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Basic Parameters and Abbreviations in Pharmacokinetic Tests

2021-11-16
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Pharmacokinetic Parameters

Pharmacokinetic parameters represent the parameters of the mathematical model of the process of drug absorption, distribution, excretion and structural transformation in the body.

Basic Parameters and Abbreviations in Pharmacokinetic Tests

Absorption

Dissolution: the degree to which the drug molecule is dissolved in the digestive tract
Bioavailability: the degree of drug absorption
Absolute bioavailability
Maximum blood concentration (Cmax)
Peak time (Tmax)

Distribution

Due to the inhomogeneity of the internal environment (blood, tissue), the drug concentration changes at different speeds.
Compartment: The drug concentration in the same compartment changes at the same speed and is homogeneous.
One-compartment model: The drug enters the blood and is rapidly distributed throughout the body, and is constantly cleared.
Two-compartment model: After the drug enters the body, it first quickly distributes in the tissue, and then enters a slower elimination process.
Apparent volume of distribution (Vd) (aparent volume of distribution): characterizes the ability of a drug to be taken up by tissues in the body. The drug body with a large apparent volume has a longer retention time.
Area under the drug concentration-time curve (AUC); Systemic Exposure
Blood-brain barrier; protein binding rate; distribution half-life (t 1/2(α)

Eliminate

Elimination: The process by which the original drug disappears in the body. Including kidney (urine) or bile (feces) or the sum of respiratory excretion and metabolic transformation.
Elimination constants (elimination constants): Reflect how fast the drug disappears in the body. Does not fully reflect the duration of action of the drug (metabolites are also active).
Half-life or half-life (t1/2): The time required for the concentration or dose of a drug to decrease by 50%. Elimination half-life t1/2(β)) Terminal Half-life, Elimination Half-life.
Clearance (clearance) or renal clearance: Reflects the speed at which drugs or metabolites are excreted from the body through the kidneys.

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