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Pharmaceutics II Exam 1 > Part 1 > Flashcards

Part 1 Flashcards

1
Q

true or false

preformulation studies are ONLY related to the API itself

A

true

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2
Q

the dosage form includes….

A

the API and all excipients

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3
Q

true or false

drug substances are often administered alone

A

FALSE

they are administered as part of a formulation, in combination with one or more nonmedical agents (excipients) that serve varied and specialized pharmaceutical functions

drug substances are SELDOM administered alone

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4
Q

name 9 functions of pharmaceutical ingredients

A

solubilize
suspend
stabilize
thicken
dilute
emulsify
preserve
color
flavor

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5
Q

in a nutshell, what is the function of pharmaceutical ingredients?

A

to fashion medicinal agents into efficacious and appealing dosage forms

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6
Q

each type of ______ is unique in its ____ and _____ characteristics

A

each type of DOSAGE FORM is unique in its PHYSICAL and PHARMACEUTICAL characteristics

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7
Q

give an example of when we would want to thicken a dosage form

A

in the case of eye drops, we can thicken them to increase the retention time. this minimizes loss of the medication and it needs to be applied less frequently

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8
Q

do elixirs need a preservative?

A

NO

elixirs have enough alcohol to not need a preservative

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9
Q

give an example of when a preservative would be needed

A

with a lot of free water

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10
Q

do large volume IVs need preservative?

A

NO they are single dose. don’t need preservative

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11
Q

give an example of when a diluent excipient would be needed

A

for the tablet dosage form

especially needed if the drug is a very low dose, as a tiny drug would be impossible to properly handle

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12
Q

of the 9 functions of pharamaceutical ingredients (excipients), which function is the most important and the biggest concern

A

STABILIZE

for example, vitamin C is highly susceptible to oxidation and needs to be stabilized

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13
Q

as mentioned, each type of dosage form is unique in its physical and pharmaceutical characteristics

the excipients used is contingent on what?

A

the duration, onset time, etc

the ultimate goal is to obtain the maximum treatment with minimum side effects

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14
Q

what is the main concern in the case of stability?

A

the environment–

-oxidation
-hydrolysis (humidity)
-photolysis (light)

also microorganisms

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15
Q

true or false

stability is a concern with both the API itself as well as the entire formulation

A

true

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16
Q

what are methods to protect the drug substance from the destructive influences of atmospheric oxygen or humidity?

A

coated tablets and sealed ampuls

oxygen can’t penetrate these things and no microorganisms can come into sealed ampuls

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17
Q

for which dosage form is gastric acid destruction the biggest concern? what is done to combat it?

A

oral dosage form. gastric acid is an extremely low pH and the API will degrade in this environment. it needs to be protected

enteric coated tablets are produced. these will not dissolve in the stomach (will dissolve at high pH) and cause irritation. the tablet will dissolve in the small intestine instead.

ex: aspirin is weakly acidic and would normally dissolve in the stomach, but enteric coating prevents this

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18
Q

what is done to conceal the bitter or bad taste or odor of a drug substance?

A

the use of capsules, coated tablets, and flavored syrups

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19
Q

explain how capsules are utilized to mask the bad taste of a drug.

wouldn’t capsules still dissolve on the tongue and leave a bad taste?

A

capsules are formulated such that they will not dissolve in the mouth – the shell will not dissolve in cold fluids but only the warmth of our body fluids

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20
Q

as long as _________the bitter taste of a drug will not be noticed

A

the drug doesnt release on the tongue

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21
Q

liquid preparations of drugs substances can be prepared as ___ or ___

A

dispersions (suspensions)
clear preparations (solutions)

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22
Q

true or false

the solid dosage form is normally preferred, but the liquid dosage form is required for some populations

A

true

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23
Q

which uses a cosolvent system – solutions or suspensions?

A

solutions. cosolvent system is used to ensure that the drug will dissolve

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24
Q

how can rate-controlled drug action be provided?

A

through various controlled release tablets, capsules, and suspension

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25
Q

true or false

the higher the drug concentration, the higher the solubility

A

FALSE – the higher the dissolution rate

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26
Q

are suspensions an example of a rate-controlled drug?

