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WorksheetsCeutics - Exam 1 - Preformulation Part 2 - Yang
Total questions: 107
Worksheet time: 1hrs 2mins
What are the different factors of preformulation
solid state properties
solubility
hydroscopicity
lipophilicity
What is solubility
concentration of solute in a saturated solution at certain temperature
concentration of solute in an unsaturated solution at certain temperature
concentration of solute in a saturated solution at varying temperatures
opposites attract
like dissolves like
What are correct descriptions of solubility designations in USP
the higher the solubility range, the more soluble it is
the higher the solubility range, the less soluble it is
the lower the solubility range, the more soluble it is
the lower the solubility range, the less soluble it is
How to you convert micrograms to milligrams
1 mcg x 1000 = 1 mg
1 mg x 1000 = 1 mcg
1 mcg x 100 = 1 mg
1 mg x 100 = 1 mcg
1 mcg x 10,000 = 1 mg
If the aqueous solution has a solubility of < 100 mcg/mL, what does that indicate
soluble
insoluble
practically insoluble
What equation is this
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Solubility Prediction
Solubility and Particle Size
What is X2
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is Hf
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is R
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is T
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is T0
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What are the possible gas constants you can use for R
1.987 cal/mol
8.314 J/mol*K
8.314 x 107 erg/mol*K
8.314 x 107 dyn/cm
0.0821 L*atm/mol*K
What is the heat of fusion
4540 cal/mol
353.2 K
293 K
1.987 cal/mol
What is the temperature of measurement
4540 cal/mol
353.2 K
293 K
1.987 cal/mol
What is the melting point
4540 cal/mol
353.2 K
293 K
1.987 cal/mol
What is the gas constant
4540 cal/mol
353.2 K
293 K
1.987 cal/mol
What equation is this
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Solubility Prediction
Solubility and Particle Size
Which solute-solvent interactions involves compounds without a permanent dipole
Van der Waals Forces
Hydrogen Bonds
Electrostatic Force
Alpha-linkages
Which solute-solvent interactions results in permanent, positively charged dipole of a hydrogen atom (functional groups can be H-bond donors or acceptors)
Van der Waals Forces
Hydrogen Bonds
Electrostatic Force
Alpha-linkages
Which solute-solvent interactions occurs between two ions from induced dipoles (attractive force can be calculated)
Van der Waals Forces
Hydrogen Bonds
Electrostatic Force
Alpha-linkages
What equation is this
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Attractive force of electrostatic interactions
Solubility and Particle Size
What are the different types of Solute-Solvent Interactions
Van der Waals Forces
Hydrogen Bonds
Electrostatic Force
Alpha linkages
What are the different classifications of solvents
Polar
Semipolar
Nonpolar
Covalent
Hydrogen bonds
What is a polar solvent and what is an example of a polar solvent
exhibit strong dipolar bonds and hydrogen bond properties
water
exhibit strong dipolar bonds but not strong hydrogen properties
glycerin, propylene glycol, ethanol, acetone
chloroform, ethyl ester, benzene, carbon tetrachloride
What is a semipolar solvent and what is an example of a semipolar solvent
exhibit strong dipolar bonds and hydrogen bond properties
water
exhibit strong dipolar bonds but not strong hydrogen properties
glycerin, propylene glycol, ethanol, acetone
chloroform, ethyl ester, benzene, carbon tetrachloride
What is a nonpolar solvent and what is an example of a nonpolar solvent
exhibit low to little dipolar character and immiscible with water
water
exhibit strong dipolar bonds but not strong hydrogen properties
glycerin, propylene glycol, ethanol, acetone
chloroform, ethyl ester, benzene, carbon tetrachloride
Which solvents are semipolar
glycerin, propylene glycol
water
ethanol, acetone
benzene, carbon tetrachloride
chloroform, ethyl ether
Which solvents are nonpolar
glycerin, propylene glycol
water
ethanol, acetone
benzene, carbon tetrachloride
chloroform, ethyl ether
What are some solubility enhancements that can be made during preformulation
chemical modification; reduce the particle size
addition of co-solvent
pH adjustment; advanced formulation
addition of complexing agent
addition of surfactant
What are examples of co-solvents
water, alcohol
caffeine, EDTA
glycerin
cyclodextrin
span
What are examples of complexing agents
Tween
caffeine, EDTA
SLS
cyclodextrin
span
What are examples of surfactants
tween
caffeine, EDTA
SLS
cyclodextrin
span
What equation is this
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Solubility Prediction
Solubility and Particle Size
What does S represent
solubility of particles
solubility of solid
surface tension
radius of particles
molar volume
What does S0 represent
solubility of particles
solubility of solid
surface tension
radius of particles
molar volume
What does lowercase gamma represent
solubility of particles
solubility of solid
surface tension
radius of particles
molar volume
What does V represent
solubility of particles
solubility of solid
surface tension
radius of particles
molar volume
What does r represent
solubility of particles
solubility of solid
absolute temperature
radius of particles
gas constant
What does R represent
solubility of particles
solubility of solid
absolute temperature
radius of particles
