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(Log P (Permeability, Solubility in Bio relevant Media, Lysosomal Traping,…
Log P
Permeability
Solubility in Bio relevant Media
Lysosomal Traping
Systemic Distribution / VD
Tmax
Long Tmax
Lysosomal Traping
Precipitation in Small Intestine
Erythrocyte Partitioning (Chlorthalidone)
Pattern of release & DT (Slow Erosion - Venetoclax)
Low Permeability
Strength
Longer for Higher Strengths
in-vivo Dissolution rate limiting step
Precipitation more for higher strengths
Shorter for Higher Strengths
Enzyme Saturation
Same Across Strengths
in-vivo Dissolution should be faster than in vivo Absorption
Short Tmax
Rapid etabolism
High Permeability
Rapid precipitation as insoluble drug
pKa
Lysosomal Traping
Lipophilic (logP > 1) / Cationic amphiphilic drugs / ionizable amines (pKa > 6)
Common ion effect
Systemic Distribution / VD
MW
Precipitation Kinetics
Fast PPT
Low MW compounds
Slow PPT
High MW Compounds
Solubility in Bio relevant Media
Compare to high MW compounds less impact expected
More impact expected for high MW Compounds
Entero Hepatic Circulation
Reabsorbed
Not Reabsorbed
Nature of Compound
Lipophilicity
Hydrophilic
Weekly Lipophylic
Lipophylic
Highly Lipophylic
Classifications
BCS
Uptake & Eflux transpoter critical for III & IV class
BDDCS
ECCS
Metabolism
High Permeability Bases/Neutrals [LogP >3]
High Permeability Acids and zwitterions with a molecular weight <400 Da
Renal
Low permeability bases/neutrals & acids/zwitterions with MW ≤400 Da
Hepatic
Transporter Uptake Rate Limited
High Permeability Acids and zwitterions with a molecular weight >400 Da [OATP]
Bile
Polar acidic drugs with high MW & Quarternary Ammonium Compounds
Base
Lysosome Traping
Enterocyte GI Tract Binding
Precipitation Kinetics
Acid Solubility
Acid
Stomach Solubility
Amphoteric
Neutral