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