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Membrane structure
Figure 2
Molecular weight and drug absorption
• The larger drug molecules are, the poorer will be their absorption.
• Lipinski devised a rule of five defining drug-like properties.
but note:
o Compounds that are substrates for transporters are exceptions
to the rule.
Permeability and
the pH-partition hypothesis
Assumption
• Only drugs in their unionised form (more lipid-soluble)
pass through membranes.
• As most drugs are weak electrolytes it is to be expected
that the unionised form (U) of either acids or bases,
the lipid-soluble species, will diffuse across the
membrane, while the ionised forms (I) will be rejected.
• Variability in pH conditions