Final Exam (Lecture #01) Flashcards
(42 cards)
Causes of ulcer
NSAID, H Pylori, smoking, too much booze, genetics, mental stress
Why should you not take NSAID right before going to bed?
b/c not much GI movement overnight, drug dissolves and stays in intestines for longer period of time and irritates the mucosa
3 examples of acid labile drugs
Erythromycin, omeprazole, pancrelipase
Mesalamine (Asacol EC)
- anti-inflammatory drug enteric coated for colonic delivery for Tx of UC, Cronh’s
- local effect, not systemic - you want low bioavailability so that it works inside the colon membrane
Cellulose acetate phthalate
- type of enteric coating
- pH sensitive, soluble polymer
- acidic - that’s why they don’t dissolve in the stomach
Hydroxypropyl methylcellulose acetate succinate
- type of enteric coating
- pH sensitive, soluble polymer
- acidic - that’s why they don’t dissolve in the stomach
Ethyl cellulose
- type of controlled release coating
- pH independent, insoluble polymer, permeable or semi-permeable
Polyvinyl acetate
- type of controlled release coating
- pH independent, insoluble polymer, permeable or semi-permeable
HPMC (hydroxypropyl methylcellulose)
- subcoat layer when dealing with an acid labile compound
- adherent that helps API solution stick to the sugar bead
Triethyl citrate
- plasticizer
- provides strength
Talc
facilitates coating process
Extrusion and spheronization process
- used to make oblong shaped mini tablets
- these do NOT use sugar beads
- can be used for large dose drugs (whereas sugar beads would be used for small dose drugs)
USP Apparatus 2
-dissolution machine
Accetable drug release from EC drug in dissolution machine in 2 hours?
5-10%
Main reason for variation in drug absorption times in population?
-different gastric emptying
n = 0.5
n= 1
0.5 < n < 1
n = 0.5 –> pure diffusion
n= 1 –> best balance of diffusion & erosion
-zero order; amt released per unit time is constant
0.5 < n < 1 –> combination of diff & erosion
Metformin HCl
- tablet with no coating
- if placed in a solution, tablet swells with gel layer then dissolves
- infiltrated layer directly adjacent to tablet exterior gradually becomes a gel –> more and more tablet is being converted to a gel over time
2 drugs that do NOT follow linear kinetics?
phenytoin and alcohol. Drugs that don’t follow linear kinetics CANNOT be designed as CR
Cause of alcohol on a CR tablet
ethanol causes faster release of API from a CR tab –> dose dumping
AND/OR
could influence metabolism of drug (liver enzymes occupied by ethanol)
Embeda
Morphine sulfate and naltrexone
- tamper resistant formula
- natrexone completely coated by impermeable ethyl cellulose so you can’t separate and extract the morphine, if you grind up the pill you’d mix the naltrexone into the morphine which would inhibit the effects of morphine
Toprol-XL
pellets in tablet
Allegra
layered
Diltiazem HCl
- triple layer tablet
- barriers layers prevent water from dissolving on the top and bottom of the tablet, so drug is only released from the sides
Procardia XL
osmotic pump
