Bioavailability and Bioequivalence: Oral Absorption

what is the major site for drug absorption

small intestine

transport is saturated at __

high drug concentration

name 6 physiological factors that affect oral absorption

pka, solubility, charge, partition coefficient, drug-drug interactions, stability

true or false: formulation factors can affect drug release from a drug product

true

name the four primary systems that affect the first pass effect of a drug

enzymes of the gastrointestinal lumen, gut wall enzymes, bacterial enzymes, hepatic enzymes

the rate and extent to which the active ingredient or active moiety is absorbed form a drug product and becomes available at the site of action is the definition of

bioavailability

AUC reflects the __ of absorption

extent

C max and T max reflect the __ of absorption

rate

the fraction of the dose that actually reaches the systemic circulation is the definition of

absolute bioavailability F

for drugs after IV administration F is

equal to one

for drugs after oral administration F is

less than or equal to one

why is bioavailability important to pharmacists

to advise patients on how to correctly take medications to achieve optimal therapeutic effects

the absence of a significant difference in the rate and extent to which the active ingredient or active moiety in pharmaceutical equivalents or pharmaceutical alternatives becomes available at the site of drug action when administered at the same molar do

bioequivalence

drug products that contain the same active drug ingredient and are identical in strength or concentration, dosage form, and route of administration are ___

pharmaceutical equivalents

drug products that contain the same therapeutic moiety but as different salts, esters, or complexes are ___

pharmaceutical alternatives

drug products that contain the same therapeutically active drug that should give the same therapeutic effect and have equal potential for adverse effects under conditions set forth in the labels of these drugs are ___

therapeutic equivalents

biosimilars are derived from

living organisms

name two statistical tests to evaluate data

ANOVA and power test

in the power test the power should be __ or greater than __ and a level of sifnificance of ___

0.8, beta = 0.2, 0.05

generic drug products must be ___ with the brand-name drug product

bioequivalent

a drug is highly soluble if the highest dose strength is soluble in ___ or less of aqueous media over the pH range of ___

250 ml , 1-8

BCS class 1 ___ solubility and ___ permeability

high, high

BCS class 2 __ solubility and ___ permeability

low, high

BCS class 3 ___ solubility and ___ permeability

high, low

BCS class 4 ___ solubility and ___ permeability

low, low

in BCS class 3 drugs bioavailability may be incomplete if the drug is not what

released and dissolved within the absorption window

in BCS class 2 drugs bioavailability is controlled by the what

dosage form and rate of drug released from the drug product