A

yes

the solid powder is in the stomach and is slowly dissolving. this controls the dissolution rate – slowly. will have low concentration available overall, degradation is less and bioavailability is INCREASED as compared to solution.

extended duration of therapy.
in the case of solutions, it will be subject to quick degradation because all of the drug is already in solution and available for degradation

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27
Q

true or false

it is easier to optimize drug action of topical drugs as compared to oral drugs

A

true

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28
Q

explain how the insertion of a drug into body orifices is available

A

through the rectal and vaginal dosage forms

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29
Q

what dosage form(s) allow doe the placement of drugs directly into the bloodstream or body tissues?

A

injections

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30
Q

name topical dosage forms (6)

topical dosage forms allow for…

A

ointment
cream
transdermal patches
ophthalmic
ear
nasal

topical dosage forms allow for OPTIMAL DRUG ACTION

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31
Q

One of the needs for dosage forms is to provide for optimal drug action through……

A

both topical administration sites and inhalation therapy (inhalants and inhalation aerosols)

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32
Q

how do you increase the retention time at the site of the stomach for a solution dosage form whose site of action is the stomach?

A

through a viscosity agent to thicken – will increase the time at the site of action of the stomach

will go from stomach to small intestine very quickly if too thin.

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33
Q

solutions include……

A
  1. API
  2. Solvent(s)
34
Q

true or false

most APIs are solid powders

A

true

35
Q

for a tablet to have an effect what has to happen?

A

it needs to dissolve

36
Q

what determines if a drug will dissolve?

A

solute-solute
solute-solvent
solvent-solvent interactions.

through various forces and bonds—

-van der waals
-ion-dipole
-ion-induced dipole
-hydrogen
-ion-ion

37
Q

WHAT 3 THINGS NEED TO BE CONSIDERED IN PREFORMULATION STUDIES?

A
  1. physiochemical properties of the drug itself (API – no excipients yet)
  2. Biopharmaceutical considerations (ADME)

3, Therapeutic consderations of the disease state

38
Q

as mentioned, one of the 3 main things to be considered in preformulation are the physiochemical properties of the drug itself.

explain this further

A

-the forces and bonds
-the states of matter
-stable solid dilutions
-UNSTABLE solid dilutions
-liquid-aqueous concentrates (mixing elixir w solution)
-acids and bases
-liquid-oil concentrates of liquids (ie: emulsion)
-drug and product stability

39
Q

give an example of a stable, solid dilution

AND an unstable, solid dilution

A

in most cases, 1mg of API combined with 99mg of excipients will be stable

unstable – nitroglycerin. nitroglycerin easily evaporates, so it is not opened in the pharmacy and the patient will receive the full bottle

40
Q

give an example of a liquid-aqueous concentrate.
is it any concern?

A

mixing elixir with solution.

this could be an issue because a solution has little to no alcohol content. this can pose a solubility issue

41
Q

explain how biopharmaceutical considerations are something to think about for preformulation

A

ADME

D – after the drug dissolves, how will it get from plasma to the receptor site? if it doesnt get there, there is no therapeutic effect

M – 1st pass effects of liver. Most of the drug is destroyed in the liver and only a small amount survives to get into circulation

42
Q

true or false

when all is said and done, all dosage forms will end up as a solution

A

true – they have to dissolve in order to have therapeutic effect

43
Q

true or false

the drug only has to reach the receptor site in order to exert therapeutic effect

A

FALSE – needs to actually bind to the receptor

44
Q

true or false

if the body considers a drug to be “safe”, it does not undergo metabolism and 1st pass effects

A

true

45
Q

what is step 1 of drug design after the drug has been discovered

A

preformulation studies

46
Q

what is the #1 concern of a solid dosage form

A

solubility.

drug MUST dissolve in order to exert effect

47
Q

under preformulation studies, what “physical description” must be studied?

A

the appearance, color, odor, and taste

48
Q

why is microscopic examination part of preformulation studies?

A

the particle size and range of the raw drug substance must be determined, as well as the crystal structure

this is related to SOLUBILITY which is the #1 concern of the solid dosage form

49
Q

why is heat of vaporization part of preformulation studies

A

mainly in determining the vapor pressure for implantable pumps and aerosol dosage forms

50
Q

why is melting point depression part of preformulation studies

A

if i add “x” excipient, how much will the melting point decrease?

for instance, salt lowers the melting point of water to melt snow

51
Q

the higher the molecular weight, the ____ the melting point

A

higher

52
Q

why is the “phase rule” part of preformulation studies

A

if we have 2 phases in a formulation, we want to know the interaction between them

if we add a surfactant to this, there are now 3 phases – we want to know the interaction between the 3 phases

53
Q

true or false

if the particle size is decreased, there is a substantial increase in solubility

A

FALSE

the intrinsic solubility does not change, but the dissolution rate increases due to higher surface area which makes it faster to prepare

HOWEVER, it is also possible for the particle size to be so small that it can’t interact with the solvent and dissolve

54
Q

what is the freezing point of water

A

the freezing point of PURE water is 32 degrees F

HOWEVER, impurities can affect the melting/freezing point

55
Q

upon the addition of a second component, which melting point is MORE LOWERED—

-a compound with a low melting point
-a compound with a high melting point

A

the low-melting point compound will be affected to a greater extent (greater lowering of melting point)

56
Q

are pka/dissociation constants part of preformulation studies?

