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Pharmaceutics II Exam 1 > Part 2 > Flashcards

Part 2 Flashcards

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
Q

true or false

acidifying agents and alkalinizing agents are used in both liquid and solid preparations

A

FALSE – only liquid

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26
Q

give 10 examples of alkalinizing agents

A

ammonia solution
ammonium carbonate
diethanolamine
monoethanolamine
potassium hydroxide
sodium borate
sodium carbonate
sodium hydroxide
triethanolamine
trolamine

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27
Q

give the definition of an adsorbent and give 2 examples

A

an adsorbent is an agent capable of holding other molecules onto its surface by physical or chemical means

powdered cellulose
activated charcoal

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28
Q

true or false

activated charcoal is an adsorbent. it does not permeate and does not go into circulation

A

true

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29
Q

define an aerosol propellant

A

an agent responsible for developing the pressure within an aerosol container and expelling the product when the valve is open

30
Q

what is a coolant?

A

a liquid that absorbs heat quickly

31
Q

what is an air displacement agent? give example(s)

A

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
Q

name the different dosage forms available for tagamet

A

solution
tablet
large volume IV
small volume IV
solution
viscous liquid

33
Q

air diaplacement is related to maintaining the ___ of the product

A

stability

34
Q

if liquid/semi-solid dosage form contains sugar and free water….

A

antifungal preservative is required

35
Q

give the definition of an antifungal preservative

A

used in LIQUID and SEMISOLID preparations to prevent the growth of fungi

effectiveness of the parabens is usually enhanced if used in combination

36
Q

name 7 examples of antifungal preservatives

A

methylparaben
ethylparaben
propylparaben
butylparaben
benzoic acid
sodium benzoate
sodium propionate

37
Q

between sodium benzoate and benzoic acid, which would you select to have HIGH ACTIVITY

A

low activity but long duration = sodium benzoate

benzoic acid = high activity but low duration

thus, benzoic acid would be the choice

38
Q

define an antimicrobial preservative

A

used in liquid and semisolid preparations to PREVENT THE GROWTH OF MICROORGANISMS

39
Q

true or false

antimicrobial preservative and antifungal preservative are interchangeable terms

A

FALSE

antifungal prevents the growth of fungi and antimicrobial prevents the growth of microorganisms.

they are NOT the same

40
Q

are preservatives used in single dose containers?

A

NO

41
Q

name 9 antimicrobial preservatives

A

benzalkonium chloride
benzethomium chloride
benzyl alcohol
cetylpyridinium chloride
chlorobutanol
phenol
phenylethyl alcohol
phenylmercuric nitrate
thimerosol

42
Q

of the 9 antimicrobial preservatives mentioned, which is very corrosive to the skin?

A

phenol. also used in lysol

43
Q

of the 9 antimicrobial preservatives listed, which is popular in eye solutions as a preservative?

A

thimerosol

44
Q

true or false

benzalkonium chloride and benzethonium chloride are both antimicrobial preservatives and surfactants

A

true

45
Q

no more than _______ mL of preservatives can be injected via IV

A

no more than 5mL

46
Q

true or false

infusions are multi dose and do not need antimicrobial preservatices

A

FALSE

they are single dose and therefore don’t need preservatives

47
Q

true or false

if there is no preservative, the liquid/semisolid dosage forms cannot be used more than once

A

true

48
Q

true or false

according to the USP, at times a small amount of microorganisms is okay

A

true, but if the limit is exceeded it poses a stability issue

49
Q

antioxidants are used to ensure _____

A

stability

50
Q

define an antioxidant

A

an agent which inhibits oxidation and is thus used to prevent the deterioration of preparations through oxidation

51
Q

how to antioxidants accomplish their function?

A

they undergo a reaction with oxygen and “sacrifice themselves” in the process. they have very high activity

52
Q

true or false

antioxidants aren’t bad for our body

A

false. too much antioxidants can cause cancer

53
Q

name 4 examples of antioxidants

A

ascorbic acid
BHA (butylated hydroxyanisole)
BHT (butylated hydroxytoluene)
Sodium ascorbate

54
Q

what is the composition of vitamin C supplement

A

ascorbic acid and sodium ascorbate and sugar

ascorbic acid is very bitter. sodium ascorbate and sugar are added to reduce the bitter taste

55
Q

which antioxidants are used in food?

A

BHT and BHA

56
Q

why are buffering agents used?

A

to resist changes in pH upon dilution or addition of acid or alkali (base)

inhibit pH change

57
Q

explain the components of a buffering agent

A

contains a weak acid and its salt (weak base) or a weak base and its salt (weak acid)

reversible reaction to maintain equivalence

58
Q

give an example of a buffering agent

A

monobasic sodium acetate

59
Q

define a chelating agent

A

a substance that forms stable, water soluble complexes (chelates) with metals

60
Q

what is a chelate

A

a stable, water soluble complex with a central metal atom

61
Q

when is a chelating agent used in pharmaceuticals?

A

used in some liquid preparations as STABILIZERS to complex heavy metals that might cause instability

(SEQUESTERING AGENT)

62
Q

True or false

a chelating agent forms a complex with organic molecules

A

FALSE – with metals

63
Q

give example(s) of a chelating agent

A

Edetate disodium (Na2 EDTA)
Edetic acid (EDTA)

64
Q

both ____ and _____ are not allowed for infants, as it causes organ damage

A

both coloring and preservatives

65
Q

define a colorant

A

used to impart color to liquid and solid pharmaceutical preparations

66
Q

colorants are mainly used for which dosage form

A

tablet dosage form. tablet is the most popular

67
Q

name 2 NATURAL colorants

A

caramel (used in coke)
ferric oxide

68
Q

true or false

it is preferred to use natural colorants over artificial

A

true

69
Q

there are ____ types of colorant:

A

2: natural and artificial

70
Q

ferric oxide imparts what color?

A

orange-pink (natural colorant)

71
Q
A

Pharmaceutics II Exam 1 (9 decks)

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