5/6/2018 Biopharmaceutical calculations - AUC and clearance

eGPAT

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Biopharmaceutical calculations - AUC and

clearance
by egpat      Posted on 08-06-2017
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Biopharmaceutical calculations are very important in order to determine the

amount of drug reaches to systemic circulation and to fix the dose and dosing
intervals.

When drugs are given orally they should undergo absorption into the systemic
circulation. Drugs cann't absorb completely due to various factors like
physicochemical properties of the drugs, physiological factors and even first pass
metabolism.

The total amount of the drug that reaches into the systemic circulation is called as
bioavailable dose.
Calculation of fraction of bioavailability
Let's start with one simple working example.

Working example 1: F From dose

400 mg of a drug is reached in to the systemic circulation when given at dose of

500 mg. Calculate the fraction of drug reached in to the systemic circulation.

Solution:

Now let’s see the solution for the above example.

Data given:

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5/6/2018 Biopharmaceutical calculations - AUC and clearance

eGPAT

Oral dose=500 mg
Bioavailble dose=400 mg
Fraction of drug absorbed=?
The fraction of the dose absorbed can be calculated as follows
Fraction of drug absorbed is the ratio of bioavailable does to oral dose
By using above equation,

Working example 2: F From AUC

The fraction of the drug reaching in to the systemic circulation for a 500 mg of
drug with clearance 20 L/hr is given produced AUC 10 mgL-1 hr

Solution:

First of let's define AUC and clearance

AUC
AUC is the Area Under Curve which indicates the rate and extent of systemic
absorption of the drug. The total amount the drug absorbed into the systemic
circulation is directly proportional to AUC.

Clearance

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5/6/2018 Biopharmaceutical calculations - AUC and clearance

We have to use the equation

eGPAT

Clearance is related with volume of distribution as

Hence combining above two equation, we can bring a final equation.

Data given:

Dose, Xo=500mg
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5/6/2018 Biopharmaceutical calculations - AUC and clearance

Clearance, Cl=20 L/hr

eGPAT
AUC=10 mgL-1 hr

What is required
Fraction of dose absorbed=?

By using above equation,

Working Example 3: AUC from Clearance

The AUC of a 400 mg of drug given by oral route having 10 L/hr clearance, if
90% absorbed is

Data given :
Dose=400 mg

Clearance=10 L/hr

Fraction of dose absorbed=90%=0.9

AUC=?

Again using the above equation,

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5/6/2018 Biopharmaceutical calculations - AUC and clearance

eGPAT

Working Example 4: Dose for given AUC

How much dose of a drug is required to achieve AUC . The clearance of the drug
is and drug is 80% absorbed.

Data given :

Clearance=10 L/hr

Fraction of dose absorbed=80%=0.8

AUC=40 mgL-1 hr

What is required

Dose=?

Again using the above equation,

Working Example 5: Dose for given clearance

Calculate dose of a drug with elimination rate constant 0.8 hr-1 that is required to
administer to attain AUC of 25 mgL-1 hr . The volume of distribution of the drug
is 20L.

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5/6/2018 Biopharmaceutical calculations - AUC and clearance

Data given :
eGPAT
Elimination rate constant, Ke=0.8 hr-1

AUC=25 mgL-1 hr

Volume of distribution, Vd=20 L

Fraction of dose absorbed=1

What is required
Dose=?

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