BIOAVAILABILITY

Honeylene B. Paloma, RPh.

BIOAVAILABILITY, F
Is the rate and
extent (amount) to
which the active
ingredient or moiety
is systemically
absorbed or
becomes available
at the site of action.

It is determined by
the drugs
concentration time
curve in the
systemic circulation
or by its excretion in
the urine.

BIOAVAILABILITY, F
After IV administration, F is equal to unity
(1.0 or 100%) because the entire dose
enters the systemic circulation. The drug
is considered to be completely available
after IV admin.
After Oral or other extravascular route of
admin of a drug, F may vary from a value
of 0 (No drug absorption) to 1 (complete
drug absorption).

BIOAVAILABILITY, F
To calculate the amount of drug
absorbed, the administered dose
should be multiplied by a
bioavailability factor.
Amount of
Drug absorbed = bioavailability factor
(F) x Dose (D)

BIOAVAILABILITY, F
Amount of
Drug absorbed = bioavailability factor
(F) x Dose (D)
Example: The bioavailability of digoxin is
estimated to be 0.62 for orally administered
tablets. This means that if 250mcg of
digoxin is given orally, the effective or
absorbed dose can be calculated as:

BIOAVAILABILITY, F
There are some factors which must be
considered
when
estimating
the
bioavailability of a drug.
*Bioavailability can vary among different
formulations and dosage forms of a
drug.

BIOAVAILABILITY, F
For example, digoxin elixir has a F of 0.77
while for tablets F is 0.62. When it is
given parenterally, F is usually
considered as 1.0.
This principle can be used to calculate
the equivalent doses of a drug when a
patient is switched from one dosage
form to another.

BIOAVAILABILITY, F
DOSE OF NEW
DOSAGE FORM

Amount of drug absorbed

from current dosage form x
DOSE
F of the new dosage form

Example:
A patient who has been receiving daily doses of
250mcg of digoxin tablet is to be switched to
an elixir. The equivalent dose of the elixir
would be calculated as:

BIOAVAILABILITY, F
*Another factor to consider is the
chemical form in which a drug is
administered.
When a salt or ester of a drug is
administered, F should be multiplied by
the fraction of the total molecular weight
which the active drug represents (S).
When a drug is administered in its parent
form, the S = 1.0

BIOAVAILABILITY, F
AMOUNT OF
DRUG
ABSORBED

S X F X DOSE

Example:
Aminophylline is the ethylenediamine salt of
theophylline. The S for aminophylline is 0.8
since 80 85% is theophylline. The F for
uncoated aminophylline tablets is 1 since it is
considered to be completely available. The
amount of theophylline absorbed from a
200mg aminophylline uncoated tablet can be
calculated as:

ABSOLUTE AND
RELATIVE
BIOAVAILABILITIES

ABSOLUTE
BIOAVAILABILITY
Is the measurement of a test
formulation dose against an IV
reference dose the bioavailability of
which is 100% by definition.
Absolute
Bioavailability =
%

AUC test / Dose test

AUC IV / Dose IV

X 100

RELATIVE
BIOAVAILABILITY
Is the measurement of a test
formulation dose against a reference
formulation. The two formulations are
may be considered bioequivalent if the
range of the ratio of their AUCS is 0.8 to
1.25.
AUC test / Dose test
Relative
X
Bioavailability = AUC reference / Dose reference
100
%

Example:
1. What is the absolute f of the drug from
the oral solution?
2. What is the relative f of the drug from
the oral tablet compared to the
reference standard?
PLASMA CONCENTRATION (mg/mL)
DOSE

AUC
(mg/mL/hr)

IV
solution

Oral
solution

Oral tab

Oral cap

2mg

10mg

10mg

10mg

29.0

145.0

116.0

116.0

Assignment:
2. Calculate the relative F of the capsule
compared to the oral solution and the
absolute F of the drug from the tablet.
PLASMA CONCENTRATION (mg/mL)
DOSE

AUC
(mg/mL/hr)

IV
solution

Oral
solution

Oral tab

Oral cap

0.2 mg

4mg

4mg

4mg

20

380.0

340.0

360.0