Syversen G B, Ratkje S K
J Pharm Sci. 1985 Oct;74(10):1071-4. doi: 10.1002/jps.2600741010.
Phase distribution and protein binding of drugs in human milk have been measured. The analytical method is reproducible, rapid, and requires only small sample volumes. Five drugs were studied: diazepam, phenobarbital, warfarin, phenytoin, and disopyramide. Experiments were carried out at 37 degrees C on milk samples with variable fat and protein contents. Results for the distribution of drugs between the skimmed-milk phase and fat-rich phase are presented, as well as the results of the dialysis of drugs in skimmed milk. It is shown that, among the physicochemical properties of a drug, the lipid solubility seems to be the most important property for predicting variations in drug concentrations in milk. The potential significance of the findings with respect to in vivo distribution of drugs into human milk is discussed.
已对母乳中药物的相分布和蛋白质结合情况进行了测定。该分析方法具有可重复性、速度快，且仅需少量样本量。研究了五种药物：地西泮、苯巴比妥、华法林、苯妥英和丙吡胺。在37摄氏度下对脂肪和蛋白质含量不同的母乳样本进行了实验。给出了脱脂乳相和富脂相间药物分布的结果，以及脱脂乳中药物透析的结果。结果表明，在药物的物理化学性质中，脂溶性似乎是预测母乳中药物浓度变化的最重要性质。讨论了这些发现对于药物在体内向母乳中分布的潜在意义。
