Biopharmaceutics

&
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).

Bioavailability is the fraction of

administered drug that reaches the
systemic circulation.
Bioavailability is expressed as the
fraction of administered drug that gains
access to the systemic circulation in a
chemically unchanged form.
Goodman&Gilmans.2010.

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.

Determination of bioavailability: Bioavailability is determined by

comparing plasma levels of a drug after a particular route of
administration (for example, oral administration) with plasma
drug levels achieved by IV injection in which all of the agent
rapidly enters the circulation.

When the drug is given orally, only part of the administered

dose appears in the plasma
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

Absolute bioavailability measures the availability

of the active drug in systemic circulation after
non-IV (i.e., after oral, rectal, transdermal,
subcutaneous administration).

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

AUCiv DOSE oral

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.

Factors influencing bioavailability

The absolute bioavailability of a drug,
when administered by an extravascular
route, is usually <1.
Various physiological factors reduce the
availability of drugs prior to their entry
into the systemic circulation.
Such factors may include, but are not
limited to:
poor absorption from the GIT
Degradation/metabolism of drug
prior to
R.S.Satoskar,2011.
absorption

Factors influencing bioavailability

Each of these factors may vary from
patient to patient, and indeed in the same
patient over time. Whether a drug is taken
with or without food will affect absorption,
other drugs taken concurrently may alter
absorption & FPM, intestinal motility alters
the dissolution of the drug & may affect
the degree of chemical degradation of the
drug by intestinal microflora.
Disease states affecting liver metabolism
or GI function will also have an effect.
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:

(Verma et. al, 2010)

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.

(Verma et. al, 2010)

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.

(Verma et. al, 2010)

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.