A

yes

expresses the extent of ionization

57
Q

how are organic salts obtained?

A

from acid base reactions

58
Q

name 5 things that particle size has an effect on

(IMPORTANT)

A

-drug dissociation rate
-bioavailability
-content uniformity
-flow characteristics
-sedimentation rates

59
Q

one of the parameters that particle size has an effect on is bioavailability.

explain what this is

A

the amount of drug available in systemic circulation and is thus able to have an effect

60
Q

explain how particle size affects content uniformity

A

if small and large particles are mixed together (not uniform), the large particles will sink and the dose will not be right

61
Q

explain how particle size affects flow characteristics

A

capsule/tablet dosage form is preferred.

when manufacturing in the industry, the powder to make the tablet/capsule needs to flow evenly so that all the dosage forms are even and uniform

62
Q

what are the methods of evaluating particle size?

A
  1. Sieving or screening
  2. Microscopy
  3. Sedimentation
  4. Stream scanning (coulter counter, hiac counter)
63
Q

when the particle size of water insoluble drugs is reduced, ____ increases, this results in higher _____

A

DISSOLUTION RATE increases and this results in higher AVAILABILITY AT THE ABSOPRTION SITE (bioavailability)

64
Q

what is sieving

A

like sifting in baking.
method to evaluate particle size

65
Q

what is microscopy

A

method of evaluating particle size AND crystal structure

66
Q

what is stream scanning

A

includes coulter counter and hiac counter.

method to evaluate particle size and the number of particles.

a shadow is created to find out this information

67
Q

true or false

the particle size of the API is the only concern

A

FALSE – both API and excipients.
want a similar size between them

68
Q

particle size is most especially important in ____ dosage form

A

parenteral

69
Q

if reducing the particle size doesn’t work to dissolve, what can be done next?

A

polymorphism

70
Q

true or false

if a drug is water soluble, bioavailability isn’t really a concern

A

TRUE

water soluble molecules don’t undergo first pass effects and are able to dissolve in the blood

71
Q

____-____% of drugs in the market use polymorphic API

does this need a new NDA?

A

15-20%

YES
when going from crystalline to amorphous form, the drug is considered new and an NDA is needed

72
Q

many new drugs are water insoluble.
this can be combatted by reducing the amount of API in the formulation.

does this need a NDA? what is the concern with this?

A

does NOT need an NDA

this is a concern bc reducing the amount of API can affect the bioavailability. we need a sufficient bioavailability to have therapeutic effect

73
Q

which has a higher dissolution rate – amorphous or crystal form?

A

amourphous

74
Q

when a drug precipitates, energy is ______ and it is now _____

A

when a drug precipitates, energy is RELEASED and it is now STABLE

LOW SOLUBILITY requires energy to reintroduce to liquid state

75
Q

is more energy required to go from liquid to solid or solid to liquid?

A

solid to liquid

76
Q

when a polymorphic drug is compared to a crystalline drug, which requires more energy from outside to transform the compound from solid to liquid?

A

crystalline requires MORE ENERGY to change

77
Q

do polymorphic drugs contain energy?

A

yes, they retain some energy

78
Q

which has a lower melting point – polymorphic or crystalline form?

A

polymorphic

79
Q

true or false

different polymorphs of the same drugs have the same physiochemical properties

A

FALSE

this is why the FDA considers it a new drug and requires a new NDA

80
Q

different polymorphs can have different ____,_____, and ____

A

density vapor pressure and stability

81
Q

how are polymorphs prepared?

A

the drug is rapidly precipitated from the solvent which does not allow the drug molecules enough time to form an orderly array.

the drug is rapidly cooled and spray dryed/freeze dried

the goal is to retain ENERGY in the structure BUT we also want it to have a decent stability and dissolution

82
Q
A

Pharmaceutics II Exam 1 (9 decks)

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