bio-availability

生物可用性
  • 文章类型: Journal Article
    背景:木犀草素(LUT),一种在蔬菜中发现的天然类黄酮,水果,和草药,其药理活性已被广泛研究,包括对各种癌细胞系的抗增殖和抗癌作用。它还表现出有效的抗氧化特性和针对人类癌症的促凋亡活性。然而,其在水中的溶解性差(45°C时为5μg/ml)和生物利用度低,阻碍了其治疗潜力。本研究开发木犀草素负载纳米载体的目的是克服这些限制,从而为癌症治疗开辟了新的可能性。
    方法:本文涵盖了为提高LUT的溶解度和生物利用度而研究的几种纳米制剂。纳米制剂的物理化学特性影响木犀草素的溶解度和生物利用度已成为更深入研究的主题。此外,它研究了LUT的抗炎和抗氧化特性如何帮助减轻化疗的副作用。
    结果:大多数纳米配方,包括植物体,脂质纳米粒,脂质体,蛋白质纳米颗粒,聚合物胶束,纳米乳液,和金属纳米粒子,在提高LUT的溶解度和生物利用度方面显示出有希望的结果。这是提高LUT在癌症治疗中的治疗潜力的重要一步。此外,研究发现,LUT清除自由基的能力可以显著降低癌症治疗的副作用,进一步强调其改善患者预后的潜力。
    结论:纳米配方,由于其独特的表面和生理化学性质,提高LUT的溶解度和生物利用度。然而,需要解决纳米制剂的弱的体外和体内相关性和可扩展性,以实现LUT在肿瘤学中的良好临床性能。
    BACKGROUND: Luteolin (LUT), a naturally occurring flavonoid found in vegetables, fruits, and herbal medicines, has been extensively studied for its pharmacological activities, including anti-proliferative and anticancer effects on various cancer lines. It also exhibits potent antioxidant properties and pro-apoptotic activities against human cancers. However, its therapeutic potential is hindered by its poor solubility in water (5 μg/ml at 45°C) and low bioavailability. This research on the development of luteolin-loaded nanocarrier aims to overcome these limitations, thereby opening up new possibilities in cancer treatment.
    METHODS: This paper covers several nanoformulations studied to increase the solubility and bioavailability of LUT. The physicochemical characteristics of the nanoformulation that influence luteolin\'s solubility and bioavailability have been the subject of more in-depth investigation. Furthermore, it examines how LUT\'s anti-inflammatory and antioxidant properties aid in lessening the side effects of chemotherapy.
    RESULTS: Most nanoformulations, including phytosomes, lipid nanoparticles, liposomes, protein nanoparticles, polymer micelles, nanoemulsions, and metal nanoparticles, have shown promising results in improving the solubility and bioavailability of LUT. This is a significant step forward in enhancing the therapeutic potential of LUT in cancer treatment. Furthermore, the study found that LUT\'s ability to scavenge free radicals can significantly reduce the side effects of cancer treatment, further highlighting its potential to improve patient outcomes.
    CONCLUSIONS: Nanoformulations, because of their unique surface and physiochemical properties, improve the solubility and bioavailability of LUT. However, poor in-vitro and in-vivo correlation and scalability of nanoformulations need to be addressed to achieve good clinical performance of LUT in oncology.
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  • 文章类型: Journal Article
    海藻消费是人体砷的主要内部暴露源之一。然而,由于缺乏具有代表性的砷物种的生物利用率,因此无法准确评估源自海藻消费的砷健康风险。在这里,调查了从中国福建采集的各种海藻中的砷种类,并在体外和体内评估了海藻中砷物种的生物可及性/生物利用率。结果表明,在海藻中存在的砷物种的体外生物利用率,用Caco-2细胞获得的,低于纯砷标准,并随无机砷(iAs)>二甲基亚砷酸(DMA)≈砷甜菜碱(AsB)>砷糖的顺序而变化。在小鼠的胃肠道消化过程中,As5+部分甲基化成单甲基arsonic酸(MMA)和DMA,这使得通过小鼠代谢实验获得的iAs的体内生物利用度(31.8%)远高于其体外生物利用度(10.3%)。DMA和总砷(tAs)的体内生物利用度与它们的体外生物利用度相似。作为大多数海藻中的主要砷物种,砷糖的体内生物利用度是0.0%,而体外生物利用度只有3.7%。目标危害商(THQ)和目标癌症风险(TR)的模拟计算表明,考虑到砷的种类和生物利用率,海藻中砷的风险大大降低。从福建收集的所有海藻都是安全食用的。模拟计算还表明,根据tAs和生物利用度,还可以更准确地评估海藻的砷风险,为海藻砷的风险评估提供了一种简单而准确的保护性方法。我们的工作提供了海藻中存在的砷物种的可能代表性生物利用率,以准确评估海藻的砷风险。以及对动物体内砷的生物利用率的新见解。
    Seaweeds consumption is one of main internal exposure sources of arsenic for human. However, the absence of representative bio-availabilities of arsenic species makes the accurate assessment of arsenic health risk originating from seaweeds consumption impossible. Herein, the arsenic species in various seaweeds collected from Fujian of China were investigated, and the bio-accessibilities/bio-availabilities of arsenic species existing in seaweeds were evaluated in vitro and in vivo. Results revealed that in vitro bio-availabilities of arsenic species presenting in seaweeds, which obtained with Caco-2 