquids
*may be complete or partial

Ceutics (2 decks)

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