PHRM 515 Exam 3 Copy Study Set
The code of federal regulations (CFR) defines a biologic as _______ - ANSWER any virus,
therapeutic serum, toxin, antitoxin, or analogues product employed for the prevention,
treatment, or cure of diseases in humans (peptides, proteins, antibodies, hormones,
fusion proteins, vaccines)
Size of a small molecule - ANSWER <900 Da
MW of an antibody? - ANSWER 150 kDa
Size of a biologic - ANSWER variable, but large compared to small molecule
Small molecules are usually synthesized in ____ - ANSWER a lab
Most biologic drugs are _____ - ANSWER protein-based (enzymes, peptides, antibodies)
How are biologics usually synthesized? - ANSWER either isolated from living sources or
use components derived from living sources
T/F: Small molecules are typically fairly robust - ANSWER TRUE
Compared to small molecules, biologics are more susceptible to __(5) - ANSWER
thermal degradation
adsorption
microbial contamination
mechanical agitation
pH variation
Biologics have a tendency to _____ - ANSWER tendency to misfold/aggregate/precipitate
causing a significant loss of efficacy
Aggregated proteins can sometimes form ____ - ANSWER superpotent materials
(causes exaggerated immune response)
Most pharmaceutical compounds are _______ - ANSWER weak acids or bases
Ionization state of weak acids or bases is dependent on ____ - ANSWER its pKa and the
pH of the solution
pka is the pH at which? - ANSWER 50% of the drug is ionized and 50% is unionized
The equilibrium between ionized/non-ionized species is dictated by - ANSWER pH of the
,solution and how much the functional group wants to give up its proton
If a weak acid really wants to give up its proton the Ka will be - ANSWER large
the greater the Ka the _____ the pka? - ANSWER lower
The permeation of weak acids in aqueous solution decreases as pH - ANSWER
increases
The solubility of weak acids in aqueous solution increases as pH - ANSWER increases
pH of a formulation may be a function of the API or as formulated with excipients to (6) -
ANSWER improve solubility
improve permeation
enhance stability
improve antimicrobial activity
improve palatability
minimize tissue irritation
Glass is made from ____ - ANSWER a network of silica and oxygen atoms
Ion exchange reactions with glass can cause ______ - ANSWER formulation pH to
increase
(Na+ from glass swap with H+ in formulation)
CO2 from ambient air can dissolve in water causing a _____ - ANSWER reduction in pH
What is the typical pH of pure water - ANSWER slightly acidic (dissolved CO2)
During packaging, how can we minimize reduction in pH due to CO2 from ambient air -
ANSWER add a buffer
single use ampule
flush head space with nitrogen or argon
T/F: pH does not affect thermal stability - ANSWER FALSE
(vitamin B1 can be autoclaved at low pH but degrades rapidly at high pH)
Drugs produced by _________ will be
generated at an optimal pH value - ANSWER enzymatic/microorganisms
Microbial growth is generally optimal between pH ____ - ANSWER 6-8
T/F: The higher the pH, the more benzoic acid a formulation needs - ANSWER TRUE
,Which pH, 2.5 or 7.5, will require a higher concentration to confer the same level of
antimicrobial activity - ANSWER 7.5
We want to avoid significant ______ of formulations and fluids in the intended
compartment - ANSWER pH differences
Which route of administration has no buffering capacity? - ANSWER Rectal
T/F: In many cases, no/minimal buffering is used in a formulation? - ANSWER TRUE
pH is reliant on buffer present in compartment
in the blood buffering comes from plasma proteins and hemoglobin/oxyhemoglobin in
RBC
What is a buffer? - ANSWER a constituent that can resist changes in pH upon intro of
acidifying or alkalinizing agents
buffers themselves are WA/WB & are not pharmacologically active
Buffers include functional groups that can _____ - ANSWER bind to/give up protons
Common functional groups for buffers - ANSWER COOH and NH2
Monovalent buffer examples - ANSWER Tris and acetate
they gain/lose 1 proton
Multivalent buffer examples - ANSWER citrate and phosphate
multiple functional groups can gain or lose protons
acetate pka - ANSWER 4.8
tris pka - ANSWER 8.1
citrate pka - ANSWER 3.1, 4.8, 6.4
phosphate pka - ANSWER 2.1, 7.2, 12.4
, A buffer can be prepared at a given pH by calculating ___ - ANSWER proportions of
acid/conjugate base
Why might we want to use acetic acid as an otic solution? - ANSWER lowering pH to
prevent microbial growth
How to select a buffer? - ANSWER define target pH
decide on the intended buffering strength
consider compatibility with process (lyphophilization)
3 primarily used buffers in FDA approved formulation - ANSWER citrate, acetate,
phosphate
Acetate range of pH where it can maintain pH as relatively constant - ANSWER 3.8-5.8
Phosphate range of pH where it can maintain pH as relatively constant - ANSWER
6.2-8.2
Citrate range of pH where it can maintain pH as relatively constant - ANSWER 3.8-5.8
Buffering capacity - ANSWER ability of a buffer to resist change in pH upon addition of
acid or base
Buffering capacity equation commonly used in pharmacy - ANSWER Van slyke equation
The more concentrated the buffer aka higher molarity, - ANSWER the greater the
