Zarif L, Postel M, Trevino L, Riess J G, Valla A, Follana R
Unité de Chimie Moléculaire, associée au CNRS, Université de Nice-Sophia Antipolis, Parc Valros, France.
Artif Cells Blood Substit Immobil Biotechnol. 1994;22(4):1193-8. doi: 10.3109/10731199409138815.
To investigate the biodistribution, possible metabolism and excretion of mixed fluorocarbon-hydrocarbon "dowel" molecules used as stabilizers of fluorocarbon emulsions, we have prepared a 25% w/v emulsion of such a molecule, and quantitatively evaluated, by means of 19F NMR, its behavior in the blood and reticuloendothelial system (RES) of rats. C6F13CH = CHC10H21 (F6H10E) was emulsified using egg yolk phospholipids (EYP). The emulsion (F6H10E/EYP: 25/6% w/v) was injected intravenously into 33 Sprague Dawley female rats at a 3.6 g/kg body weight dose of F6H10E. The animals were sacrificed at regular intervals of time. 24 hours after the injection, 70% of the injected dose was located in the liver, 17% in the spleen, 4% in the lungs, 2% in the kidneys and 2% in the blood. The half-time retention of the dowel molecule in the liver was estimated to be 25 +/- 5 days. None of the 33 treated animals died prior to the planned sacrifice date. The dowel molecule F6H10E proved to be well tolerated, and excreted reasonably fast, without metabolism. This appears to warrant the use of such molecules as stabilizers in injectable fluorocarbon emulsions destined to serve as oxygen carriers, contrast agents or drug delivery systems.
为了研究用作氟碳乳液稳定剂的氟碳 - 碳氢“销钉”分子的生物分布、可能的代谢和排泄情况，我们制备了这种分子的25%（w/v）乳液，并通过¹⁹F NMR定量评估了其在大鼠血液和网状内皮系统（RES）中的行为。使用蛋黄磷脂（EYP）乳化C6F13CH = CHC10H21（F6H10E）。将乳液（F6H10E/EYP：25/6% w/v）以3.6 g/kg体重的F6H10E剂量静脉注射到33只雌性Sprague Dawley大鼠体内。在定期的时间间隔处死动物。注射后24小时，70%的注射剂量位于肝脏，17%在脾脏，4%在肺，2%在肾脏，2%在血液中。销钉分子在肝脏中的半衰期估计为25±5天。33只接受治疗的动物在计划处死日期之前均未死亡。销钉分子F6H10E被证明耐受性良好，排泄相当快，且无代谢。这似乎保证了将此类分子用作注定要用作氧载体、造影剂或药物递送系统的可注射氟碳乳液的稳定剂。
