antacid

抗酸剂
  • 文章类型: Journal Article
    农业废物是生物资源利用不足以及缺乏以适当方式或循环经济方法重新利用这种废物的知识的结果。在印度的医疗系统中,Cyperusscariosus(CS)的根由于其重要的药用特性而被大规模使用。不幸的是,CS的空中部分被视为农业废物,是未充分利用的生物资源。由于缺乏知识,CS被视为杂草。本研究是首次尝试探索CS叶作为药用和营养丰富的来源。确定被忽略部分的莎草R.Br.的食物和营养价值。(CS),即CS叶,通过新开发的HPLC和基于ICPOES的方法对CS的植物化学物质和金属离子进行定量。在咖啡酸的HPLC分析中观察到的植物化学物质的含量,儿茶素,表儿茶素,反式-对-香豆酸,反式阿魏酸为10.51、276.15、279.09、70.53和36.83µg/g,分别。在GC-MS/MS分析中,脂肪酸包括亚麻酸,植物醇,棕榈酸,等。已确定。在ICPOES分析中,Na的显著含量,K,Ca,Cu,Fe,Mg,Mn,并观察到Zn。CS叶的TPC和TFC为17.933mgGAEq。/g和130.767mgQCEeq。与标准品(CaCO3)相比,在DPPH测定中以及2.78mg/mL的IC50值和更好的抗酸活性。CS叶的甲醇提取物对金黄色葡萄球菌(15±2mm)具有抗微生物活性,铜绿假单胞菌(12±2mm)和大肠杆菌(10±2mm)。计算机模拟研究证实了从抗氧化剂获得的体外结果,抗酸剂,和抗微生物研究。此外,计算机模拟研究揭示了CS叶的抗癌和抗炎潜力。这项研究,因此,证明了CS未充分利用部分的药用意义,以及将农业废物转化为人类活性的药物有效材料。因此,本研究强调,CS叶具有良好的营养效用,具有重要的药用价值,在制药行业具有巨大的潜力,以及改善生物价值和环境。
    Agro-waste is the outcome of the under-utilization of bioresources and a lack of knowledge to re-use this waste in proper ways or a circular economy approach. In the Indian medicinal system, the root of Cyperus scariosus (CS) is used at a large scale due to their vital medicinal properties. Unfortunately, the aerial part of CS is treated as agro-waste and is an under-utilized bioresource. Due to a lack of knowledge, CS is treated as a weed. This present study is the first ever attempt to explore CS leaves as medicinally and a nutrient rich source. To determine the food and nutritional values of the neglected part of Cyperus scariosus R.Br. (CS), i.e. CS leaves, phytochemicals and metal ions of CS were quantified by newly developed HPLC and ICPOES-based methods. The content of the phytochemicals observed in HPLC analysis for caffeic acid, catechin, epicatechin, trans-p-coumaric acid, and trans-ferulic acid was 10.51, 276.15, 279.09, 70.53, and 36.83 µg/g, respectively. In GC-MS/MS analysis, fatty acids including linolenic acid, phytol, palmitic acid, etc. were identified. In ICPOES analysis, the significant content of Na, K, Ca, Cu, Fe, Mg, Mn, and Zn was observed. The TPC and TFC of the CS leaves was 17.933 mg GAE eq./g and 130.767 mg QCE eq./g along with an IC50 value of 2.78 mg/mL in the DPPH assay and better antacid activity was measured than the standard (CaCO3). The methanolic extract of CS leaves showed anti-microbial activity against Staphylococcus aureus (15 ± 2 mm), Pseudomonas aeruginosa (12 ± 2 mm) and Escherichia coli (10 ± 2 mm). In silico studies confirmed the in vitro results obtained from the antioxidant, antiacid, and anti-microbial studies. In addition, in silico studies revealed the anti-cancerous and anti-inflammatory potential of the CS leaves. This study, thus, demonstrated the medicinal significance of the under-utilized part of CS and the conversion of agro-waste into mankind activity as a pharmaceutical potent material. Consequently, the present study highlighted that CS leaves have medicinal importance with good nutritional utility and have a large potential in the pharmaceutical industry along with improving bio-valorization and the environment.
