hw 4 study set Flashcards
rate of drug dissolution is ___ proportional to particle size?
inversely
what can pH deependant drug release be achieved by?
enteric coating (shellac)
what improves drug release?
reduction in size or unstirred boundary layer
what plays major role in killing infected cells of antibodies?
glycosltion pattern
what is solid phase peptide syntheis?
peptide assembling on resin
deprotection and cleavage
column purification
lyphoilization
ion exchange
lypholization
packing and labelling
(depreotection, coupling, cleavage)
are antifboy based therapeutics produced from E coli?
no, peptide products are like hGH
PEGylation increases half-life while albumin-conjugation decreases half-life of a
protein therapeutic
false, both increase HL
sustained release and immediate release tablets can both be split in half without
affecting their in vivo performance
false, can only split IR and SR can be harmful
If we know the buffer-less rate constant of degradation of a peptide drug at multiple
higher temperatures?
we can calculate its shelf life at its storage temperature in a
refrigerator
Monoclonal antibodies are composed of?
4 chains bonded through
cysteine amino acids by disulfide bonds
Hydrolysis and deamidation of proteins, both usually proceed ?
through succinimide
intermediates
Ethyl cellulose can be used as a polymer when you want drug release from a matrix
by swelling?
no it is a non-swelling, hydrophobic polymer that relies primarily on the diffusion of the drug through the polymer matrix
Semaglutide by itself has?
low solubility and low permeability
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.
true
what does effect of ionic strength on reaction rate k depend on?
the reaction rate constant depends on the nature of the reactants (charged vs neutral), the reaction mechanism, and the solvent.
what are natural polymers?
degradable in vivo, non toxic byproducts
chaargen, chitin, cellulose, strarch
what are semi snyheic polymers?
modified natural polymers
cellulose ethers, cellose acetates—
what are artificial polymers?
what are advanges?
artificial orgins, like rubbers, Dacron , plastic, PVS, PLGA, silicon
localize drug delivery
stabilization of drug
reduced side effects
what are hydrophobic philic, and hydrogel polymers?
non polar function groups
polar charged groups –water soluble (sodium, alginate, chitosan)
swell but do not dissolve
( ethyl methyl , polyvinyl alcohol, PVP)
what is the function of disintegrate in a tablet?
to ensure the the tablet degredes in the GIT upon consumptions
absorbs water and swells
-cellulose, strach
what is the function of lubricants?
lubricant powers
reduced die and tablet fiction
ensure drug is blended well with other excipient
ejection from equipment
magnesium sterate
talc
what are glidants?
improve flow in equipment
uniformity
can affect dissolution/ bioavaility
talc
colloidal silicaon
magnesium oxide
what is the processs in wet granulation?
rinding/milling of drugs to reduce particle size →
blending with excipients →
addition of binder →
granulation →
drying →
blending with lubricants → compression
what are examples of homopolymers?
PLA, PGA, povidone
what is 0 order rate law ?
wha is the linear plot?
what is the slope and units of K?
rate=k
A vs t
-k and M/s
what is 1 order rate law?
what is the linear plot?
what is slope and units?
rate= k[A]
ln[A] vs t
-k and 1/s
what is second order rate law?
linear plot?
slope and units?
rate = k[A]^2
1/A vs T
k and 1/Ms
what could increase reaction rate?
decrease in ionic strength with one positive and one negative ion
what is immediate release?
drug release is immediate–> used when rapid onset of action is desired
what is modified ER?
drug is released from dosage form occur slowly over time–> used for convenient dosingg to maintain plasma concentration over time
what is modified delayed release?
drug release from the dosage form is delayed but still immediate–> used to protect acid labile drugs or stomach against irritation
what is delayed released entering coating?
polymer degregation and drug release is pH dependent
how are tablets usuallylly manufactured?
what is involved with wet granulation?
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
what must tablets go under for quality control?
rigorous testing like physical characterization and dissolution testing
what is a binder?
bind powder particles into granules to impart uniformity– HPMC
what is a diluents?
increase the bulk size of tablets to ease manufacturing, handling and swallowing–> lactose monohydrate
what is processs for making hard capsules?
dipping–> spinning–> drying–> stripping–> cutting–joining
what are polymers?
what affects their function?
applications ans excipients in. variety of dose forms
material composed of repeating units that link together
MW, composition, monomers properties
what is homopolymers, block, random, and alternate copolymer?
homo: all the same
block: half/ half type 1 and 2
random: random ABABABbbb order
alternate: alternating ABABAB
what are 3 mechanism to release drug from polymer?
diffusion, swelling, erosion
what is diffusion mechanism for polymer?
contained in a cored & release depend on its diffusion rate thru the polymer
wha is swelling mechanism for polymer?
drugs is dispersed in polymer matrix–> when water penetrates, it swells and creates pores that the drug goes thru
what is erosion polymer mechanism?
surface: polymer is eroded from the surface
bulk: water penetrate the polymer and the p[olymer erodes throough
polymers aren’t fully?
how does temp increase affect polymer?
how does MW affect this?
crystalline–> semi and have Tg
inc temp–> polymer transitions form glassy to rubbery liquid
inc MW–> inc Tg
what increase bioavailability its, half life and avoids immonigenitcty of peptide drugs?
PEGlation, fusion proteins
lipidation
PLGA
inhaled & oral formulations
as ionic strength increases, the reaction rate……
decreases
what happens to protein therapies at air/ water interfaces?
can unfold at air/water interface & walls of storage vial
what are the main barriers to oral delivery for protein & peptides?
low permeability and degefatin the GI due to acid/enzymes
what can affect proteins function for degeneration pathways?
location of affected aa
oxidation of aa involved in bind may reducing binding affinity
aggregation can occur
what is rybelsus?
what polymer does it use?
oral semiglutide
SNAC as abosrbance enchanter
how does SNAC work?v
how is SNAC allow to pass thru gastric epithelium to circulation?
what is SNAC dependent on?
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
what is the bioavaibilty of rybelssus with SNAC?
0.4-1%
for lypohilization, what can be added as a protectant?
sucrose
for cryo concentration, what ph is green and red, and what can be attest to adjunct tonicity?
what buffer can be used?
green at ph 7
red ph 4
sucrose
histidine
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?
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
what can still be used for active targeting of nano medicine products?
small molecule, peptides, proteins
