7. • Rate: how rapidly does the drug get from
its site of administration, to the general
circulation?
• Extent: How much of the administered
dose enters the general circulation (per cent
bioavailability = F)?
8.
9.
10. Absorption of Drugs
1. Sites of absorption through the GI tract
2. Factors that modify absorption in the GI tract
3. Bioavailability
4. Other sites of drug administration/absorption
10
11. Absorption of Drugs
1. Sites of absorption through the GI tract
1) Mouth
2) Stomach
3) Small intestine
4) Large intestine
11
12. Absorption of Drugs
2. Factors that modify absorption in the GI tract
1) Drug solubilization
2) Ph of the medium
3) Lipid solubility of the drug
4) Blood flow at the absorption site
5) Surface area of absorption
6) Route of administration (First Pass Effect in Oral Route)
7) Gastric emptying
8) Food
9) Intestinal motility
10) Metabolism of drug by GI tract
12
13. Absorption of Drugs
Factors that modify absorption in the GI tract
Drug solubilization – breaking drugs into smaller, more
absorbable particles
.
DISINTEGRATION (solid )
⇓
DISSOLUTION (solution)
⇓
ABSORPTION
⇓
SYSTEMIC CIRCULATION (% bioavailability)
13
14. Ph of the medium
stomach (pH 1~3)
in favour of weak acid
absorption
duodenum (pH 5~7)
in favour of weak base
absorption
ileum (pH 7~8)
in favour of weak base
absorption
15. pH and ionization
Acidic drugs are best absorbed in Acidic
medium
Basic drugs are best absorbed in Basic
medium
16. Gastric emptying
small intestine – primary site of drug absorption
Anything that delays/accelerates gastric emptying will
decrease/increase drug absorption.
Food
High fat food – delay gastric emptying – slow
absorption
16
19. Bioavailability of a drug
• The bioavailability of a drug (by a route
other than intravenous) is given by:
AUC (extra vascular)
• F= -----------------------------
AUC (intravenous)
Notas do Editor
The action of the body on the drugs The way the body handles drugs determines the dose, route and frequency of administration The handling of drugs by the body can be split into absorption, distribution and elimination
Rate of absorption determines the time to the peak concentration The extent of absorption determines the height of the peak concentration
1 1 1 1
AUC is an index of the total amount of drug absorbed systemically.