gas constant
What does T represent
solubility of particles
solubility of solid
absolute temperature
radius of particles
gas constant
What are the possible gas constants you can use for R
1.987 cal/mol
8.314 J/mol*K
8.314 x 107 erg/mol*K
8.314 x 107 dyn/cm
0.0821 L*atm/mol*K
What is the log (S/S0)
log(1.10)
log(100)
log(1)
log(50)
log(0.90)
What is lowercase gamma
100 dynes/cm
1.10
50 cm3
300 K
8.314*107 dynes/cm
What is V
100 dynes/cm
1.10
50 cm3
300 K
8.314*107 dynes/cm
What is T
100 dynes/cm
1.10
50 cm3
300 K
8.314*107 dynes/cm
What is the best R to use
100 dynes/cm
8.314 J/mol*K
0.0821 L*atm/mol*K
8.314*107 erg/K*mol
8.314*107 dynes/cm
The solubility of ____ can be affected by pH
weak electrolytes
weak acid
weak base
What relationship does this equation establish
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Solubility Prediction
Solubility and pH
What is St
Total Solubility
Starting Solubility
Acid Dissociation Constant
Acid Concentration
Molecular Weight
What is S0
Total Solubility
Starting Solubility
Acid Dissociation Constant
Acid Concentration
Molecular Weight
What is Ka
Total Solubility
Starting Solubility
Acid Dissociation Constant
Acid Concentration
Molecular Weight
What is [H+]
Total Solubility
Starting Solubility
Acid Dissociation Constant
Acid Concentration
Molecular Weight
What are characteristics of a cosolvent system
used when a drug is not completely soluble in water
must be biocompatible and miscible in each other
the mole fraction of the cosolvent system affects the dielectric constant of the mixture
used when a drug is not soluble in water
What equation is this
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Solubility Prediction
Mole fraction
What relationship does this equation establish
Drug Solubility in Ideal Solution
Temperature and Solubility
Stoke's-Einstein Equation
Solubility Prediction
Solubility and pH
What is X2
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is Delta Hf
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is R
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Melting Point
Temperature of Measurement
What is T
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Starting Temperature
Temperature of Measurement
What is T0
Mole Fraction Solubility
Heat of Fusion
Gas Constant
Starting Temperature
Temperature of Measurement
What type of process is dissolution typically and what is the exception
endothermic
exothermic
Ca(OH)2
Ce2(SO4)3
What can you use to initially investigate solubility if resources were limited
water
saline
0.1M HCl
0.1M NaOH
propylene glycol
What can you use to initially investigate solubility if resources were sufficient
PEG 400
oils
0.1M HCl
surfactant systems
propylene glycol
Hygroscopy is the ability of a substance to
attract and hold water molecules from the surrounding environment
repel and push away water molecules from the surrounding environment
attract and use water molecules from the surrounding environment
What is hygroscopicity
the degree which a substance is hygroscopic
the degree which a substance is hydroscopic
Hygroscopicity refers to how moisture affects
flow
compaction
dissolution
stability
storage/packaging
What are ways in which a hygroscopic compound can retain water
bulk or surface adsorption
capillary condensation
chemical reaction
deliquescence
efflorescence
What is deliquescence
a solid dissolves and saturates a thin film of water on its surface
moisture is absorbed to the extent that deliquescence takes place, the liquid film surrounding the solid is saturated
process dictated by vapor diffusion and heat transport rates
a crystal loses water of crystallization below a critical water vapor pressure
What is efflorescence
a solid dissolves and saturates a thin film of water on its surface
moisture is absorbed to the extent that deliquescence takes place, the liquid film surrounding the solid is saturated
process dictated by vapor diffusion and heat transport rates
a crystal loses water of crystallization below a critical water vapor pressure
the opposite of deliquescence
What equation is this
Drug Solubility in Ideal Solution
Temperature and Solubility
Relative Humidity
Solubility Prediction
Mole fraction
What is relative humidity normally expressed as
a percentage
a decimal
a fraction
a temperature
What does phi represent
relative humidity
water vapor
equilibrium vapor pressure of water
temperature
pressure
What does ew represent
relative humidity
water vapor
equilibrium vapor pressure of water
temperature
pressure
What does ew* represent
relative humidity
water vapor
equilibrium vapor pressure of water
temperature
pressure
RH (phi) depends on the ___ and ____ of the system of interest
relative humidity
water vapor
equilibrium vapor pressure of water
temperature
pressure
Vapor pressure or equilibrium vapor pressure is defined as the pressure exerted by a vapor in thermodynamic equilibrium with its (1) at a (2) in a (3)
1 - condensed phases; 2 - given temperature; 3 - closed system
1 - condensed phases; 2 - any temperature; 3 - closed system
1 - condensed phases; 2 - given temperature; 3 - open system
1 - condensed phases; 2 - any temperature; 3 - open system
Which equation is displayed and what does it relate to
Antoine equation
August equation
Vapor Pressure
Relative Humidity
Which equation is displayed and what does it relate to
Antoine equation
August equation
Vapor Pressure
Relative Humidity
What are the hygroscopicity classifications
non-hygroscopic
slightly hygroscopic
