The majority of women have health problems that require medication after giving birth. Complications such as allergies, postpartum depression, and diabetes are often treated with drugs such as cetirizine, venlafaxine, and metformin, respectively. These treatments are considered safe during lactation, but information of the transfer of drugs to breast milk and possible effects on the infant is scarce. Therefore, this needs to be systematically investigated in larger populations. To enable the determination of drug transfer, we here describe the validation of two rapid, sensitive, and high-throughput analysis methods for 1) simultaneous quantification of cetirizine, venlafaxine, and O-desmethylvenlafaxine in human breast milk, and 2) metformin in human breast milk and plasma. In both methods, a simple protein precipitation protocol with acetonitrile and benchtop-centrifugation was used prior to compound analysis with liquid-chromatography tandem mass spectrometry. The methods had linear ranges between 0.39 – 194.5 ng/mL for cetirizine, 0.28 – 138.7 ng/mL for venlafaxine, 0.26 – 131.7 ng/mL for O–desmethylvenlafaxine, in milk, and 0.65 – 193.7 ng/mL for metformin in both milk and plasma. Intra-run and inter-run precision and accuracy were ≤ 9% for cetirizine, venlafaxine, and O–desmethylvenlafaxine in milk, and ≤ 7% for metformin in milk and plasma. Cetirizine was measured to median milk concentrations of 13 ng/mL (range: 0.65 – 65 ng/mL) in 228 donor samples from breast-feeding women.

大多数妇女在分娩后都有健康问题需要服药。过敏、产后抑郁和糖尿病等并发症通常分别用西替利嗪、文拉法辛和二甲双胍等药物治疗。这些治疗在哺乳期被认为是安全的，但关于药物转移到母乳以及对婴儿可能产生的影响的信息很少。因此，这需要在更大的人群中进行系统的研究。为了确定药物转移，我们在此描述了两种快速、灵敏和高通量分析方法的验证，用于 1) 同时定量西替利嗪、文拉法辛和O-人母乳中的去甲基文拉法辛，和 2) 人母乳和血浆中的二甲双胍。在这两种方法中，在使用液相色谱串联质谱法进行化合物分析之前，都使用了简单的乙腈和台式离心蛋白质沉淀方案。这些方法在牛奶中的线性范围为 0.39 – 194.5 ng/mL，文拉法辛为 0.28 – 138.7 ng/mL，O-去甲基文拉法辛为 0.26 – 131.7 ng/mL ，两种牛奶中的二甲双胍为 0.65 – 193.7 ng/mL和等离子。西替利嗪、文拉法辛和O的批内和批间精密度和准确度≤9%–牛奶中的去甲基文拉法辛，牛奶和血浆中的二甲双胍≤7%。在来自哺乳期妇女的 228 个供体样本中，西替利嗪的中位乳浓度为 13 ng/mL（范围：0.65 – 65 ng/mL）。