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92 Cards in this Set

  • Front
  • Back
buccal pH
7
buccal membrane
thin
buccal blood flow
good
buccal SA
small
buccal transit time
short unless controlled
buccal bypass liver
yes
esophagus pH
5-6
esophagus membrane
thick
esophagus SA
small
esophagus transit time
short
stomach pH
1-3
stomach membrane
normal
stomach blood flow
good
stomach SA
small
stomach time
30-40 min
stomach bypass liver
no
stomach enzymes
pepsinogen, gelatinase, lipase
duodenum pH
6-6.5
duodenum membrane
normal
duodenum blood
good
duodenum SA
very large
duodenum transit time
short
duodenum bypass liver
no
duodenum enzymes
trypsin, chymotrypsin, elastases, carboxypeptidases
SI pH
7-8
SI membrane
normal
SI blood
good
SI SA
very large
SI transit time
3 hours
SI bypass liver
no
SI enzymes
disaccharises, peptidases, lipases
LI pH
5.5-7
LI blood
good
LI SA
not large, 4-5 ft
LI transit time
24 hours
LI bypass liver
yes
TOI seconds
IV inj
TOI minutes
IM, SC, SL, aerosols, gas
TOI minutes to hours
short term depot injections, sol, powder, granules, capsules, tablets, SR tablets
TOI hours
EC tablets
TOI days
depot, implants
TOI varies
topicals
cydot
backing, rate-limiting membrane, mucoadhesive
enhance permeability
organic solvents, chelating agents, surfactants and detergents, lysolecithin, antibiotics, proteins
factors that affect dissolution
SA, h, D, Cs, crystal form, GI motility
empty 50% stomach
2.5-3 hours
empty all of stomach
4-5 hours
empty 50% SI
2.5-3 horus
time in colon
30-40 hours
biological barriers to oral drugs
bacterial degradation
enzymatic degradation
first pass
immunological
physciochemical barriers to oral drugs
chemical degradation
thermodynamics
partitioning, extent, rate
absorption, molecular size, solubility/dispersability
physiological variables to oral drugs
PM 3Gs SLB
pH, membrane permeability, gut wall metabolism, Gi motility, GI secretions, site specific absorption, luminal contents, blood flow
capsule 000
1200 mg lactose
capsule 2
350 lactose
capsule 3
270 mg lactose
soft geletin capsules
LC, liquigels, sequels, perles
official capsule tests
content uniformity
weight variation
disintegrationi
dissolution
CT
compressed tablet
SCT
sugar coated tablet
FCT
film coated tablet
ECT
enteric coated tablet
MCT
multiple compressed tablet
DT
dispersing tablet
diluent
adds bulk
binders
helps with flow
disintegrators
hydrophilic
lubricant
hydrophobic, magnesium stearate
glidants
improve flow
absorbents
volatile oil are absorbed
coloring agents
FD&C approved, soluble dyes, insoluble pigments, lakes
flavoring agents
sugar and flavoring, taken up like volatile oils
tablet tests
thickenss
frialibility
weight variation
hardness
disintegraton
content uniformity
dissolution
weight variation
10%- <130 mg
7.5%- 131-324 mg
5% >325 mg
common tablet problems
capping
lamination
chipping
picking
stress cracking
types of oral release
quick
immediate
delayed
sustained
controlled
quick release tablets
on tongue or SL
low dose
rapid onset
dissolve rapidly in mouth
approaches for quick release
effervescent
amorphous water-soluble granules
why delayed release
avoid release in stomach, if you deliver drugs to the lower intestine you can avoid the stomach and SI
why sustained release
better compliance
less side effects
sustained pharmacodynamic response
enhanced bioavailability
LA
long acting
SA
sustained action
SR
sustained release
TR
time release
ER
extended release
stealth concept
PEG looks like self, small enough to leak out of capillaries at correct site of action
approaches to sustained release
monolithic, multiparticulate system
mechanisms of controlled release systems
diffusion
solvent-activated
polymeric degradation
diffusion controlled release
polymeric matrix or polymeric membrane
solvent-activated
pressure forces durg out
**predetermined also has a membrane, may be ec or fast release drug
polymeric degradation
drug in polymer membrane or matrix and is released when polymer breaks down
polymer degradation mechanisms
cross linking is removed causing solubility to increase, water insoluble polymers are made water soluble by hydrolysis or ionization of side group, polymer broken into monomers
challenges of oral drug delivery
API dissolution and permeability,
stomach stability,
pre-systemic metabolism and efflux, biological macromolecular oral delivery