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Oral Dosage Forms— Modified Release > hw 4 study set > Flashcards

hw 4 study set Flashcards

1
Q

rate of drug dissolution is ___ proportional to particle size?

A

inversely

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2
Q

what can pH deependant drug release be achieved by?

A

enteric coating (shellac)

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3
Q

what improves drug release?

A

reduction in size or unstirred boundary layer

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4
Q

what plays major role in killing infected cells of antibodies?

A

glycosltion pattern

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5
Q

what is solid phase peptide syntheis?

A

peptide assembling on resin

deprotection and cleavage

column purification
lyphoilization
ion exchange
lypholization
packing and labelling

(depreotection, coupling, cleavage)

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6
Q

are antifboy based therapeutics produced from E coli?

A

no, peptide products are like hGH

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7
Q

PEGylation increases half-life while albumin-conjugation decreases half-life of a
protein therapeutic

A

false, both increase HL

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8
Q

sustained release and immediate release tablets can both be split in half without
affecting their in vivo performance

A

false, can only split IR and SR can be harmful

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9
Q

If we know the buffer-less rate constant of degradation of a peptide drug at multiple
higher temperatures?

A

we can calculate its shelf life at its storage temperature in a
refrigerator

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10
Q

Monoclonal antibodies are composed of?

A

4 chains bonded through
cysteine amino acids by disulfide bonds

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11
Q

Hydrolysis and deamidation of proteins, both usually proceed ?

A

through succinimide
intermediates

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12
Q

Ethyl cellulose can be used as a polymer when you want drug release from a matrix
by swelling?

A

no it is a non-swelling, hydrophobic polymer that relies primarily on the diffusion of the drug through the polymer matrix

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13
Q

Semaglutide by itself has?

A

low solubility and low permeability

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14
Q

A contraceptive drug formulated as a 200 mg PLGA-based intramuscular implant
will be able to release drug over a longer period of time as compared to the same drug
formulated as a 200 mg olive oil in water emulsion-based intramuscular depot.

A

true

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15
Q

what does effect of ionic strength on reaction rate k depend on?

A

the reaction rate constant depends on the nature of the reactants (charged vs neutral), the reaction mechanism, and the solvent.

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16
Q

what are natural polymers?

A

degradable in vivo, non toxic byproducts
chaargen, chitin, cellulose, strarch

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17
Q

what are semi snyheic polymers?

A

modified natural polymers

cellulose ethers, cellose acetates—

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18
Q

what are artificial polymers?
what are advanges?

A

artificial orgins, like rubbers, Dacron , plastic, PVS, PLGA, silicon

localize drug delivery
stabilization of drug
reduced side effects

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19
Q

what are hydrophobic philic, and hydrogel polymers?

A

non polar function groups

polar charged groups –water soluble (sodium, alginate, chitosan)

swell but do not dissolve
( ethyl methyl , polyvinyl alcohol, PVP)

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20
Q

what is the function of disintegrate in a tablet?

A

to ensure the the tablet degredes in the GIT upon consumptions

absorbs water and swells
-cellulose, strach

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21
Q

what is the function of lubricants?

A

lubricant powers
reduced die and tablet fiction
ensure drug is blended well with other excipient
ejection from equipment

magnesium sterate
talc

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22
Q

what are glidants?

A

improve flow in equipment
uniformity
can affect dissolution/ bioavaility

talc
colloidal silicaon
magnesium oxide

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23
Q

what is the processs in wet granulation?

A

rinding/milling of drugs to reduce particle size →
blending with excipients →
addition of binder →
granulation →
drying →
blending with lubricants → compression

23
Q

what are examples of homopolymers?

A

PLA, PGA, povidone

24
Q

what is 0 order rate law ?
wha is the linear plot?
what is the slope and units of K?

A

rate=k
A vs t
-k and M/s

25
Q

what is 1 order rate law?
what is the linear plot?
what is slope and units?

A

rate= k[A]
ln[A] vs t
-k and 1/s

26
Q

what is second order rate law?
linear plot?
slope and units?

A

rate = k[A]^2
1/A vs T
k and 1/Ms

27
Q

what could increase reaction rate?

A

decrease in ionic strength with one positive and one negative ion

28
Q

what is immediate release?

