Topik 4

Kinetics is important in all phases of the drug

development process as well as in quality
control, stability, bioavailability, and therapeutic
drug monitoring.
Drug kinetics
(pharmacokinetics) describes how the
body handles a drug and accounts for the
processes of absorption, distribution,
metabolism, and elimination.

Drug treatment requires getting a drug to its specific

target site or sites in tissues where the drug performs
its action. Typically, the drug is introduced into the
body (the process of administration), sometimes far
from this target site. The drug must move into the
bloodstream (the process of absorption) and be
transported to the target sites where the drug is
needed (the process of distribution). Some drugs are
chemically altered (the process of metabolism) by the
body before they perform their action, others are
metabolized afterward, and still others are not
metabolized at all. The final step is the removal of the
drug and its metabolites from the body (the process
of elimination).

Many factors, including a persons weight,

genetic makeup, and kidney or liver function,
can influence these kinetic processes

 Drug dissolution from dosage forms that do not

disaggregate and release the drug slowly can be
represented by the equation:
Rearrangement of equation (3) yields:
Where Qt is the amount of drug dissolved in time
t, Q0 is the initial amount of drug in the solution
(most times, Q0 = 0) and K0 is the zero order
release constant expressed in units of
concentration/time.
(Dash, Suvakanta, 2010)

 To study the release kinetics, data obtained from

in vitro drug release studies were plotted as
cumulative amount of drug released versus time.
Application: This relationship can be used to
describe the drug dissolution of several types of
modified release pharmaceutical dosage forms,
as in the case of some transdermal systems, as
well as matrix tablets with low soluble drugs in
coated forms, osmotic systems, etc.
(Dash, Suvakanta, 2010)

The term k is the zero-order

rate constant and is expressed
in units of mass/time (eg,
mg/min).
Integration
of
Equation 2.19 yields the
following expression:

where A 0 is the amount of drug

at t = 0. Based on this
expression , a graph of A
versus t yields a straight line .
The y intercept is equal to A 0,
and the slope of the line is equal
to k 0.

First orde reaction

pharmacetic reactions that often
happen such as: drug absorption
and degradation of the drug
Speed of reaction is influenced by
the concentration of the reactants

d C

kc
dt

t
dC
c0 c k 0 dt
ln c ln c0 k (t 0)
c

ln c ln c0 kt
log c log c0 kt

Martin, 1993

2,303

Half life (t1/2)

The time it takes to decay/loss of substance,
became half.
For a first-order:

0,693
t1 / 2
k
Martin, 1993

Time Expired (t90)

Time a substance has been broken down to live
to 90% of the initial concentration (i.e., breaks
down 10%).
For a first-order:

0,105
t90
k

Martin, 1993

konsentrasi

Log konsentrasi

Plot the concentration and log

concentration against time

waktu

Kemiringan
2,303/k

waktu
Martin, 1993

Differences between zero-order kinetics

and Fist order kinetics

(Rao,Koteswara,G.S.N)

(Rao,Koteswara,G.S.N)