Oral Absorption Flashcards
What are the 3 definitions of absorption?
- Absorption occurs when drug reaches the systemic circulation
- When drug reaches the portal veins blood stream
- Drug is assumed to be absorbed when it leaves the lumen and crosses the apical membrane of the enterocytes lining the intestine
What are the factors that affect drug absorption?
- Physiochemical properties of drug and environment of small intestine
- Dosage form
- Anatomy and physiology of absorption site
What are the properties of the absorption site an can effect drug absorption?
- SA or GIT
- Stomach emptying rate
- GI motility
- Blood flow to absorption site
What are the studies of absorption kinetics?
- Top-down
- Bottom-up
What is the difference between top-down and bottom-up?
TD: Based on observed clinical data
BU: Based on the broader understanding of the human body and its mechanism
What is the top-down approach?
- Based on compartmental models
What is the bottom-up approach?
- Small elements of system are defined in great detail
- Smaller elements are combined into subsystems, and systems to describe overall process
- More complicated approach with many variables
What is the goal of top-down and bottom-up methods?
To make plausible physiologic predictions
Describe the PK of drug absorption?
- Can be 1st or 0
- Rate of drug amount is dependent of rates of elimination and absorption
- Net rate of drug accumulation is body is equal to the rate of absorption less than elimination regardless of 0 or 1st order
What is the equation for PK drug absorption?
What is the absorption phase?
- Rate of drug absorption is greater than the rate of drug elimination
- Elimination phase still occurring during absorption phase
What is the peak-drug concentration?
- Rate of drug absorption equals the rate of drug elimination
- No net change in the amount of drug in the body
What is post-absorption phase?
- Immediately after peak drug absorption
- Some drug is still absorbed
- Rate of drug elimination is faster than rate of absorption
What is the elimination phase?
- Drug at the absorption site becomes deplete
- The rate of drug absorption approaches 0
- Curve represents elimination only
- First order
Identify the phases of drug absorption
A: Absoprtion
B: Peak drug concentration
C: Post absorption
D: Elimination
What is are the factors that effect the rate of absorption?
- Drug dissolution
- GI motility
- Blood flow
- Drug transport across membranes