Kimura T, Sternson L A, Stella V J, Higuchi T
J Natl Cancer Inst. 1977 May;58(5):1311-4. doi: 10.1093/jnci/58.5.1311.
The pharmacokinetics of dianhydrogalactitol (DAG), NSC-132313, were studied in the beagle dog at doses of 3 mg - kg-1 and 6 mg - kg-1. DAG concentrations in plasma were determined by a gas chromatographic method capable of specifically detecting the parent drug and differentiating between it and products of its degradation or metabolism. Plasma disappearance time curves were generated and shown to follow simple two-compartment model behavior after iv administration of DAG. Distribution and elimination of DAG appeared to be dose-independent in the limited dose range studied. After iv administration, the drug was rapidly distributed throughout extracellular fluids (volume of the central compartment = 462 ml - kg-1) and subsequently was rapidly cleared (total body clearance = 23.4 ml - min-1 - kg-1) and eliminated (t1/2, b = 26.2 min) from the animal. Experiments (in vitro) with the use of radiolabeled DAG indicated that the drug binds reversibly and irreversibly to red blood cells.
在比格犬中研究了二脱水半乳糖醇（DAG，NSC - 132313）在3 mg·kg⁻¹和6 mg·kg⁻¹剂量下的药代动力学。通过一种能够特异性检测母体药物并区分其与降解或代谢产物的气相色谱法测定血浆中DAG的浓度。静脉注射DAG后生成血浆消失时间曲线，结果显示其符合简单的二室模型行为。在所研究的有限剂量范围内，DAG的分布和消除似乎与剂量无关。静脉注射后，药物迅速分布至整个细胞外液（中央室容积 = 462 ml·kg⁻¹），随后迅速被清除（总体清除率 = 23.4 ml·min⁻¹·kg⁻¹）并从动物体内消除（t1/2，b = 26.2分钟）。使用放射性标记的DAG进行的（体外）实验表明，该药物与红细胞可逆且不可逆地结合。
