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全氟戊烷乳剂作为一种氧气治疗剂。

Dodecafluoropentane emulsion as an oxygen therapeutic.

机构信息

NuvOx Pharma, Tucson, AZ, USA.

出版信息

Artif Cells Nanomed Biotechnol. 2024 Dec;52(1):462-475. doi: 10.1080/21691401.2024.2402908. Epub 2024 Sep 22.

DOI:10.1080/21691401.2024.2402908
PMID:39308047
Abstract

Dodecafluoropentane emulsion (DDFPe) is a fluorocarbon (FC) under clinical development as an oxygen therapeutic and is regulated as a blood substitute. Compared to all the prior FCs studied, DDFP is the most advantageous for oxygen delivery and it is active at a lower concentration (1/200th to 1/1000th the weight of other FCs). DDFP has a boiling point of 29 °C, is more water soluble than prior FCs, and following IV administration clears exhalation. Prior FCs had boiling points ≥ 140 °C and were retained long-term in the body causing adverse events. DDFP is a gas at biological temperature while prior FCs were liquids. Gases deliver roughly 1000 times more oxygen than liquids. DDFPe has two mechanisms of action: (1) The size of the molecule is the smallest that is a liquid at room temperature; on a molar volume basis this equates to more dissolution of oxygen. (2) Because of its boiling point close to physiologic temperature, DDFP delivers oxygen more effectively than liquid FCs.Highlight PointsFluorocarbons (FCs) dissolve oxygen and other respirable gases.FC emulsions generally do not have biological effects of and by themselves, but rather they increase the oxygen carrying capacity of the blood.There are a variety of FCs that were developed in the past as blood substitutes but they all caused accumulation in humans leading to toxic responses.Dodecafluoropentane emulsion (DDFPe) is being developed as an oxygen therapeutic to increase the oxygen carrying capacity of the blood and oxygen delivery to tissues.

摘要

全氟戊烷乳剂(DDFPe)是一种正在临床开发中的氟碳化合物(FC),可用作氧气治疗剂,并被监管为血液替代品。与之前研究的所有氟碳化合物相比,DDFP 在输送氧气方面最具优势,而且其有效浓度更低(重量为其他氟碳化合物的 1/200 到 1/1000)。DDFP 的沸点为 29°C,水溶性优于之前的氟碳化合物,且静脉给药后可通过呼气清除。之前的氟碳化合物沸点≥140°C,在体内长期滞留,引起不良反应。DDFP 在生理温度下为气体,而之前的氟碳化合物为液体。气体输送的氧气大约是液体的 1000 倍。DDFPe 有两种作用机制:(1)分子大小是室温下呈液态的最小尺寸;按摩尔体积计算,这相当于更多氧气的溶解。(2)由于其沸点接近生理温度,DDFP 比液态 FC 更有效地输送氧气。要点氟碳化合物(FCs)溶解氧气和其他可呼吸气体。FC 乳剂通常没有生物学效应,也不会自行产生效应,而是增加血液的携氧能力。过去曾开发过各种用作血液替代品的 FC,但它们都会在人体内积累,导致毒性反应。全氟戊烷乳剂(DDFPe)正被开发为一种氧气治疗剂,以增加血液的携氧能力和向组织输送氧气。

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