bioavailability and bioequivalence

the established non-proprietary common name of active ingredient is known as…

a) chemical name

b) generic name

c) brand name

b) generic name

when the name indicates structure, it is known as…

a) chemical name

b) generic name

c) brand name

a) chemical name

the privately owned trade name of a drug is known as…

a) chemical name

b) generic name

c) brand name

c) brand name

SATA: bioavailability is a reference to the ____ and ____ to which a drug is absorbed.

a) rate

b) dosage

c) cost

d) extent

a) rate

d) extent

T/F: F and k_a are used as direct measures of bioavailability

• false

  • too variable

  • use Cmax, tmax, AUC

Cmax is a measure of…

a) rate only

b) extent only

c) rate and extent

c) rate and extent

tmax is a measure of…

a) rate only

b) extent only

c) rate and extent

a) rate only

AUC is a measure of…

a) rate only

b) extent only

c) rate and extent

b) extent only

how does increasing the dose affect extent, AUC, and Cmax of absorption

• increased dose = increased extent = increased AUC = increased Cmax

T/F: A, B, and C all have the same tmax, which indicates that they have the same rate of absorption

• true

A_u (infinity) is a measure of…

a) rate only

b) extent only

c) rate and extent

b) extent only

what is the most correct statement when describing the bioequivalence between drug A + B?

a) they have the same rate of absorption and extent of absorption

b) they have the same rate of absorption but different extent of absorption

c) they have different rates of absorption but the same extent of absorption

d) a) they have the different rate of absorption and extent of absorption

c) they have different rates of absorption but the same extent of absorption

since drug reaches the plateau slower, it has a ____ tmax

• longer

test product in relative bioavailability refers to …

• generic drug

reference product in relative bioavailability refers to …

• brand drug

the reference product in absolute bioavailability refers to…

• IV route drug

The AUC calculated after an oral tablet of 50 mg was 136 mg/hr/L. After an oral capsule dose of 150 mg, the calculated AUC was 700 mg/hr/L.

Calculate the relative bioavailability of the tablet with respect to the capsule assuming the elimination and distribution properties of the drug are unchanged between dose administrations.

• test = tablet

• reference = capsule

• 136/50 × 150/700 = 0.58 = 58%

The AUC calculated after an oral tablet of 50 mg was 136 mg/hr/L. After an oral capsule dose of 150 mg, the calculated AUC was 700 mg/hr/L. The relative bioavailability of the tablet is 0.58. If the absolute bioavailability of the oral capsule is determined to be 0.98, calculate the absolute bioavailability of the tablet dosage form.

• F_tab / F_cap = 0.58

• F_tab = F_cap * 0.58

• F_tab = 0.98 × 0.58

• F_tab = 0.57

T/F: for a plasma concentration versus time plot following the administration of an oral drug dose, the AUC is a measure of the rate of absorption

• false

  • AUC = extent of absorption

data from bioavailability studies help determine appropriate ______

• dose regimens

Bioequivalence is demonstrated by …

• establishing no statistical difference exists among C_max, t_max, and AUC

  • test product should be within 20% of that of the reference product

T/F: bioequivalent drug products show similar bioavailability when studied under similar conditions

• true

The rate and extent of absorption of the test drug do not show a significant difference

a) bioavailability

b) bioequivalence

b) bioequivalence

there is no difference in the extent of absorption but a significant difference in the rate of absorption that is intentional, reflected in the label and is medically insignificant

a) bioavailability

b) bioequivalence

b) bioequivalence

what are the methods for assessing bioavailability and bioequivalence

1. plasma drug concentration

2. urinary drug excretion

3. acute pharmacodynamic effect

4. clinical observations

5. in

what is a latin-square crossover design for a bioequivalence study?

• all subjects gets all products (A, B, C, etc) with sufficient time passed between each administration

• difference sequence in each patient

  • to show no effect on outcome

dispensing an unbranded product or a different brand in place of prescribed product. they have the same dosage form, same active ingredient, but different manufacturers.

a) generic substitution

b) pharmaceutical equivalents

c) therapeutic alternatives

d) pharmaceutical alternatives

a) generic substitution

how to know if a drug is deemed therapeutically equivalent in the Orange book?

• A = deemed therapeutically equivalent

• B = inadequate evidence of bioequivalence

same therapeutic entity but presented as different forms or different dosage forms, and strengths by a single manufacturer.

a) pharmaceutical equivalents

b) pharmaceutical alternatives

c) therapeutic alternatives

d) therapeutic equivalents

b) pharmaceutical alternatives

same active ingredient, same amount, dosage form, route of administration. However, differed in outside features (packaging, label, shape, color, etc) or release mechanism or excipients.

a) pharmaceutical equivalents

b) pharmaceutical alternatives

c) therapeutic alternatives

d) therapeutic equivalents

a) pharmaceutical equivalents

differenct active ingredients that share the same indications and used for the same therapeutic objectives

a) pharmaceutical equivalents

b) pharmaceutical alternatives

c) therapeutic alternatives

d) therapeutic equivalents

c) therapeutic alternatives

pharmaceutic equivalents that are expected to ave same clinical effect and safety profile. Indicated by A in the Orange Book.

a) pharmaceutical equivalents

b) pharmaceutical alternatives

c) therapeutic alternatives

d) therapeutic equivalents

d) therapeutic equivalents

NDA (new drug applications) must have ..

• animal and clinical data

• bioavailability data

ANDAs (abbreviated new drug applications) must have…

• bioequivalence data

what is the biopharmaceutics classification system used for?

• used to predict in vivo absorption based on solubility and permeability characteristics

what is class 1 of biopharmaceutics classification system

• high solubility - high permeability

what is class 4 of biopharmaceutics classification system

• low solubility - low permeability