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For drug with very poor aqueous solubility, the rate at which it
_______.
Rate limiting step: __________ (drug crosses the GI membrane)
The rate of release of drug from the dosage form (i.e. controlled-release
dosage form)
Solubility
The rate at which the stomach empties the drug into the small intestine
Permeability
cells
The rate of metabolism during its initial passage through the liver.
6 Sep 2016
stomach.
Thick, 250 mm long and 20 mm
in diameter
Contains squamous epithelium of
non-proliferative cells.
Secrete mucus into lumen to
pH 5-6
Rapid transit of dosage forms,
2 major functions:
to act as a temporary
reservoir for ingested food
and to deliver it to the
duodenum at a controlled
rate;
to reduce ingested solids to
a uniform creamy
consistency, by the action
of acid and enzymatic
digestion.
6 Sep 2016
Parts:
Duodenum (200-300
mm)
Jejunum (2 m)
Ileum (3 m)
Folds of Kerckring
Villi: finger-like projections into
6 Sep 2016
pH 6-7.5
Apprx 1.5 m
Secretions:
Brunners glands (duodenum):
bicarbonate
Intestinal cells: mucus and enzymes
Pancreatic secretions: NaHCO3
and enzymes (proteases, principally
trypsin, chymotrypsin &
carboxypeptidases, lipase,
amylases)
Bile: secreted by hepatocytes in the
liver into bile canaliculi,
concentrated in the gallbladder and
hepatic biliary system.
Functions
Absorption of Na+, Cl-, and
H2) from the lumen in
exchange for HCO3 and K
ions.
Storage and compaction of
feces.
pH 6-6.5 to 7-7.5
Gastric emptying
Small Intestinal transit
Colonic transit
rate.
Highly variable and is dependent on the dosage form and the fed/fasted state of the
stomach.
Generally, drugs are between absorbed in the small intestine than in the
(MMC) the electrical activity in the stomach that governs transit of dosage form.
6 Sep 2016
Increase
Decrease
Volume
Large volume
(initial)
Type of meal
Warm food
Body position
Standing, supine
Drugs
Metoclopramide
Anticholinergics, narcotics,
analgesics, propantheline
Emotional
state
Aggression, stress
Depression
Exercise
Disease
After exercise
Hyperthyroidism
Parkinsons