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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.
Solution:
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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,
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:
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
Data given:
Dose, Xo=500mg
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5/6/2018 Biopharmaceutical calculations - AUC and clearance
What is required
Fraction of dose absorbed=?
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
AUC=?
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5/6/2018 Biopharmaceutical calculations - AUC and clearance
eGPAT
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
AUC=40 mgL-1 hr
What is required
Dose=?
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
What is required
Dose=?
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