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Pharmaceutics II Exam 1 > Part 2 > Flashcards

Part 2 Flashcards

(71 cards)

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1
Q

besides reducing particle size and polymorphism, name 5 more ways in which solubility can be improved

A

-salt/ester formation
-pH
-cosolvent system (solutions)
-surfactants
-complexation

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2
Q

explain how salt/ester formation can improve solubility (give a specific example)

A

phenobarbital is a weak acid and is not very water soluble.
when it reacts with a base, the salt is formed which is very hydrophilic and thus water soluble

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3
Q

explain how pH can improve solubility

A

changing pH changes the ratio of ionized: unionized (Hendersen Hasselbalch eqn)

this is not really done a lot because the pH of the body can’t be changed

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4
Q

explain how cosolvent systems can improve solubility

A

can improve the solubility of poorly soluble drugs by using cosolvents such as–

-propylene glycol
-glycerin
-sorbitol
-polyethylene glycol

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5
Q

can the cosolvent system be used for the solid dosage form?

A

NO

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6
Q

explain how surfactants can improve solubility

A

ONLY for liquid and semisolid dosage forms (NOT SOLID)

through the formation of micelles

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7
Q

give a specific example of a natural surfactant

A

bile salts increase our absorption of lipids

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8
Q

give a specific example of complexation

what is the function

A

cyclodextrins can form complexes with drug molecules to improve solubility

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9
Q

true or false

a drug does not necessarily need to cross a biological membrane to have a pharmacological response

A

FALSE

the drug needs to cross

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10
Q

explain the properties of the biological membrane

A

has protein and lipid material.
serves as a lipophilic barrier to most drugs

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11
Q

what is alpha (a) value represent

A

the extent/degree of ionization

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12
Q

give the 2 formulas for partition coefficient

A

P = (conc of drug in octanol)/(conc of drug in water)

P=(conc of drug in octanol)/(1-a)(conc of drug in water)

a=extent/degree of ionization. usually very small

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13
Q

the ratio of ionized:unionized molecules depends on…

A

the pH and pka (according to the Hendersen Hasselbalch equation)

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14
Q

the salt form of a drug _______ the ionized concentration and therefore ______ permeate and the partition coefficient is _____

A

the salt form INCREASES the ionized concentration and therefore CANNOT permeate and the partition coefficient is LOW

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15
Q

why is octanol part of the formula for the partition coefficient

A

it is an organic solvent that represents the biological membrane

hexanol can be used too

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16
Q

what is the ideal partition coefficient between:

P>1
P=1
P<1

explain

A

P=1 is the most ideal

if P is greater than 1, there will be good permeability but the concentration at the absorption site will be very low

however, if P=1, this means that if there are 200 molecules, 100 will permeate and 100 will not. this is ideal to maintain the balance between dissolution and permeation

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17
Q

if P is low, this means the drug is ____ soluble

A

water

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18
Q

if P is small, the concentration at the absorption site will be______

A

high, but it will not permeate

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19
Q

in regards to drug stability, are we concerned with the API or the entire product?

A

the entire product (obviously including the API)

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20
Q

name 8 stability issues

A

-hydrolysis
-oxidation
-drug substance-excipient interaction
-photolysis
-polymerization
-isomerization
-deamination
-decarboylation

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21
Q

give the definition of an acidifying agent and give examples

A

acidifying agent is used in liquid preparations to provide an acidic medium for PRODUCT STABILITY

examples:

acetic acid
citric acid
fumaric acid
hydrochloric acid
nitric acid

they basically adjust the pH of the solution

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22
Q

what is the main concern in LIQUID dosage form?

A

STABILITY

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23
Q

what is the main concern in the SOLID dosage form?

