Basic concepts Flashcards
is the extent or fraction of drug absorbed upon extravascular administration in comparison to the dose size administered
Absolute bioavailability
the process of uptake of the compound from the site of administration into the systemic circulation. A prerequisite for absorption is that the drug be in aqueous solution. The only rare exception is absorption by pinocytosis.
Absorption
rate constant of the entire process of drug transfer into the body, through all biological membranes.
Absorption rate constant
increase of drug concentration in blood and tissue upon multiple dosing until steady state is reached
Accumulation
the ratio of the concentrations at equilibrium between a lipid phase (usually n-octanol) and an aqueous phase (usually buffer pH 7.4). The apparent partition coefficient is uncorrected for dissociation or association in either phase.
Apparent partition coefficient
integral of drug blood level over time from zero to infinity, and is a measure of quantity of drug absorbed and in the body.
Area under the curve
is the phenomenon that drugs emptied via bile into the small intestine can be reabsorbed from the intestinal lumen into systemic circulation
Biliary recycling/
Enterohepatic recirculation
rate and extent to which an active drug substance or moiety is absorbed from the pharmaceutical dosage form and becomes available at its site of action
Bioavailability
achieved if its extent and rate of absorption are not statistically different from those of the standard when administered at the same molar dose
Bioequivalence
requirement imposed by the FDA for in vitro and/or in vivo testing of specified drug products which must be satisfied as a condition of marketing
Bioequivalence requirement
deals with the physical & chemical properties of the drug substance, the dosage form, and the body and the biological effectiveness of a drug and/or drug products upon administration, i.e. the drug availability to the human or animal body from a given dosage form, considered as a drug delivery system. The time course of the drug in the body and the quantifying of the drug concentration pattern are explained by pharmacokinetics
Biopharmaceutics
actual site of action of a drug in the body. It is the drug-receptor interaction on the molecular level or the effect of the presence of a drug on biopolymers. The biophase may be the surface of a cell or within the cell, i.e. one of the organelles
Biophase
speed of blood perfusion in an organ, usually expressed in mL/100 g organ weight/min. Blood flow rates may differ several-fold between rest and exercise
Blood flow rate
demonstrate the concentration in blood, plasma, or serum upon administration of a dosage form by various routes of administration. Blood, plasma, or serum level curves are plots of drug concentration versus time on numeric or semilog graph paper. Blood, plasma, or serum levels are obtained from blood samples by venipuncture in certain time intervals after administration of the drug product and chemical or microbiological analysis of the drug in the biological fluid
Blood, plasma, serum level
sum of all body regions (organs and tissue) in which the drug concentration is in instantaneous equilibrium with that in blood or plasma. The blood or plasma is always part of the central compartment
Central compartment
is the hypothetical volume of distribution in mL of the unmetabolized drug which is cleared per unit of time (mL/min or mL/h) by any pathway of drug removal
Clearance
an entity which can be described by a definite volume and a concentration of drug contained in that volume.
Compartment
the difference in the concentration in two phases usually separated by a membrane
Concentration gradient
are plots of the actual cumulative amounts of drug and/or its metabolites excreted into urine versus time upon administration of a drug product by various routes of administration.
Cumulative urinary excretion curve
portion of a prolonged release dosage form which liberates the drug from the dosage form at a slower rate than its unrestricted absorption rate
Depot phase
the viscous layer of concentrated drug solution around a dissolving particle
Diffusion layer
the loss of drug from the central compartment due to distribution into other compartments and/or elimination.
Disposition
systematized dosage schedule for therapy, i.e. the proper dose sizes and proper dosing intervals required to produce clinical effectiveness or to maintain a therapeutic concentration in the body.
Dosage regimen/
Dose rate
change of one or more of the pharmacokinetic processes of absorption, distribution, metabolism, & excretion with increasing dose size
Dose dependency
term used to describe the achievement of sustained drug concentration by simply increasing the dose size or by accidental fast release of drug from a sustained release dosage form
Dose dumping
amount of drug in µg, mg, units
Dose size
time period between administration of maintenance doses
Dosing interval
chemical compound of synthetic, semisynthetic, natural, or biological origin which interacts with human or animal cells
Drug