Description about the

pharmacokinetics of drug
absorption model
Submitted by
Most. Sonia Khatun
Roll: 559
Batch: 19th
Department of Pharmacy
World University of Bangladesh
Contents
• Introduction
• Factors affecting systemic drug absorption
• Plasma level time curve
• Absorption phase
• Peak absorption phase
• Post absorption phase
• Elimination phase
• Drug absorption model
• Zero order absorption model
• First order absorption model.
Introduction

• In pharmacokinetics, the overall rate of drug absorption

may be described as either a first-order or a zero-order
input process. Most pharmacokinetic models assume
first-order absorption unless an assumption of zero-order
absorption improves the model significantly or has been
verified experimentally.
Factors affecting systemic drug absorption
• The absorption of drug from GIT or any other extravascular site is dependent on
the following factors:
• Physicochemical properties of the drug.
• Dosage form of drug.
• Route of administration.
• Anatomy and physiology of the absorption site.
• Surface area of GIT.
• Stomach emptying rate.
• GI motility.
• Blood flow to the absorption site.
Plasma level time curve
• After drug administration, the rate of change in the amount of drug in
the body (dDB/dt) is dependent on the rate of drug absorption and rate
of drug elimination.

• So the rate of drug accumulation in the body at any time is equal

to the rate of drug absorption minus the rate of drug elimination.
As a result drug concentration attain in plasma.
 Plasma level time curve

Where, DGI is amount of drug in the gastrointestinal tract.

D is amount of drug eliminated.
E

A plasma level time curve can be obtained by

plotting the plasma drug concentration versus time
and the absorption phase and elimination phase can
be observed. The drug absorption and elimination
phases of the curve are shown in the curve:
Figure: A Plasma level–time curve for a drug given in a single oral dose.
Plasma level time curve
1. Absorption phase: During the absorption phase of a plasma level–
time curve, the rate of drug absorption is greater than the rate of
drug elimination. So in this phase drug increase in the plasma
gradually.

Note that during the absorption phase, elimination occurs whenever

drug is present in the plasma, even though absorption predominates.
2. Peak absorption phase: At the time (tmax) of peak drug concentration (Cmax) in the
plasma, the rate of drug absorption just equals the rate of drug elimination, and there is
no net change in the amount of drug in the body.

3. Post absorption phase: Immediately after the time of peak drug absorption (tmax),
some drug may still be at the absorption site (i.e, in the GI tract or other site of
administration).
The rate of drug elimination at this time is faster than the rate of absorption (the
postabsorption phase). However in this stage the rate of drug elimination is faster than
the rate of drug absorption.
4. Elimination phase: When the drug at the absorption site becomes
depleted, the rate of drug absorption (dD /dt) approaches becomes zero
GI

or very less. The plasma level–time curve (now the elimination phase)
then represents only the elimination of drug from the body, which is a
first order process. During the elimination phase the rate of change in the
amount of drug in the body is described as a first-order process.

Where, k is the first-order elimination rate constant.

Figure- Linear Plot of Cp versus Time after Oral

Administration
DRUG ABSORPTION MODEL:
•Drug absorption and over all elimination in the body can be described by a model is
call drug absorption model.
 Most pharmacokinetic models assume first-order absorption unless an
assumption of zero-order absorption improves the model significantly or has been
verified experimentally.
 The rate of change in the amount of drug in the body, dDB/dt, is dependent on the
relative rates of drug absorption and elimination.
 The net rate of drug accumulation in the body at any time is equal to the rate of
drug absorption less the rate of drug elimination.
• Over all drug absorption can be described by two model:
• Zero order absorption model
• First order absorption model.

•Zero order process: It can be defined as the process whose rate is independent of
concentration of drug undergoing reaction that is the rate of reaction cannot be increased
by further increase in concentration of reactants.

•First Order process: It is the process whose rate is directly proportional to concentration
of the drug undergoing reaction that is greater the concentration faster the reaction
process.
Zero-Order Absorption Model:

 In zero-order absorption model – drug is absorbed from GIT at zero-order process

(k ) and eliminated at first order process (k).
0

 Zero-order drug absorption from the administration site into the plasma usually
occurs when either the drug is absorbed by a saturable process or a zero-order
controlled-release delivery system is used.
 The pharmacokinetic model assuming zero-order absorption is described here.
 In this model, drug in the gastrointestinal tract, D , is absorbed systemically at a
GI

constant rate, k .
0
• One-compartment pharmacokinetic model for zero-order drug
absorption and first-order drug elimination:

• Drug is simultaneously and immediately eliminated from the

body by a first-order rate process defined by a first-order rate
constant, k.
• This model is analogous to that of the administration of a drug
by intravenous infusion.
First-Order Absorption Model
• Absorption of most drug is usually assumed to be a first order process.
• This model assumes a first-order input from the GIT by absorption
rate constant (k ) .
a

• First-order elimination from the body by rate constant k.

One-compartment pharmacokinetic model for first-

order drug absorption and first order elimination.
•Application: This model applies mostly to the oral absorption of drugs
in solution or rapidly dissolving dosage (immediate release) forms such
as tablets, capsules, and suppositories and drugs given by IM or SC
aqueous injections.
Sir