Relationship between human milk lipid-ultrafiltrate and octanol-water partition coefficients.
The distribution into human milk lipid of 16 drugs with widely varying lipophilicity is reported. There is a high degree of correlation between milk lipid-ultrafiltrate and octanol-water partition coefficients, measured at 37 degrees C, provided digoxin and prednisolone are excluded. These steroid-based molecules may interact with free fatty acids in milk, forming micelles and thus perturbing the milk lipid-ultrafiltrate relationship. Equations are described which enable estimation of drug distribution into milk for lipid-soluble drugs, based on drug pKa and octanol-water partition coefficients.
Atkinson
H C
HC
Department of Clinical Pharmacology, Christchurch School of Medicine, Christchurch Hospital, New Zealand.
Begg
E J
EJ
D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008055:Lipids / Q000032:analysis*; D008895:Milk, Human / Q000032:analysis*; D000442:Octanols; D004364:Pharmaceutical Preparations / Q000032:analysis; D012995:Solubility; D014462:Ultrafiltration; D014867:Water
D008055:Lipids; D000442:Octanols; D004364:Pharmaceutical Preparations; D014867:Water