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在一项开放标签的1期单臂研究中,单次服用植物源生物等效无机硝酸盐口服补充剂后唾液和血浆N-氧化物的药代动力学。

The Pharmacokinetics of Saliva and Plasma N-Oxides Following a Single Administration of a Plant-Based Bioequivalent Inorganic Nitrate Oral Supplement in an Open-Label, Phase 1, Single-Arm Study.

作者信息

Stahl Macy E, Grammer Emily E, Allen Jason D, Weltman Arthur

机构信息

Department of Kinesiology, University of Virginia, Charlottesville, VA 22903, USA.

School of Medicine, University of Virginia, Charlottesville, VA 22903, USA.

出版信息

J Clin Med. 2025 Jun 27;14(13):4581. doi: 10.3390/jcm14134581.

DOI:10.3390/jcm14134581
PMID:40648959
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12250075/
Abstract

Hypertension and other modifiable risk factors for cardiovascular disease are characterized by a dysfunctional vascular endothelium and decreased nitric oxide (NO) bioavailability. The oral supplementation of inorganic nitrate (NO) has been shown to increase the salivary and plasma nitrite (NO), a precursor to NO, though there may be significant variation in the pharmacokinetics of this process between different supplements. The purpose of this open-label, phase 1, single-arm study was to investigate the pharmacokinetic profile of the plasma and salivary NO and NO concentrations following the administration of a single serving of a plant-based bioequivalent inorganic nitrate oral supplement ("Berkeley Life Nitric Oxide Foundation Capsules", Chicago, IL, USA). Nine males and three females (age: 33 ± 15 years; BP: 129 ± 6 mmHg; BMI: 27.58 ± 4.27 kg/m) participated in the protocol. Following the baseline collection of saliva and plasma samples, the participants consumed 314 mg (two capsules) of the supplement. Saliva and plasma samples were collected at 2 h, 4 h, 8 h, and 24 h post consumption. The peak salivary NO (13,326.12 ± 4926.60 µM), salivary NO (1375.27 ± 679.28 µM), plasma NO (498.37 ± 168.89 µM), and plasma NO (231.66 ± 97.26 nM) were observed at 2 h post-supplementation ( < 0.01 vs. the baseline). The concentrations of the salivary and plasma NO remained elevated at 8 h after administration (220% and 50% above the baseline, respectively), and the concentrations of the salivary and plasma NO remained elevated at 24 h after administration (22% and 50% above the baseline, respectively). These data suggest that a single serving of "Berkeley Life Nitric Oxide Foundation Capsules" taken once to twice per day is a viable strategy to provide sustained salivary and plasma NO and NO availability over 24 h and therefore may provide a viable approach for long-term blood pressure maintenance.

摘要

高血压和心血管疾病的其他可改变风险因素的特征是血管内皮功能失调和一氧化氮(NO)生物利用度降低。口服补充无机硝酸盐(NO)已被证明可增加唾液和血浆中亚硝酸盐(NO的前体)的含量,不过不同补充剂在此过程中的药代动力学可能存在显著差异。这项开放标签的1期单臂研究的目的是调查单次服用一种植物源生物等效无机硝酸盐口服补充剂(“伯克利生命一氧化氮基础胶囊”,美国伊利诺伊州芝加哥)后血浆和唾液中NO及亚硝酸盐浓度的药代动力学特征。9名男性和3名女性(年龄:33±15岁;血压:129±6 mmHg;体重指数:27.58±4.27 kg/m²)参与了该方案。在收集唾液和血浆样本作为基线后,参与者服用了314毫克(两粒胶囊)的补充剂。在服用后2小时、4小时、8小时和24小时收集唾液和血浆样本。补充剂服用后2小时观察到唾液中NO(13,326.12±4926.60微摩尔)、唾液中亚硝酸盐(1375.27±679.28微摩尔)、血浆中NO(498.37±168.89微摩尔)和血浆中亚硝酸盐(231.66±97.26纳摩尔)的峰值(与基线相比,P<0.01)。服用后8小时唾液和血浆中NO的浓度仍高于基线(分别比基线高220%和50%),服用后24小时唾液和血浆中NO的浓度仍高于基线(分别比基线高22%和50%)。这些数据表明,每天服用1至2次“伯克利生命一氧化氮基础胶囊”是一种可行的策略,可在24小时内持续提供唾液和血浆中的NO及亚硝酸盐,因此可能为长期维持血压提供一种可行的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/d38dbdf328e6/jcm-14-04581-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/ce7ab14fbf61/jcm-14-04581-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/9329d95992d3/jcm-14-04581-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/2e17e29e91e3/jcm-14-04581-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/9745655dc5a2/jcm-14-04581-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/82ff3bf0a52e/jcm-14-04581-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/d38dbdf328e6/jcm-14-04581-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/ce7ab14fbf61/jcm-14-04581-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/9329d95992d3/jcm-14-04581-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/2e17e29e91e3/jcm-14-04581-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/9745655dc5a2/jcm-14-04581-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/82ff3bf0a52e/jcm-14-04581-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a99/12250075/d38dbdf328e6/jcm-14-04581-g006.jpg

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