Important Definitions

 Biopharmaceutics: the study of how the physicochemical properties of drugs, dosage forms and routes of
administration affect the rate and extent of the drug absorption.

 ADME: is an acronym in pharmacokinetics and pharmacology for absorption, distribution, metabolism, and
excretion, and describes the disposition of a pharmaceutical compound within an organism.

 Pharmacokinetics: The study and characterization of the time course (kinetics) of drug absorption,
distribution, metabolism and elimination (ADME).

 Absorption: is the process of a substance entering the body. Or appearance of the drug in the blood.

 Distribution: is the dispersion of substances throughout the fluids and tissues of the body.

 Metabolism: is the irreversible transformation of parent compounds into daughter metabolites.

 Excretion: is the elimination of the substances from the body.

 Bioavailability: The rate and extent of drug absorption.

 Bioavailable dose: The fraction of an administered dose of a particular drug that reaches the systemic
circulation intact.

 Plasma level-time curve: The plasma level-time curve is generated by measuring the drug concentration in
plasma samples taken at various time intervals after a drug product is administered.

 Drug Product Performance Parameters:

1- Minimum effective concentration (MEC): The minimum concentration of drug needed at the receptors to produce
the desired pharmacologic effect.

2- Minimum toxic concentration (MTC): The drug concentration needed to just produce a toxic effect.

3- Onset time: The time required for the drug to reach the MEC.

4- Duration of action: The difference between the onset time and the time for the drug to decline back to the MEC.

5- The time of peak plasma level: The time of maximum drug concentration in the plasma and is proportional to the
rate of drug absorption.

6- The peak plasma level: The maximum drug concentration, usually related to the dose and the rate constants for
absorption and elimination of the drug.

7- Area under the curve: It is related to the amount of drug absorbed systemically.

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8-Therapeutic range: The plasma or serum concentration (e.g. mgmL_1) range within which the drug is likely to
produce the therapeutic activity or effect.
 Lipid Solubility: Lipid solubility will affect the ability of the drug to bind to plasma proteins and to cross lipid
membrane barriers.
 Plasma protein binding: Extensive plasma protein binding will cause more drugs to stay in the central blood
compartment. Therefore drugs which bind strongly to plasma protein tend to have lower volumes of
distribution. (↑ protein binding = ↓ V)
 Metabolism is defined as: The irreversible biotransformation of drug in the body → typically involves making
it more polar to enhance renal excretion
 Conjugation: Conjugation reactions covalently add large, polar endogenous molecules to parent drug or Phase
I metabolite →inactive and excretable

 Glucuronidation: This is the main conjugation reaction in the body. This occurs in the liver. Aliphatic alcohols
and phenols are commonly conjugated with glucuronide. Thus hydroxylated metabolites can also be
conjugated.

 Acylation: Acylation, especially acetylation with the acetyl group, e.g. sulfonamides

 Induction: Induction ~ ↑ metabolic activity of enzyme = ↓ [drug]

 Bioavailability: It is a measurement of the extent of a therapeutically active drug that reaches the systemic
circulation and is available at the site of action.

 Absolute bioavailability: Absolute bioavailability compares the bioavailability (estimated as area under the
curve, or AUC) of the active drug in systemic circulation following non-intravenous administration (i.e., after
oral, rectal, transdermal, subcutaneous administration), with the bioavailability of the same drug following
intravenous administration.

 Relative bioavailability: This measures the bioavailability (estimated as area under the curve, or AUC) of a
certain drug when compared with another formulation of the same drug, usually an established standard, or
through administration via a different route.

 Bioequivalence: means pharmaceutical equivalents or pharmaceutical alternatives whose rate and extent of
absorption do not show a significant difference when administered at the same molar dose of the therapeutic
moiety under similar experimental conditions.

 Pharmaceutical Alternatives: means drug products that contain the identical therapeutic moiety, or its
precursor, but not necessarily in the same amount or dosage form or as the same salt or ester.

 Pharmaceutical Equivalent: means drug products that contain identical amounts of the identical active drug
ingredient, i.e., the salt or ester of the same therapeutic moiety, in identical dosage forms, but not necessarily
containing the same inactive ingredients, and that meet the identical compendial or other applicable standard

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 of identity, strength, quality, and purity, including potency and where applicable, content uniformity,
disintegration times and/or dissolution rate.

 Brand Name: is the trade name of the drug.

 Chemical Name: is the name used by the organic chemist to indicate the chemical structure of the drug.

 Generic Name: is the established, non proprietary or common name of the active drug in a drug product.

 Active transport: a type of specialized transport where energy is used to move a drug molecule against a
concentration gradient.
 Systemic circulation: blood vessels that distribute absorbed drug throughout the body; intravenously
administered drug goes directly into the systemic circulation.
 Clearance: a pharmacokinetic parameter that indicates the volume of plasma from which all drug is removed
(cleared) per unit time.
 Compartment: a virtual space into which absorbed drug can be considered to be distributed; some drugs
remain in a central compartment comprising the vasculature and the well-perfused organs and tissues, while
other drugs undergo a further transfer into a more peripheral space termed the tissue compartment.
 Diffusion: movement of drug molecules that is powered by a concentration gradient.
 Disintegration a process by which a tablet or capsule is broken down into particles called granules.
 Dissociation in solution: the physical separation of anions and cations of an acid, a base or a salt; dissociation
approaches 100% for most salts and for strong acids and bases, while the degree of dissociation of weak acids
and bases is governed by their dissociation constants.
 Dissolution: the process by which a drug goes into solution in which individual drug molecules are separated
by molecules of solvent (water).
 Effect: response of the body to a pharmacological agent; this response may be either therapeutic or toxic; it is
characterized by an onset, intensity, and duration.
 Elimination half life: for a drug with linear elimination pharmacokinetics, the time it takes for 50% of drug
present to be eliminated; it is constant for a given patient receiving a particular drug.
 First-order process: a process whose rate is directly proportional to the current amount of the compound
being transferred by the process; linear elimination pharmacokinetic is an example of a first-order process
 First pass effect: the situation whereby the fraction of a dose of orally administered drug that reaches the
systemic circulation is equal to 1 minus its hepatic extraction ratio.
 Formulation: a dosage form of a particular drug.
 Parameter: a pharmacokinetic constant for a given patient receiving a particular drug.
 Volume of distribution: apparent the volume of plasma that would be required to dilute a given dose of drug,
resulting in its observed plasma drug concentration.