Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease

IF 1.6 Q3 MEDICINE, RESEARCH & EXPERIMENTAL
Neal Stolowich Ph.D. , Jason Vittitow Ph.D. , Robert Kissling M.D. , Douglas Borchman Ph.D.
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引用次数: 3

Abstract

Objective

One-hundred percent perfluorohexyloctane (PFHO) is a water-free, preservative-free eye drop approved by the Food and Drug Administration in the United States for the treatment of dry eye disease. PFHO has shown relief of dry eye signs and symptoms in clinical trials and has potent antievaporative action in vitro. The objective of this study was to measure the level of oxygen in PFHO.

Methods

T1 relaxation times (time taken for proton spins to translate from a random alignment to an alignment with the main magnetic field) for fluorine-19 in perfluorohexyloctane were measured using fluorine-19 nuclear magnetic resonance spectroscopy. The level of oxygen was interpolated from published data.

Results

The hydrogen-1 and fluorine-19 nuclear magnetic resonance spectra of PFHO were well resolved and the resonance assignments and intensities were as expected. The T1 values calculated for the CF3 group resonance in the current study was 0.901 seconds and 1.12 seconds at 25 °C and 37 °C, respectively. The T1 values for the CF2 group resonances increased by 17% to 24% with an increase in temperature from 25 °C to 37 °C. The mean (SD) partial pressure of oxygen in PFHO was calculated to be 257 (36) mm Hg and 270 (38) mm Hg at 25 °C and 37 °C, respectively.

Conclusions

The current study confirms that PFHO contains a significant amount of oxygen, more so than that calculated for tears in equilibrium with air. Once instilled on the eye, PFHO is not expected to be a barrier to the oxygen necessary for a healthy cornea and may in fact deliver nonreactive oxygen to the cornea to facilitate healing in patients with dry eye disease.

Abstract Image

Abstract Image

新型干眼病滴眼液全氟己辛烷的携氧能力
目的百分之百全氟己基辛烷(PFHO)是一种经美国食品药品监督管理局批准用于治疗干眼病的无水、不含防腐剂的滴眼液。PFHO在临床试验中显示出对干眼症体征和症状的缓解,并在体外具有强大的抗蒸发作用。本研究的目的是测量PFHO中的氧水平。方法使用氟-19核磁共振光谱测量全氟己基辛烷中氟-19的弛豫时间(质子自旋从随机排列转化为与主磁场排列所需的时间)。根据公布的数据对氧气水平进行插值。结果PFHO的氢-1和氟-19核磁共振谱得到了很好的分辨,共振归属和强度符合预期。当前研究中计算的CF3组共振的T1值在25°C和37°C时分别为0.901秒和1.12秒。随着温度从25°C增加到37°C,CF2组共振的T1值增加了17%到24%。PFHO中氧气的平均分压(SD)在25°C和37°C时分别为257(36)mm Hg和270(38)mm Hg。结论目前的研究证实,PFHO含有大量的氧气,比与空气平衡的眼泪所含的氧气更多。PFHO一旦滴入眼睛,预计不会成为健康角膜所需氧气的屏障,事实上可能会向角膜输送非活性氧气,以促进干眼症患者的愈合。
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来源期刊
CiteScore
3.50
自引率
0.00%
发文量
31
审稿时长
3 months
期刊介绍: We also encourage the submission of manuscripts presenting preclinical and very preliminary research that may stimulate further investigation of potentially relevant findings, as well as in-depth review articles on specific therapies or disease states, and applied health delivery or pharmacoeconomics. CTR encourages and supports the submission of manuscripts describing: • Interventions designed to understand or improve human health, disease treatment or disease prevention; • Studies that focus on problems that are uncommon in resource-rich countries; • Research that is "under-published" because of limited access to monetary resources such as English language support and Open Access fees (CTR offers deeply discounted English language editing); • Republication of articles previously published in non-English journals (eg, evidence-based guidelines) which could be useful if translated into English; • Preclinical and clinical product development studies that are not pursued for further investigation based upon early phase results.
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