Pharmacokineti Pharmacodyna

c methods mic methods

Plasma level Acute

time studies pharmacologi
cal response

Urinary
Therapeutic
excretion
response
studies
Collection of serial blood
samples for a period of 2-3
biological half-lives after
drug administration

Plot of concentration v/s time

to obtain the plasma level
time profiles

At least 3 points should be

taken on the ascending part
of the curve for accurate
determination of ka
Drug administration for atleast 5 biological half-
lives with a dosing interval equal to or greater
than the biological half-lives to reach the steady
state

A blood sample should be taken at the end of

previous dosing interval & 8-10 samples after
the administration of the next dose
Plot of urinary excretion rate versus time
The extent of bioavailability is calculated by these
equations :
1. Single dose :

𝑋𝑢∞ 𝐷 𝑖𝑣
F= 𝑜𝑟𝑎𝑙
𝑋𝑢∞ 𝑖𝑣
𝐷 𝑜𝑟𝑎𝑙

𝑋𝑢∞ 𝐷 𝑠𝑡𝑑
Fr = 𝑡𝑒𝑠𝑡
𝑋𝑢∞ 𝑠𝑡𝑑
𝐷 𝑡𝑒𝑠𝑡

2. Multiple dose:
𝑋𝑢 𝑠𝑠 𝑡𝑒𝑠𝑡 𝐷 𝑠𝑡𝑑 τ 𝑡𝑒𝑠𝑡
Fr = ,
𝑋𝑢 𝑠𝑠 𝑠𝑡𝑑 𝐷 𝑡𝑒𝑠𝑡 τ 𝑠𝑡𝑑
,
 Class Solubility Permeability IVIVC Possibility of
Expectations for immediate-release predicting IVIVC
product from dissolution
data
I High High IVIVC expected, if dissolution rate is slower Yes
than gastric emptying rate, otherwise limited
or no correlation.
II Low High IVIVC expected, if in vitro dissolution rate is Yes
similar to in vivo dissolution rate, unless dose
is very high.
III High Low Absorption (permeability) is rate determining No
and limited or no IVIVC with dissolution.

IV Low Low Limited or no IVIVC is expected. No

Class Solubility Permeability IVIVC

Ia High and site independent High and site independent IVIVC Level A expected

Ib High and site independent Dependent on site and narrow absorption IVIVC Level C expected
window

IIa Low and site independent High and site independent IVIVC Level A expected

IIb Low and site independent Dependent on site and narrow absorption Little or no IVIVC
window

Va; Acidic Variable Variable Little or no IVIVC

Vb; Basic Variable Variable IVIVC Level A expected