moderately hygroscopic
very hygroscopic
What is a class 1: non-hygroscopic classification
essentially no moisture increase occur at relative humidities below 90%
essentially no moisture increase occur at relative humidities below 80%
moisture content does not increase more than 5% after storage for 1 week at relative humidities below 60%
moisture content increase may occur at relative humidities as low as 40-50%
What is a class 2: slightly hygroscopic classification
essentially no moisture increase occur at relative humidities below 90%
essentially no moisture increase occur at relative humidities below 80%
moisture content does not increase more than 5% after storage for 1 week at relative humidities below 60%
moisture content increase may occur at relative humidities as low as 40-50%
What is a class 3: moderately hygroscopic classification
essentially no moisture increase occur at relative humidities below 90%
essentially no moisture increase occur at relative humidities below 80%
moisture content does not increase more than 5% after storage for 1 week at relative humidities below 60%
moisture content increase may occur at relative humidities as low as 40-50%
What is a class 4: very hygroscopic classification
essentially no moisture increase occur at relative humidities below 90%
essentially no moisture increase occur at relative humidities below 80%
moisture content does not increase more than 5% after storage for 1 week at relative humidities below 60%
moisture content increase may occur at relative humidities as low as 40-50%
In lipophilicity, what is the partition coefficient
ratio of the concentration of the compound in the two phases of a mixture of two immiscible solvents at equilibrium
ratio of the concentration of the compound in the two phases of a mixture of two immiscible solvents not at equilibrium
ratio of the concentration of the compound in the two phases of a mixture of two miscible solvents at equilibrium
ratio of the concentration of the compound in the two phases of a mixture of two miscible solvents not at equilibrium
What does this equation represent
octanol-water partition coefficient
immiscible solvent coefficient
hygroscopicity
octanol-water hygroscopicity
If the logP is = 0
the mixture is in equal amounts
the mixture is more lipid soluble
the mixture is more water soluble
If the logP is > 0
the mixture is in equal amounts
the mixture is more lipid soluble
the mixture is more water soluble
If the logP is < 0
the mixture is in equal amounts
the mixture is more lipid soluble
the mixture is more water soluble
What partition coefficient substituents increase P
-alkyl
-aryl
-OH, -COOH
-O, -CO
-NH2
What partition coefficient substituents decrease P
-alkyl
-aryl
-OH, -COOH
-O, -CO
-NH2
To increase lipophilicity,
most programs use a group additivity approach
some programs use more complicated algorithms
most use clogP
most programs use a group reductive approach
some programs use more basic algorithms
What is apparent partition coefficient (Papp)
the effective lipophilicity of a compound at a given pH
a function of both the lipophilicity of the unionized compound and the degree of ionization
the ineffective lipophilicity of a compound at a given pH
a function of both the lipophilicity of the ionized compound and the degree of ionization
What equation is this
Apparent Partition Coefficient for Weak Acids
Apparent Partition Coefficient for Weak Bases
Apparent Partition Coefficient
Effective Lipophilicity
What equation is this
Apparent Partition Coefficient for Weak Acids
Apparent Partition Coefficient for Weak Bases
Apparent Partition Coefficient
Effective Lipophilicity
What is this equation for
weak acids
weak bases
strong acids
strong bases
What is the slope
1/Papp
1/P
Ka/P
1/[H+]
What is the y-intercept
1/Papp
1/P
Ka/P
1/[H+]
What is the y-axis
1/Papp
1/P
Ka/P
1/[H+]
What is the x-axis
1/Papp
1/P
Ka/P
1/[H+]
What is this equation for
weak acids
weak bases
strong acids
strong bases
What is the x-axis
1/Papp
1/P
1/Ka*P
[H+]
What is the y-axis
1/Papp
1/P
1/Ka*P
[H+]
What is the y-intercept
1/Papp
1/P
1/Ka*P
[H+]
What is the slope
1/Papp
1/P
1/Ka*P
[H+]
What are the applications of log P when using it to predict the solubility of a drug
drugs with high logP values have low aq solubility
drugs with low logP values have high aq solubility
drugs with high logP values have high aq solubility
drugs with low logP values have low aq solubility
What are the applications of log P when using it to predict the drug absorption
drugs with high logP values are easily bound to protein, have low aq solubility, and bind to extraneous sites
drugs with low logP values may be too hydrophilic to have any affinity for the membranes and may be poorly absorbed
drugs with low logP values are easily bound to protein, have low aq solubility, and bind to extraneous sites
drugs with high logP values may be too hydrophilic to have any affinity for the membranes and may be poorly absorbed
LogP helps to discover the preservation of oral liquid pharmaceutical dosage forms because
the preservatives take effects under their unionized forms
in emulsion, the unionized preservative is lipid soluble whereas microbes grow in aq phases where the ionic form of the preservatives likes to accumulate
the preservatives take effects under their ionized forms
in emulsion, the ionized preservative is lipid soluble whereas microbes grow in aq phases where the ionic form of the preservatives likes to accumulate