cells, were lower than those of pure arsenic standards, and varied with order of inorganic arsenic (iAs) > dimethylarsinic acid (DMA) ≈ arsenobetaine (AsB) > arsenosugars. During gastrointestinal digestion of mice, As5+ was partly methylated into monomethylarsonic acid (MMA) and DMA, which makes the in vivo bioavailability of iAs (⁓31.8 %) obtained with mouse metabolic experiment is much higher than its in vitro bio-availability (⁓10.3 %). The in vivo bio-availabilities of DMA and total arsenic (tAs) are similar to their in vitro bio-availabilities. As the dominant arsenic species in most seaweeds, arsenosugars have an ⁓0.0 % of in vivo bioavailability and only a ⁓3.7 % of in vitro bioavailability. The simulated calculation of target hazard quotient (THQ) and target cancer risk (TR) revealed that the arsenic risk originating from seaweeds was greatly degraded by taking into consideration of arsenic species and bio-availabilities, and all seaweeds collected from Fujian are safety for consumption. The simulated calculation also revealed that arsenic risk of seaweeds can be also more accurately assessed based on tAs together with bioavailability, which provides a simple but accurate and protective method for the risk assessment of arsenic originating from seaweeds. Our work provides the possible representative bio-availabilities of arsenic species presenting in seaweeds for accurately assessing arsenic risk of seaweeds, and novel insights into the bio-availabilities of arsenic in animal.
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  • 文章类型: Journal Article
    Climate changes are one of the biggest threats to food security. Sustainable agriculture, focused on eco-friendly practices for highly efficient food production, enables greater resilience and safety. This study experimented on intercropping and bio-fertilizer application as convenient ecological solutions for crop yield stability and quality. The experiment was conducted during 2018 and 2020 with soybean and common millet sown in three sowing patterns: alternating rows, alternating strips 1 (2 rows of soybean + 2 rows of millet), and alternating strips 2 (2 rows of soybean + 4 rows of millet), as well as sole crops (control), with or without a bio-fertilizer Coveron. Grain yield and nutrient grain yield response were calculated through land equivalent ratio (LER) and element-LER (E-LER), while quality was estimated based on the concentration of antioxidants (phytate phosphorus, total phenolic compounds, and yellow pigment) and elements in grains, including potential bio-availability of essential elements. Results revealed LER values to be >1 for all sowing patterns, with the highest one achieved in alternating strips 1 (1.38) together with a greater level of all antioxidants in millet grain. Intercropping significantly enhanced Fe and Mn accumulation in both crops and simultaneously decreased the concentration of potentially toxic elements (Al, Cr) in millet grain. Potential bio-availability of essential elements, expressed through the ratio between phytic acid and Ca, Mg, Fe, and Zn revealed smaller values in intercropped soybean and millet with the bio-fertilizer. The bio-fertilizer also increased the concentration of some micro-elements in millet grain, classifying it as a highly dependent plant to microbial inoculation. Interaction of intercropping and bio-fertilizer was most pronounced for LER, E-LER, and accumulation of Fe and Mn in grains. These results highlighted the benefits of soybean-common millet intercropping, especially in combination with the bio-fertilizer, in light of enhanced land utilization and nutrient absorption, thus increasing the resilience of soybean and millet under dry land conditions and low-input systems toward stability and food security.