A

SOLUBILITY

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24
Q

Define an alkalinizing agent

A

used in liquid preparations to provide an alkaline medium for product stability

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25
true or false acidifying agents and alkalinizing agents are used in both liquid and solid preparations
FALSE -- only liquid
26
give 10 examples of alkalinizing agents
ammonia solution ammonium carbonate diethanolamine monoethanolamine potassium hydroxide sodium borate sodium carbonate sodium hydroxide triethanolamine trolamine
27
give the definition of an adsorbent and give 2 examples
an adsorbent is an agent capable of holding other molecules onto its surface by physical or chemical means powdered cellulose activated charcoal
28
true or false activated charcoal is an adsorbent. it does not permeate and does not go into circulation
true
29
define an aerosol propellant
an agent responsible for developing the pressure within an aerosol container and expelling the product when the valve is open
30
what is a coolant?
a liquid that absorbs heat quickly
31
what is an air displacement agent? give example(s)
an agent that displaces air in a hermetically sealed (airtight) container to enhance product stability nitrogen carbon dioxide. they're sealed into the container to displace air and prevent oxidation
32
name the different dosage forms available for tagamet
solution tablet large volume IV small volume IV solution viscous liquid
33
air diaplacement is related to maintaining the ___ of the product
stability
34
if liquid/semi-solid dosage form contains sugar and free water....
antifungal preservative is required
35
give the definition of an antifungal preservative
used in LIQUID and SEMISOLID preparations to prevent the growth of fungi effectiveness of the parabens is usually enhanced if used in combination
36
name 7 examples of antifungal preservatives
methylparaben ethylparaben propylparaben butylparaben benzoic acid sodium benzoate sodium propionate
37
between sodium benzoate and benzoic acid, which would you select to have HIGH ACTIVITY
low activity but long duration = sodium benzoate benzoic acid = high activity but low duration thus, benzoic acid would be the choice
38
define an antimicrobial preservative
used in liquid and semisolid preparations to PREVENT THE GROWTH OF MICROORGANISMS
39
true or false antimicrobial preservative and antifungal preservative are interchangeable terms
FALSE antifungal prevents the growth of fungi and antimicrobial prevents the growth of microorganisms. they are NOT the same
40
are preservatives used in single dose containers?
NO
41
name 9 antimicrobial preservatives
benzalkonium chloride benzethomium chloride benzyl alcohol cetylpyridinium chloride chlorobutanol phenol phenylethyl alcohol phenylmercuric nitrate thimerosol
42
of the 9 antimicrobial preservatives mentioned, which is very corrosive to the skin?
phenol. also used in lysol
43
of the 9 antimicrobial preservatives listed, which is popular in eye solutions as a preservative?
thimerosol
44
true or false benzalkonium chloride and benzethonium chloride are both antimicrobial preservatives and surfactants
true
45
no more than _______ mL of preservatives can be injected via IV
no more than 5mL
46
true or false infusions are multi dose and do not need antimicrobial preservatices
FALSE they are single dose and therefore don't need preservatives
47
true or false if there is no preservative, the liquid/semisolid dosage forms cannot be used more than once
true
48
true or false according to the USP, at times a small amount of microorganisms is okay
true, but if the limit is exceeded it poses a stability issue
49
antioxidants are used to ensure _____
stability
50
define an antioxidant
an agent which inhibits oxidation and is thus used to prevent the deterioration of preparations through oxidation
51
how to antioxidants accomplish their function?
they undergo a reaction with oxygen and "sacrifice themselves" in the process. they have very high activity
52
true or false antioxidants aren't bad for our body
false. too much antioxidants can cause cancer
53
name 4 examples of antioxidants
ascorbic acid BHA (butylated hydroxyanisole) BHT (butylated hydroxytoluene) Sodium ascorbate
54
what is the composition of vitamin C supplement
ascorbic acid and sodium ascorbate and sugar ascorbic acid is very bitter. sodium ascorbate and sugar are added to reduce the bitter taste
55
which antioxidants are used in food?
BHT and BHA
56
why are buffering agents used?
to resist changes in pH upon dilution or addition of acid or alkali (base) inhibit pH change
57
explain the components of a buffering agent
contains a weak acid and its salt (weak base) or a weak base and its salt (weak acid) reversible reaction to maintain equivalence
58
give an example of a buffering agent
monobasic sodium acetate
59
define a chelating agent
a substance that forms stable, water soluble complexes (chelates) with metals
60
what is a chelate
a stable, water soluble complex with a central metal atom
61
when is a chelating agent used in pharmaceuticals?
used in some liquid preparations as STABILIZERS to complex heavy metals that might cause instability (SEQUESTERING AGENT)
62
True or false a chelating agent forms a complex with organic molecules
FALSE -- with metals
63
give example(s) of a chelating agent
Edetate disodium (Na2 EDTA) Edetic acid (EDTA)
64
both ____ and _____ are not allowed for infants, as it causes organ damage
both coloring and preservatives
65
define a colorant
used to impart color to liquid and solid pharmaceutical preparations
66
colorants are mainly used for which dosage form
tablet dosage form. tablet is the most popular
67
name 2 NATURAL colorants
caramel (used in coke) ferric oxide
68
true or false it is preferred to use natural colorants over artificial
true
69
there are ____ types of colorant:
2: natural and artificial
70
ferric oxide imparts what color?
orange-pink (natural colorant)
71

Pharmaceutics II Exam 1 (9 decks)

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