Atkinson H C, Begg E J
Department of Clinical Pharmacology, Christchurch School of Medicine, Christchurch Hospital, New Zealand.
J Pharm Sci. 1988 Sep;77(9):796-8. doi: 10.1002/jps.2600770916.
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.
本文报道了16种亲脂性差异很大的药物在人乳脂质中的分布情况。如果排除地高辛和泼尼松龙，在37℃下测得的乳脂质超滤物与正辛醇-水分配系数之间存在高度相关性。这些基于类固醇的分子可能与乳汁中的游离脂肪酸相互作用，形成胶束，从而扰乱乳脂质超滤物之间的关系。文中描述了一些方程，可根据药物的pKa和正辛醇-水分配系数来估算脂溶性药物在乳汁中的分布情况。
