A non-binary biopharmaceutical classification of drugs: the ABΓ system.
The purpose of the present work is to develop a non-binary biopharmaceutical classification system the so called ABΓ system. The original mathematical model used for the development of BCS, appropriately modified, was applied to estimate the limiting values of drug solubility and permeability when the fraction of dose absorbed, Fa, was 0.90 or 0.20. The ABΓ system is based on the fraction of dose absorbed and relies on permeability, solubility plane. The first category (A, alpha) includes drugs with Fa ≥ 0.90, whereas the B (beta) category consists of drugs with Fa ≤ 0.20. The area lying between the two boundaries of A and B defines the third category (gamma), Γ, (0.20<Fa<0.90). For comparative purposes, the BCS classes I-IV were co-plotted together with the ABΓ system. Most of the BCS classes II and III are included in category Γ which mainly consists of drugs with properties like moderate or low solubility and permeability. Due to the dynamic character of dissolution and uptake processes, category A is expanded toward BCS Class II. The ABΓ system allows the classification of all compounds into three categories (A, B, Γ) in terms of the fraction of dose absorbed.
Laboratory of Biopharmaceutics - Pharmacokinetics, Faculty of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece. Electronic address: macheras@pharm.uoa.gr.
Panos
P
Macheras
Laboratory of Biopharmaceutics - Pharmacokinetics, Faculty of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece.
Vangelis
V
Karalis
D001702:Biopharmaceutics / Q000145:classification* / Q000379:methods*; D008962:Models, Theoretical; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000145:classification*; D012995:Solubility
D004364:Pharmaceutical Preparations
Dose; Fraction of dose absorbed; Non-binary BCS; Permeability; Simulations; Solubility