Riess Jean G
MRI Institute, University of California at San Diego, San Diego, California, USA.
Artif Cells Blood Substit Immobil Biotechnol. 2005;33(1):47-63. doi: 10.1081/bio-200046659.
The unique behavior of perfluorocarbons (PFCs), including their high oxygen dissolving capacity, hydrophobic and lipophobic character, and extreme inertness, derive directly, in a predictable manner, from the electronic structure and spatial requirements of the fluorine atom. Their low water solubility is key to the prolonged in vivo persistence of the now commercially available injectable microbubbles that serve as contrast agents for diagnostic ultrasound imaging. Oxygent, a stable, small-sized emulsion of a slightly lipophilic, rapidly excreted PFC, perfluorooctyl bromide (perflubron), has been engineered. Significant oxygen delivery has been established in animal models and through Phase II and III human clinical trials. However, an inappropriate testing protocol and the lack of funding led to temporary suspension of the trials.
全氟碳化合物(PFCs)具有独特的性质,包括高氧溶解能力、疏水性和疏脂性以及极高的惰性,这些性质以可预测的方式直接源于氟原子的电子结构和空间需求。它们的低水溶性是目前作为诊断超声成像造影剂的市售可注射微泡在体内长期存留的关键。已经研制出了Oxygent,它是一种稳定的、小尺寸的乳液,含有一种略带亲脂性、排泄迅速的全氟碳化合物——全氟辛基溴(全氟溴辛烷)。在动物模型以及通过II期和III期人体临床试验已证实其具有显著的氧输送能力。然而,不恰当的测试方案和资金短缺导致试验暂时中止。