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  • 文章类型: Journal Article
    筛选环保高效Cd污染修复材料,分析了Cd暴露条件下BC和BF对土壤Cd生物有效性和棉花Cd吸收的影响。此外,还分析了生物炭(BC)和生物肥料(BF)影响Cd污染土壤和棉花的代谢机制的差异。结果表明,施用BC和BF增加了棉花干物质积累,棉铃号,和单棉铃重量,降低了棉花根中的Cd含量,茎,叶子,还有Bolls.在收获的时候,BC和BF组棉花根中Cd含量分别降低了15.23%和16.33%,分别,与控制相比。这归因于BC和BF将碳酸盐结合的Cd(碳Cd)和可交换Cd(EX-Cd)转化为残留Cd(Res-Cd)。应当指出,BF组土壤有效Cd(Ava-Cd)含量低于BC组。代谢组学分析结果表明,对于BC和BF,差异代谢产物咖啡酸的相对丰度,Xanthurenicacid,土壤和棉花根系中的莽草酸表达上调。Mantel检验发现,棉花根系渗出液l-Histinine与棉花各器官中Cd的富集有关。因此,施用BC和BF可以通过降低土壤Ava-Cd含量和棉花对Cd的吸收来缓解Cd胁迫,在降低土壤和棉花器官中Cd含量方面,BF优于BC。本研究将为开发高效的Cd污染碱性土壤修复技术提供参考,并为后续的宏基因组学分析提供依据。
    To screen environmentally friendly and efficient Cd pollution remediation material, the effects of BC and BF on soil Cd bio-availability and cotton Cd absorption were analyzed under Cd exposure. Besides, the differences in metabolic mechanisms by which biochar (BC) and biofertilizer (BF) affect Cd-contaminated soil and cotton were also analyzed. The results showed that the application of BC and BF increased cotton dry matter accumulation, boll number, and single boll weight, and reduced the Cd content in cotton roots, stems, leaves, and bolls. At harvest, the Cd content in cotton roots in the BC and BF groups reduced by 15.23% and 16.33%, respectively, compared with that in the control. This was attributed to the conversion of carbonate-bound Cd (carbon-Cd) and exchangeable Cd (EX-Cd) by BC and BF into residual Cd (Res-Cd). It should be noted that the soil available Cd (Ava-Cd) content in the BF group was lower than that in the BC group. The metabolomic analysis results showed that for BC vs BF, the relative abundance of differential metabolites Caffeic acid, Xanthurenic acid, and Shikimic acid in soil and cotton roots were up-regulated. Mantel test found that cotton root exudate l-Histinine was correlated with the enrichment of Cd in various organs of cotton. Therefore, the application of BC and BF can alleviate Cd stress by reducing soil Ava-Cd content and cotton\'s Cd uptake, and BF is superior to BC in reducing Cd content in soil and cotton organs. This study will provide a reference for the development of efficient techniques for the remediation of Cd-polluted alkaline soil, and provide a basis for subsequent metagenomics analysis.
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  • 文章类型: Journal Article
    这篇综述的目的是收集有关番茄红素及其异构体的相关化学数据,可以使用不同的非极性或极性非质子溶剂通过SC-CO2或生物合成作为友好技术提取。番茄红素和其他类胡萝卜素可以通过UV-Vis和HPLC使用C18或C30柱进行鉴定和定量。虽然它们的表征可以通过紫外-可见,荧光,FTIR,MS,NMR,和DSC分析。在这些技术中,最后四个可以比较番茄红素的异构体和识别顺式或全反式番茄红素。FTIR,MS,和NMR技术更适合于验证番茄红素提取物的纯度,由于每个异构体产生的信号复杂性,这使得能够通过细微的差异来识别。此外,从红色蔬菜中分离出的番茄红素的一些生物活性已经得到证实,如抗炎,抗氧化剂,和对癌细胞的细胞毒活性,可能是通过激活几种途径。番茄红素在纳米颗粒中的封装证明了口服递送的改善,和离体评估确定这些纳米颗粒具有更好的渗透性和对人细胞的低细胞毒性,具有增强的渗透性。这些数据表明,番茄红素具有在食品和制药工业中应用的潜力,以及化妆品。
    The purpose of this review was to collect relevant chemical data about lycopene and its isomers, which can be extracted using different non-polar or polar aprotic solvents by SC-CO2 or biosynthesis as a friendly technique. Lycopene and other carotenoids can be identified and quantified by UV-Vis and HPLC using a C18 or C30 column, while their characterization is possible by UV-Vis, Fluorescence, FTIR, MS, NMR, and DSC assays. Among these techniques, the last four can compare lycopene isomers and identify cis or all-trans-lycopene. FTIR, MS, and NMR techniques are more suitable for the verification of the purity of lycopene extracts due to the signal complexity generated for each isomer, which enables identification by subtle differences. Additionally, some biological activities of lycopene isolated from red vegetables have already been confirmed, such as anti-inflammatory, antioxidant, and cytotoxic activity against cancer cells, probably by activating several pathways. The encapsulation of lycopene in nanoparticles demonstrated an improvement in oral delivery, and ex vivo assessments determined that these nanoparticles had better permeation and low cytotoxicity against human cells with enhanced permeation. These data suggest that lycopene has the potential to be applied in the food and pharmaceutical industries, as well as in cosmetic products.
