Partition coefficient optimization balances lipophilicity enhancing membrane permeability against aqueous solubility requirements. Excessive lipophilicity impairs solubility causing bioavailability loss. Insufficient lipophilicity prevents absorption. LogP measurement quantitates lipophilicity. Calculated partition coefficients guide design.
Formulation strategies enhance apparent solubility compensating for lipophilicity. Structure modification iteratively optimises partition coefficient. Regulatory submissions justify selections. Post-approval bioavailability monitoring confirms predictions. Emerging ADME prediction improves optimization.
General Biopharmaceutical Concepts
Partition Coefficient Optimization
Partition coefficient optimisation adjusts the lipophilicity of a compound to improve absorption, tissue distribution, formulation performance and overall pharmacokinetic properties.
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