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Pharmacokinetics
3st presentation
Lecturer: Dr. Muslim Suardi, M.Si,
Apt
Kelompok 2
1.Nova Lestari
2.Rama saputri
3.Anna fadhila
4.Nur Azlin
5.Suci Dita Ramadhani
(1411011043)
(1411011046)
(1411011049)
(1411011061)
(1401101164)
Bioavailability
The fraction of an administered dose of
medication that reaches the systemic
circulation
When the drug is administered
intravenously, bioavailability is 100%.
However, when a medication is
administered via other routes (such as
by mouth), its bioavailability decreases
Goodman&Gilmans.2010.
(due to incomplete absorption
& FPM).
Definition
Bioavailability is a measurement of
the rate & extent of a therapeutically
active drug that reaches the
systemic circulation & is available at
the site of action.
Goodman&Gilmans.2010.
BIOAVAILABILITY
The extent and the rate to which a drug
substance or its therapeutic moiety is
delivered from a pharmaceutical form into the
general circulation
absolute bioavailability
relative bioavailability
Goodman&Gilmans.2010.
Absolute bioavailability
Goodman&Gilmans.2010.
Absolute bioavailability
In order to determine absolute bioavailability
of a drug, a pharmacokinetic study must be
done to obtain a plasma drug concentration vs
time plot for the drug after both IV and non-IV
dministration.
Goodman&Gilmans.2010.
The absolute bioavailability is the dosecorrected AUC non-IV divided by AUC IV.
Ex: the formula for calculating F for a drug
administered by the oral route (po) is given
below.
Therefore, a drug given by the IV route will
have an absolute bioavailability of 1 (F=1)
while drugs given by other routes usually
have an absolute bioavailability of < 1.
Goodman&Gilmans.2010.
ABSOLUTE BIOAVAILABILITY
AUCoral DOSEiv
F
Goodman&Gilmans.2010.
Relative bioavailability
This measures the bioavailability of the a certain
drug when compared with another formulation
of the same drug, usually an established
standard, or through administration via a
different route. When the standard consists of
IV-ly administered drug, this is known as
absolute bioavailability.
R.S.Satoskar,2011.
RELATIVE BIOAVAILABILITY
tablet A
AUC formA
Frel
AUC formB
tablet B
R.S.Satoskar,2011.
ADME
The four criteria all influence the drug levels &
kinetics of drug exposure to the tissues & hence
influence the performance & pharmacological
activity of the compound as a drug:
Absorption
Before a compound can exert a
pharmacological effect in tissues, it has to be
taken in to the bloodstream usually via
mucous surfaces like the digestive tract
(intestinal absorption). Uptake into the target
organs or cells needs to be ensured, too. This
can be a serious problem at some natural
barriers like the blood-brain barrier. Factors
such as poor compound solubility, chemical
instability in the stomach, and inability to
permeate the intestinal wall can all reduce the
extent to which a drug is absorbed after oral
administration. Absorption critically determines
(Verma et. al, 2010)
the compound's bioavailability.
Distribution
The compound needs to be carried to its effector
site, most often via the bloodstream. From there,
the compound may distribute into tissues and
organs, usually to differing extents.
Metabolization
Compounds begin to be broken down as soon as they
enter the body. The majority of small-molecule drug
metabolism is carried out in the liver by redox
enzymes, termed cytochrome P450 enzymes. As
metabolism occurs, the initial (parent) compound is
converted to new compounds called metabolites.
When metabolites are pharmacologically inert,
metabolism deactivates the administered dose of
parent drug and this usually reduces the effects on the
body. Metabolites may also be pharmacologically
active, sometimes more so than the parent drug
(Verma et. al, 2010)
Excretion
Compounds and their metabolites need to be
removed from the body via excretion, usually
through the kidneys (urine) or in the feces.
Unless excretion is complete, accumulation of
foreign substances can adversely affect normal
metabolism.
Reference
R.S.Satoskar,2011.Pharmacology and
Parmacotherapeutics second edition.Popular
Prakashan
Goodman&Gilmans.2010.The pharmacological
Basis of Therapeutics 12th edition.Laurence
Brunton
Verma, P., et al. 2010. Routes of Drug
Administration. International Journal
of Pharmaceutical Studies and
Research. India: Technical Journal
Online.