A

drug release is immediate–> used when rapid onset of action is desired

29
Q

what is modified ER?

A

drug is released from dosage form occur slowly over time–> used for convenient dosingg to maintain plasma concentration over time

30
Q

what is modified delayed release?

A

drug release from the dosage form is delayed but still immediate–> used to protect acid labile drugs or stomach against irritation

31
Q

what is delayed released entering coating?

A

polymer degregation and drug release is pH dependent

32
Q

how are tablets usuallylly manufactured?
what is involved with wet granulation?

A

wet granulation

drugs ground to small pieces
small. volume is added to form granules

increase size but makes it more uniform

granules go thru a sieve to assure uniformity

33
Q

what must tablets go under for quality control?

A

rigorous testing like physical characterization and dissolution testing

34
Q

what is a binder?

A

bind powder particles into granules to impart uniformity– HPMC

35
Q

what is a diluents?

A

increase the bulk size of tablets to ease manufacturing, handling and swallowing–> lactose monohydrate

36
Q

what is processs for making hard capsules?

A

dipping–> spinning–> drying–> stripping–> cutting–joining

37
Q

what are polymers?
what affects their function?

A

applications ans excipients in. variety of dose forms

material composed of repeating units that link together

MW, composition, monomers properties

38
Q

what is homopolymers, block, random, and alternate copolymer?

A

homo: all the same
block: half/ half type 1 and 2

random: random ABABABbbb order

alternate: alternating ABABAB

39
Q

what are 3 mechanism to release drug from polymer?

A

diffusion, swelling, erosion

40
Q

what is diffusion mechanism for polymer?

A

contained in a cored & release depend on its diffusion rate thru the polymer

41
Q

wha is swelling mechanism for polymer?

A

drugs is dispersed in polymer matrix–> when water penetrates, it swells and creates pores that the drug goes thru

42
Q

what is erosion polymer mechanism?

A

surface: polymer is eroded from the surface

bulk: water penetrate the polymer and the p[olymer erodes throough

43
Q

polymers aren’t fully?
how does temp increase affect polymer?
how does MW affect this?

A

crystalline–> semi and have Tg

inc temp–> polymer transitions form glassy to rubbery liquid

inc MW–> inc Tg

44
Q

what increase bioavailability its, half life and avoids immonigenitcty of peptide drugs?

A

PEGlation, fusion proteins

lipidation
PLGA
inhaled & oral formulations

45
Q

as ionic strength increases, the reaction rate……

A

decreases

46
Q

what happens to protein therapies at air/ water interfaces?

A

can unfold at air/water interface & walls of storage vial

47
Q

what are the main barriers to oral delivery for protein & peptides?

A

low permeability and degefatin the GI due to acid/enzymes

48
Q

what can affect proteins function for degeneration pathways?

A

location of affected aa
oxidation of aa involved in bind may reducing binding affinity

aggregation can occur

49
Q

what is rybelsus?
what polymer does it use?

A

oral semiglutide

SNAC as abosrbance enchanter

50
Q

how does SNAC work?v
how is SNAC allow to pass thru gastric epithelium to circulation?
what is SNAC dependent on?

A

as tabel erodes–> causes local increase in pH leading to higher solubility & protect from degradation

transcellular absorption enchanting effect of SNAc

time and concentration dependent & is reversible

51
Q

what is the bioavaibilty of rybelssus with SNAC?

A

0.4-1%

52
Q

for lypohilization, what can be added as a protectant?

A

sucrose

53
Q

for cryo concentration, what ph is green and red, and what can be attest to adjunct tonicity?
what buffer can be used?

A

green at ph 7
red ph 4

sucrose

histidine

54
Q

what is the EPR effect?
why does this happen?
what are the blood vessels formed like?

what kind of lymph draining do tumors tissues have?

A

high MW non trageted drugs passively accumulate in tumors tissue

bo growing tumors need to rapidly generate new vasulatre for blood supply

abdornaml with badly aligned endothelial cells, so nanoparticles enter

poor

55
Q

what can still be used for active targeting of nano medicine products?

A

small molecule, peptides, proteins

Oral Dosage Forms— Modified Release (5 decks)

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