Table 4 In vivo PK studies
From: An integrated pharmacokinetics ontology and corpus for text mining
Category | Name | Description | Unit | reference |
|---|---|---|---|---|
PK parameters | AUCinf | Area under the drug concentration time curve. | mg h L-1 | RT p37 |
AUCSS | Area under the drug concentration time curve within a dosing curve at steady state. | mg h L-1 | RT pxi | |
AUCt | Area under the drug concentration time curve from time 0 to t. | mg h L-1 | RT p37 | |
AUMC | Area under the first moment of concentration versus time curve. | mg2 h L-2 | RT p486 | |
AUCR | AUC ratio (drug interaction parameter). | Unit free | Â | |
CL | Total clearance is defined as the proportionality factor relating rate of drug elimination to the plasma drug concentration. | ml h-1 | RT p23 | |
CLb | Blood clearance is defined as the proportionality factor relating rate of drug elimination to the blood drug concentration. | ml h-1 | RT p160 | |
CLu | Unbound clearance is defined as the proportionality factor relating rate of drug elimination to the unbounded plasma drug concentration. | ml h-1 | RT p163 | |
CLH | Hepatic portion of the total clearance. | ml h-1 | RT p161 | |
CLR | Renal portion of the total clearance. | ml h-1 | RT p161 | |
CLpo | Total clearance of drug following an oral dose. | ml h-1 | Â | |
CLIV | Total clearance of drug following an IV dose. | ml h-1 | Â | |
CLint | Intrinsic metabolic clearance is defined as ratio of maximum metabolism rate, Vmax, and the Michaelis-Menten constant, Km. | ml h-1 | RT p165 | |
CL12 | Inter-compartment distribution between the central compartment and the peripheral compartment. | ml h-1 | Â | |
CL ratio | Ratio of the clearance (drug interaction parameter). | Unit free | Â | |
Cmax | Highest drug concentration observed in plasma following administration of an extravascular dose. | mg L-1 | RT pxii | |
Cmax ratio | The ratio of Cmax (drug interaction parameter). | Unit free | Â | |
Css | Concentration of drug in plasma at steady state during a constant rate intravenous infusion. | mg L-1 | RT pxii | |
Css ratio | The ratio of Css (drug interaction parameter). | Unit free | Â | |
E | Extraction ratio is defined as the ratio between blood clearance, CLb, and the blood flow. | Unit free | RT p159 | |
EH | Hepatic extraction ratio. | Unit free | RT p161 | |
F | Bioavailability is defined as the proportion of the drug reaches the systemic blood. | Unit free | RT p42 | |
FG | Gut-wall bioavailability. | Unit free | Â | |
FH | Hepatic bioavailability. | Unit free | RT p167 | |
FR | Renal bioavailability. | Unit free | RT p170 | |
fe | Fraction of drug systemically available that is excreted unchanged in urine. | Unit free | RT pxiii | |
fm | Fraction of drug systemically available that is converted to a metabolite. | Unit free | RT pxiii | |
fu | Ratio of unbound and total drug concentrations in plasma. | Unit free | RT pxiii | |
k | Elimination rate constant. | h-1 | RT pxiii | |
K12, k21 | Distribution rate constants between central compartment and peripheral compartment. | h-1 | Â | |
ka | Absorption rate constant. | h-1 | RT pxiii | |
ke | Urinary excretion rate constant. | h-1 | RT pxiii | |
km | Rate constant for the elimination of a metabolite. | h-1 | RT pxiii | |
Km | Michaelis-Menten constant. | mg L-1 | RT pxiii | |
MRT | Mean time a molecular resides in body. | h | RT pxiv | |
Q | Blood flow. | L h-1 | RT pxiv | |
QH | Hepatic blood flow. | L h-1 | RT pxiv | |
tmax | Time at which the highest drug concentration occurs following administration of an extravascular dose. | h | RT pxiv | |
t1/2 | Half-life of the drug disposition. | h | RT pxiv | |
t1/2 ratio | Half-life ratio (drug interaction parameter). | Unit free | Â | |
t1/2,α | Half-life of the fast phase drug disposition. | h |  | |
t1/2,β | Half-life of the slow phase drug disposition. | h |  | |
V | Volume of distribution based on drug concentration in plasma. | L | RT pxiv | |
Vb | Volume of distribution based on drug concentration in blood. | L | RT pxiv | |
V1 | Volume of distribution of the central compartment. | L | RT pxiv | |
V2 | Volume of distribution of the peripheral compartment. | L | Â | |
Vss | Volume of distribution under the steady state concentration. | L | RT pxiv | |
Vmax | Maximum rate of metabolism by an enzymatically mediated reaction. | mg h-1 | RT pxiv | |
λ1, λ2 | Disposition rate constants in a two-compartment model. | h-1 | GP p84 | |
Pharmacokinetics Models | Non-Compartment | Use drug concentration measurements directly to estimate PK parameters, such as AUC, CL, Cmax, Tmax, t1/2, F, and V. | GP p409 | |
One Compartment Model | It assumes the whole body is a homogeneous compartment, and the distribution of the drug from the blood to tissue is very fast. It assumes either a first order or a zero order absorption rate and a first order eliminate rate. Its PK parameters include (ka, V, CL, F). | RT p34 | ||
GP p1 | ||||
Two Compartment Model | It assumes the whole body can be divided into two compartments: central compartment (i.e. systemic compartment) and peripheral compartment (i.e. tissue compartment). It assumes either a first order or a zero order absorption rate and a first order eliminate and distribution rates. Its PK parameters include (ka, V1, V2, CL, CL12, F). | GP p84 | ||
Study Designs | Hypothesis | Bioequivalence, drug interaction, pharmacogenetics, and disease conditions. | Â | |
Design | Single arm or multiple arms; cross-over or fixed order design; with or without randomization; with or without stratification; prescreening or no-prescreening; prospective or retrospective studies; and case reports or cohort studies. | Â | ||
Sample size | The number of subjects, and the number of plasma or urine samples per subject. | Â | ||
Time points | Sampling time points and dosing time points. | Â | ||
Sample types | Blood, plasma, and urine. | Â | ||
Dose | Subject specific doses. | Â | ||
Quantification methods | HPLC/UV, LC/MS/MS, LC/MS, radiographic | Â | ||