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PHRD5925 Pharmaceutics Lecture 11 - Drug Absorption (Part 1)
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5 physiological factors affecting oral drug absorption
1) surface area
2) GI pH
3) gastric emptying
4) effects of food
5) absorption mechanisms
what part of the GI has the highest surface area?
ileum of the SI
rank GI surface area
ileum > jejunum > duodenum > stomach
drug form that is more lipid soluble & better (passively) transported
UN-ionized
3 parameters involved in the pH-partition theory
1) pKa (dissociation constant)
2) pH
3) lipid solubility (partition)
pH in relation to drug absorption from stomach
ABSORBED
: weak acidic, neutral
NOT ABSORBED
: basic
pH in relation to drug absorption from the intestine
ABSORBED
: weak basic and neutral
NOT ABSORBED
: acidic
Henderson-Hasselbalch equation
Acid
:
Base:
for a given pKa, _____ (increasing/decreasing) pH increases absorption of a weak acid
decreasing
for a given pKa, _____ (increasing/decreasing) pH increases absorption of a weak
base
increasing
normal low bulk or liquid intake takes ____ min to empty from the stomach
20-60min
effect of delayed stomach emptying on the rate of drug absorption
reduced rate of drug absorption
effect of hot contents on gastric emptying rate
increased emptying rate
effect of aggression on gastric emptying rate
increased rate
effect of lying on left hand side on gastric emptying rate
decreased rate
when increased rate of gastric emptying has a favorable effect (2)
1) well soluble drugs
2) drugs degraded in stomach
when decreased gastric emptying rate has a favorable effect (2)
1) poorly soluble drugs
2) drugs transported by carriers
the quicker the stomach emptying, the ____ the plasma concentration
higher
3 ways food effects drug absorption
1) delayed gastric emptying
2) pH change
3) physical/chemical interaction of food w/ drug
- absorption occurs by passing
through
the intestinal cells
- most significant route of drug transport
passive transcellular transport
- absorption occurs by transport
between
intestinal cells (aqueous tight junctions)
- small hydrophilic cations are best candidates
passive paracellular transport
what happens to tight junctions from the SI to colon?
junctions become progressively tighter
best candidates for transcellular transport
small, amphipathic drugs
major example of an efflux transporter
p-glycoprotein (P-gp)
Author
daynuhmay
ID
271257
Card Set
PHRD5925 Pharmaceutics Lecture 11 - Drug Absorption (Part 1)
Description
Drug Absorption
Updated
2014-04-21T00:17:46Z
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