Gelijkens C F, Van Peer A, Lenoir H, Knaeps A, Woestenborghs R, Heykants J
Biomed Mass Spectrom. 1985 Jan;12(1):38-42. doi: 10.1002/bms.1200120108.
Lorcainide, a new antiarrhythmic agent currently undergoing clinical trial, has been pentadeuterated and the usefulness of this labelled compound in pharmacokinetic and metabolism studies has been investigated in dogs. Specific analytical methods based on capillary gas chromatography/mass spectrometry (GC/MS) were developed for quantitative and qualitative analysis of plasma and urine samples. Following oral administration of an equimolar mixture of 5 : 5 mg of (2H0/2H5)lorcainide, eight major metabolites were rapidly identified in urine by the ion cluster technique. Quantitative analysis of (2H0/2H5)lorcainide in plasma and urine indicated an enhanced systematic availability of the deuterated compound, probably due to a secondary isotope effect. According to these findings in the dog, the use of deuterated lorcainide in human bioavailability and metabolism studies is probably of limited value.
劳卡尼，一种目前正在进行临床试验的新型抗心律失常药物，已被五氘代，并且已在犬类中研究了这种标记化合物在药代动力学和代谢研究中的用途。开发了基于毛细管气相色谱/质谱联用（GC/MS）的特定分析方法，用于血浆和尿液样本的定量和定性分析。口服5:5毫克（2H0/2H5）劳卡尼的等摩尔混合物后，通过离子簇技术在尿液中迅速鉴定出八种主要代谢物。血浆和尿液中（2H0/2H5）劳卡尼的定量分析表明，氘代化合物的系统可用性增强，这可能是由于二级同位素效应。根据犬类的这些研究结果，氘代劳卡尼在人体生物利用度和代谢研究中的应用可能价值有限。