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  • 文章类型: Journal Article
    通常,大多数口服非甾体抗炎药(NSAIDs)由于长期和高剂量给药而存在已知的胃不良反应。在这项研究中,设计了一种基于多单元原位水凝胶珠的新型液体缓释系统来解决这个问题。该系统由海藻酸钠(SA),结冷胶(GG),氧化锌(ZnO),和氧化镁(MgO)。此外,将吲哚布芬加载到系统中以评估其胃粘膜保护作用。这种效果可以归因于局部抗酸剂,胃蛋白酶抑制,和系统的持续药物释放特性。事实证明,储存的固体凝胶系统在摇动后可以经历“固体到液体”的转变。一旦吞下,液体凝胶可以作为水凝胶珠很好地分散在胃中。然后,从每个多单位凝胶珠的外部到内部发生“液体到固体”凝胶化,由中和反应中Zn2+和Mg2+的释放触发。形成的凝胶表现出持续3小时的温和抗酸作用和66.3%的体内胃蛋白酶抑制作用。此外,与用市售制剂(YinDuo®)组治疗的大鼠相比,用吲哚布芬凝胶系统治疗的大鼠显示出具有较小波动的药物血浆浓度对时间的曲线。凝胶系统还表现出延长的Tmax(6.50小时)和降低的Cmax(52.87μg/mL)。此外,使用三种类型的消化性胃溃疡模型验证了凝胶系统的胃粘膜保护作用。这些发现表明,这种多单元原位凝胶可能是一种潜在的NSAID口服液持续释放系统。
    Commonly, most oral non-steroidal anti-inflammatory drugs (NSAIDs) have known gastric adverse reactions due to their long-term and high dose administration. In this study, a novel liquid sustained-release system based on multiple-unit in situ hydrogel beads was designed to address this issue. The system is composed of sodium alginate (SA), gellan gum (GG), zinc oxide (ZnO), and magnesium oxide (MgO). Furthermore, indobufen was loaded into the system to evaluate its gastric mucosal protection effect. This effect can be attributed to the topical antacid, pepsin inhibition, and sustained drug release properties of the system. It was proven that the stored solid gel system could undergo a \"solid to liquid\" transition after shaking. Once swallowed, the liquid gel could disperse well in the stomach as hydrogel beads. Then, the \"liquid to solid\" gelation occurred from the exterior to interior of each multiple-unit gel bead, triggered by the release of Zn2+ and Mg2+ from neutralization reactions. The formed gel demonstrated mild antacid effect that lasted for 3 hours and 66.3% pepsin inhibition in vivo. Moreover, the rats treated with the indobufen gel system showed a drug plasma concentration versus time curve with less fluctuation compared to the rats treated with the marketed preparation (YinDuo®) group. The gel system also exhibited an extended Tmax (6.50 hours) and reduced Cmax (52.87 μg/mL). Additionally, the gastric mucosal protection of the gel system was verified using three types of peptic gastric ulcer models. These findings suggested that this multiple-unit in situ gel could be a potential oral liquid sustained release delivery system for NSAIDs.