buffering capacity
The code of federal regulations (CFR) defines a biologic as _______ - ANSWER any virus,
therapeutic serum, toxin, antitoxin, or analogues product employed for the prevention,
treatment, or cure of diseases in humans (peptides, proteins, antibodies, hormones,
fusion proteins, vaccines)
Size of a small molecule - ANSWER <900 Da
MW of an antibody? - ANSWER 150 kDa
Size of a biologic - ANSWER variable, but large compared to small molecule
Small molecules are usually synthesized in ____ - ANSWER a lab
Most biologic drugs are _____ - ANSWER protein-based (enzymes, peptides, antibodies)
How are biologics usually synthesized? - ANSWER either isolated from living sources or
use components derived from living sources
T/F: Small molecules are typically fairly robust - ANSWER TRUE
Compared to small molecules, biologics are more susceptible to __(5) - ANSWER
thermal degradation
adsorption
microbial contamination
mechanical agitation
pH variation
Biologics have a tendency to _____ - ANSWER tendency to misfold/aggregate/precipitate
causing a significant loss of efficacy
Aggregated proteins can sometimes form ____ - ANSWER superpotent materials
(causes exaggerated immune response)
Most pharmaceutical compounds are _______ - ANSWER weak acids or bases
Ionization state of weak acids or bases is dependent on ____ - ANSWER its pKa and the
pH of the solution
pka is the pH at which? - ANSWER 50% of the drug is ionized and 50% is unionized
The equilibrium between ionized/non-ionized species is dictated by - ANSWER pH of the
,solution and how much the functional group wants to give up its proton
If a weak acid really wants to give up its proton the Ka will be - ANSWER large
the greater the Ka the _____ the pka? - ANSWER lower
The permeation of weak acids in aqueous solution decreases as pH - ANSWER
increases
The solubility of weak acids in aqueous solution increases as pH - ANSWER increases
pH of a formulation may be a function of the API or as formulated with excipients to (6) -
ANSWER improve solubility
improve permeation
enhance stability
improve antimicrobial activity
improve palatability
minimize tissue irritation
Glass is made from ____ - ANSWER a network of silica and oxygen atoms
Ion exchange reactions with glass can cause ______ - ANSWER formulation pH to
increase
(Na+ from glass swap with H+ in formulation)
CO2 from ambient air can dissolve in water causing a _____ - ANSWER reduction in pH
What is the typical pH of pure water - ANSWER slightly acidic (dissolved CO2)
During packaging, how can we minimize reduction in pH due to CO2 from ambient air -
ANSWER add a buffer
single use ampule
flush head space with nitrogen or argon
T/F: pH does not affect thermal stability - ANSWER FALSE
(vitamin B1 can be autoclaved at low pH but degrades rapidly at high pH)
Drugs produced by _________ will be
generated at an optimal pH value - ANSWER enzymatic/microorganisms
Microbial growth is generally optimal between pH ____ - ANSWER 6-8
T/F: The higher the pH, the more benzoic acid a formulation needs - ANSWER TRUE
,Which pH, 2.5 or 7.5, will require a higher concentration to confer the same level of
antimicrobial activity - ANSWER 7.5
We want to avoid significant ______ of formulations and fluids in the intended
compartment - ANSWER pH differences
Which route of administration has no buffering capacity? - ANSWER Rectal
T/F: In many cases, no/minimal buffering is used in a formulation? - ANSWER TRUE
pH is reliant on buffer present in compartment
in the blood buffering comes from plasma proteins and hemoglobin/oxyhemoglobin in
RBC
What is a buffer? - ANSWER a constituent that can resist changes in pH upon intro of
acidifying or alkalinizing agents
buffers themselves are WA/WB & are not pharmacologically active
Buffers include functional groups that can _____ - ANSWER bind to/give up protons
Common functional groups for buffers - ANSWER COOH and NH2
Monovalent buffer examples - ANSWER Tris and acetate
they gain/lose 1 proton
Multivalent buffer examples - ANSWER citrate and phosphate
multiple functional groups can gain or lose protons
acetate pka - ANSWER 4.8
tris pka - ANSWER 8.1
citrate pka - ANSWER 3.1, 4.8, 6.4
phosphate pka - ANSWER 2.1, 7.2, 12.4
, A buffer can be prepared at a given pH by calculating ___ - ANSWER proportions of
acid/conjugate base
Why might we want to use acetic acid as an otic solution? - ANSWER lowering pH to
prevent microbial growth
How to select a buffer? - ANSWER define target pH
decide on the intended buffering strength
consider compatibility with process (lyphophilization)
3 primarily used buffers in FDA approved formulation - ANSWER citrate, acetate,
phosphate
Acetate range of pH where it can maintain pH as relatively constant - ANSWER 3.8-5.8
Phosphate range of pH where it can maintain pH as relatively constant - ANSWER
6.2-8.2
Citrate range of pH where it can maintain pH as relatively constant - ANSWER 3.8-5.8
Buffering capacity - ANSWER ability of a buffer to resist change in pH upon addition of
acid or base
Buffering capacity equation commonly used in pharmacy - ANSWER Van slyke equation
The more concentrated the buffer aka higher molarity, - ANSWER the greater the
buffering capacity
