Brekle A, Zierenberg O
Arzneimittelforschung. 1985;35(1):130-2.
Deuterium-labelled di-[( 15,15,16,16-2H4]-linoleoyl) -3-sn-glycero-phosphocholine was used as a tracer of the major component of soybean polyene-3-sn-phosphatidylcholine to study the pharmacokinetics of a natural product after oral administration to rats. For this purpose a method was developed to isolate the phosphatidylcholine fraction from blood in a highly purified form. Only 200 pg deuterium-labelled fatty acid generated from the phosphatidylcholine fraction and a ratio of one molecule of deuterium-labelled stearic acid to 500 molecules of stearic acid are necessary for a reproducible measurement by gas chromatography/mass spectrometry. The highest amount of di-[( 15,15,16,16-2H4]-linoleoyl) -3-sn-glycerophosphocholine (0.12% dose/ml, i.e. 2.1% of the maximum absorbed dose) was detected in blood 6 h after administration. The results are comparable with those found after administration of di-[l-14C]-linoleoyl-3-sn-glycerophosphocholine. Hence it is possible to use deuterium-labelled polyenphosphatidylcholine instead of radioactively labelled polyenphosphatidylcholine, especially if a harmless tracer is required.
氘标记的二 - [(15,15,16,16 - 2H₄)-亚油酰基]-3 - 磷酸甘油胆碱被用作大豆多烯 - 3 - 磷酸甘油胆碱主要成分的示踪剂，以研究一种天然产物经口给予大鼠后的药代动力学。为此，开发了一种方法来以高纯度形式从血液中分离磷脂酰胆碱部分。通过气相色谱/质谱法进行可重复测量时，仅需从磷脂酰胆碱部分产生200皮克氘标记脂肪酸，且氘标记硬脂酸与500分子硬脂酸的比例即可。给药后6小时，在血液中检测到最高量的二 - [(15,15,16,16 - 2H₄)-亚油酰基]-3 - 磷酸甘油胆碱（0.12%剂量/毫升，即最大吸收剂量的2.1%）。结果与给予二 - [1 - ¹⁴C]-亚油酰基-3 - 磷酸甘油胆碱后发现的结果相当。因此，尤其是在需要无害示踪剂时，可以使用氘标记的多烯磷脂酰胆碱代替放射性标记的多烯磷脂酰胆碱。