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  • 文章类型: Journal Article
    酸中毒,如呼吸性酸中毒和代谢性酸中毒,可由2019年冠状病毒病(COVID-19)感染诱发,并与重症COVID-19患者死亡率增加相关。目前尚不清楚酸中毒是否进一步促进患者的SARS-CoV-2感染,使病毒清除变得困难。抗酸治疗,碳酸氢钠造成钠过载的巨大风险,碳酸氢盐副作用,和低钙血症.因此,迫切需要新的抗酸解毒剂。我们的研究表明,酸中毒相关的pH值为6.8,可通过调节细胞内微丝聚合来增加细胞膜上SARS-CoV-2受体血管紧张素转换酶2(ACE2)的表达,促进SARS-CoV-2假病毒感染。基于此,我们合成了聚谷氨酸-PEG材料,利用钙离子和羧基的络合形成核心,并采用生物矿化方法形成碳酸钙纳米颗粒(CaCO3-NP)纳米解毒剂以中和过量的氢离子(H),并将pH从6.8恢复到约7.4(正常血液pH)。CaCO3-NP有效地防止了由于pH6.8引起的SARS-CoV-2感染效率的提高。我们的研究表明,酸中毒相关的pH促进SARS-CoV-2感染,这表明SARS-CoV-2感染引起的酸中毒增强SARS-CoV-2感染的正反馈回路的存在。因此,酸中毒COVID-19患者的抗酸治疗是必要的。CaCO3-NP可能成为优于碳酸氢钠的有效抗酸纳米解毒剂。
    Acidosis, such as respiratory acidosis and metabolic acidosis, can be induced by coronavirus disease 2019 (COVID-19) infection and is associated with increased mortality in critically ill COVID-19 patients. It remains unclear whether acidosis further promotes SARS-CoV-2 infection in patients, making virus removal difficult. For antacid therapy, sodium bicarbonate poses great risks caused by sodium overload, bicarbonate side effects, and hypocalcemia. Therefore, new antacid antidote is urgently needed. Our study showed that an acidosis-related pH of 6.8 increases SARS-CoV-2 receptor angiotensin-converting enzyme 2 (ACE2) expression on the cell membrane by regulating intracellular microfilament polymerization, promoting SARS-CoV-2 pseudovirus infection. Based on this, we synthesized polyglutamic acid-PEG materials, used complexation of calcium ions and carboxyl groups to form the core, and adopted biomineralization methods to form a calcium carbonate nanoparticles (CaCO3-NPs) nanoantidote to neutralize excess hydrogen ions (H+), and restored the pH from 6.8 to approximately 7.4 (normal blood pH). CaCO3-NPs effectively prevented the heightened SARS-CoV-2 infection efficiency due to pH 6.8. Our study reveals that acidosis-related pH promotes SARS-CoV-2 infection, which suggests the existence of a positive feedback loop in which SARS-CoV-2 infection-induced acidosis enhances SARS-CoV-2 infection. Therefore, antacid therapy for acidosis COVID-19 patients is necessary. CaCO3-NPs may become an effective antacid nanoantidote superior to sodium bicarbonate.
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  • 文章类型: Journal Article
    This population-based study demonstrates a strong link between Mg-containing antacid exposure and hip fracture risk in nondialysis CKD and dialysis patients. As an Mg-containing antacid, MgO is also commonly used as a stool softener, which can be effortlessly replaced by other laxatives in CKD patients to maintain bone health.
    OBJECTIVE: Bone fracture is a severe complication in chronic kidney disease (CKD) patients, leading to disability and reduced survival. In CKD patients, blood magnesium (Mg) concentrations are usually above the normal range due to reduced kidney excretion of Mg. The present study examines the association between Mg-containing antacid exposure and the risk of hip fracture of CKD patients.
    METHODS: In this nationwide nested case-control study, we enrolled 44,062 CKD patients with hip fracture and 44,062 CKD matched controls, among which the mean age was 77.1 years old, and 87.9% was nondialysis CKD.
    RESULTS: As compared to non-users, Mg-containing antacid users were significantly more likely to experience hip fracture (adjusted odds ratio (OR) 1.36, 95% CI, 1.32 to 1.41; p < 0.001). Subgroup analysis showed that such risk exists in both nondialysis CKD patients and long-term dialysis patients. In contrast, aluminum or calcium-containing-antacid use did not reveal such association. Next, we examined the influence of Mg-containing antacid dosage on hip fracture risk, the adjusted ORs in the first quartile (Q1), Q2, Q3, and Q4 were 1.20 (95% CI, 1.15 to 1.25; p < 0.001), 1.35 (95% CI, 1.30 to 1.41; p < 0.001), 1.49 (95% CI, 1.43 to 1.56; p < 0.001), and 1.54 (95% CI, 1.47 to 1.61; p < 0.001), respectively, showing that such risk exists regardless of the antacid dosage. A receiver operating characteristic curve analysis demonstrated that the best cutoff value of the exposed Mg dose to discriminate the hip fracture is 532 mEq during the follow-up period.
    CONCLUSIONS: This population-based study demonstrates a strong link between Mg-containing antacid exposure and the hip fracture risk in both nondialysis CKD and dialysis patients.
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