Prediction of Milk/Plasma concentration ratio of drugs
Prediction of Milk/Plasma concentration ratio of drugs
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DOI：
10.1345/aph.1c379
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发表时间：
2003-09-01
影响因子：
2.9
通讯作者：
Koren, G
中科院分区：
文献类型：
--
作者：
Larsen, LA;Ito, S;Koren, G
目的：药物的乳汁与血浆浓度比（m/p）用于估计提供给哺乳期婴儿的药物量。已发表的文献进行了审查，以确定药物的存在足够的数据计算的m/p比，并检查是否现有的经验数据同意与出版的方法阿特金森的数学预测的m/p比的基础上的physicalchemicalpropertys.METHODS：使用一个全面的参考文本，我们确定了研究报告足够的数据来计算m/p比的基础上的AUC牛奶和血浆。随后，我们根据pKa、亲脂性和蛋白质结合用Atkinson公式计算m/p比。然后，我们相关的经验与预测（计算）m/p raties.RESULTS：192药物，其中至少有一些关于牛奶积累的数据已公布，有足够的数据来量化m/p比只有69种药物（78项研究）。有没有显着的经验M/P比值和预测值之间的相关性使用Atkinson的model.CONCLUSIONS：可靠的数据M/P浓度比存在几种药物。目前，还没有合适的模型来预测人类乳汁中的药物浓度。
OBJECTIVE: The milk to plasma (m/p) concentration ratio of drugs is used to estimate the amount of drug offered to the suckling infant. Published literature was reviewed to identify drugs for which sufficient data exist for calculation of m/p ratio and to examine whether the existing empiric data agree with the published method of Atkinson for mathematical prediction of m/p ratios based on physiochemical characteristics.METHODS: Using a comprehensive reference text, we identified studies reporting sufficient data to calculate m/p ratio based on the AUC for milk and plasma. Subsequently, we calculated the m/p ratio with Atkinson's formula based on pKa, lipophilicity, and protein binding. We then correlated the empiric versus predicted (calculated) m/p ratios.RESULTS: Of 192 drugs of which at least some data on milk accumulation have been published, there were sufficient data to quantify m/p ratios for only 69 medications (78 studies). There was no significant correlation between the empiric m/p ratios and the predicted values using the Atkinson's model.CONCLUSIONS: Reliable data on m/p concentration ratios exist for few medications. Presently, there is no appropriate model to predict milk concentrations of drugs in humans.