ADME-PK - Prediction Systems

BCS

biopharmaceutics classification system

BCS predicts:

potential formulation problems for oral absorption

BCS is used to judge:

generic drug formulations

BCS Class I - oral absorption

• not solubility limited

• not permeability limited

BCS Classes with high permeability extent

• Class I

• Class II

BCS Classes with low permeability extent

• Class III

• Class IV

BCS Class I - formulation

formulation is simple

BCS Class II - oral absorption

• solubility limited

• not permeability limited

BCS Class II - formulation

may need solubility enhancer like salt form

BCS Class III - oral absorption

• not solubility limited

• is permeability limited

BCS Class III - formulation

may need permeability enhancer excipient 

BCS Class IV - oral absorption

• is solubility limited

• is permeability limited

BCS Class IV - formulation

very challenging for formulation, may need alternate route of administration

BCS Classes with high solubility

• Class I

• Class III

BCS Classes with low solubility

• Class II

• Class IV

BCS Class I has _____ permeability extent and _____ solubility

• high permeability extent

• high solubility

BCS Class II has _____ permeability extent and _____ solubility

• high permeability extent

• low solubility

BCS Class III has _____ permeability extent and _____ solubility

• low permeability extent

• high solubility

BCS Class IV has _____ permeability extent and _____ solubility

• low permeability extent

• low solubility

BCS Class I drug example

acetaminophen

BCS Class II drug example

ibuprofen

BCS Class III drug example

atenolol

BCS Class IV drug example

• chlorothiazide

• neomycin

BCS extent of permeability:

Caco-2 cell experiment compared to known molecules of low, moderate, and high permeability

BCS extent of solubility

highest single therapeutic dose is completely soluble in 250 mL or less of aqueous media at pH 1.2, 4.5, and 6.8 at 37 ± 1 degrees C

BCS rate of solubility

≥ 85% of dose dissolved in ≤ 30 minutes