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  • 文章类型: Journal Article
    饮食是邻苯二甲酸酯(PAEs)对人类的重要暴露途径。从西安收集了涵盖11个食物组的174个食物样本,中国西北地区典型的山谷城市,并分析评估食品中PAEs的发生和暴露风险。检测到22例PAEs。22个PAEs的总和(∑22PAEs)在0.0340和56.8µg/g之间变化,平均值为3.94微克/克。主要的PAEs是邻苯二甲酸二异丁酯(DiBP),邻苯二甲酸二正丁酯(DnBP),邻苯二甲酸二(2-乙基己基)酯(DEHP),邻苯二甲酸二异壬酯(DiNP),和邻苯二甲酸二异癸酯(DiDP),这主要与增塑剂的使用有关。合并的消化胃肠液模拟物中PAEs的生物利用度高于单一的胃或肠液模拟物中PAEs的生物利用度。在三种模拟物中,双(2-甲氧基乙基)邻苯二甲酸酯均表现出最高的生物利用度。PAEs的生物利用度与PAEs的分子量和辛醇-水分配系数呈负相关,与PAEs的溶解度和蒸汽压呈正相关。根据国家和城市食品消费数据估算的PAEs每日摄入量(EDI)低于美国环境保护局的参考剂量(RfD)和欧洲食品安全局(EFSA)的可容忍乳制品摄入量(TDI)。除了DnBP和DiBP的EDI高于EFSA的TDI。谷物和蔬菜是人类膳食暴露于PAEs的主要来源。人类饮食暴露于PAEs的危险商数小于临界值1,邻苯二甲酸丁酯苄酯和DEHP的癌症风险在10-11-10-6的范围内,表明相对较低的健康风险。结果表明,人类暴露于DnBP,DiBP,DEHP,DiNP,食品中的DiDP是相当大的,也是一个健康问题。
    Diet is an important exposure pathway of phthalate esters (PAEs) for humans. A total of 174 food samples covering 11 food groups were collected from Xi\'an, a typical valley city in Northwest China, and analyzed to assess the occurrence and exposure risks for PAEs in the food. Twenty-two PAEs were detected. The sum of the 22 PAEs (∑22PAEs) varied between 0.0340 and 56.8 µg/g, with a mean of 3.94 µg/g. The major PAEs were di-iso-butyl phthalate (DiBP), di-n-butyl phthalate (DnBP), bis(2-ethylhexyl) phthalate (DEHP), di-iso-nonyl phthalate (DiNP), and di-iso-decyl phthalate (DiDP), which were associated mainly with the usage of plasticizers. Bio-availability of the PAEs in the combined gastro-intestinal fluid simulant of digestion was higher than that in the single gastric or intestinal fluid simulant. Bis(2-methoxyethyl) phthalate exhibited the highest bio-availability in each of the three simulants. Bio-availability of the PAEs was negatively correlated with the molecular weight and octanol-water partition coefficient of the PAEs and positively correlated with the solubility and vapor pressure of the PAEs. The estimated daily intake (EDI) of PAEs based on national and municipal food consumption data was lower than the reference dose (RfD) of the United States Environmental Protection Agency and the tolerable dairy intake (TDI) of European Food Safety Authority (EFSA), except for the EDI of DnBP and DiBP being higher than the TDI of EFSA. Grains and vegetables were the major sources of human dietary exposure to PAEs. The hazardous quotient for human dietary exposure to PAEs was less than the critical value of 1 and the cancer risk of butyl benzyl phthalate and DEHP was in the range of 10-11-10-6, suggesting relatively low health risks. The results indicated that human exposure to DnBP, DiBP, DEHP, DiNP, and DiDP in food is considerable and a health concern.
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  • 文章类型: Journal Article
    白藜芦醇是广泛存在于葡萄和红葡萄酒中的多酚二苯乙烯衍生物。以其抗氧化作用而广为人知,大量研究还表明,它具有抗炎和抗衰老的能力,在癌症治疗中具有巨大的潜力。遗憾的是,白藜芦醇的口服给药具有药代动力学和物理化学限制,例如阻碍其作用,因此需要有效的给药方法来确保其效率。因此,本综述探讨了白藜芦醇纳米制剂在癌症治疗中应用的已发表数据,使用不同类型的纳米递送系统。在癌症治疗中具有潜在用途的作用机制,负面影响,白藜芦醇纳米制剂在不同类型癌症中的影响也被强调。最后,还讨论了纳米白藜芦醇的毒理学特征。
    Resveratrol is a polyphenolic stilbene derivative widely present in grapes and red wine. Broadly known for its antioxidant effects, numerous studies have also indicated that it exerts anti-inflammatory and antiaging abilities and a great potential in cancer therapy. Regrettably, the oral administration of resveratrol has pharmacokinetic and physicochemical limitations such as hampering its effects so that effective administration methods are demanding to ensure its efficiency. Thus, the present review explores the published data on the application of resveratrol nanoformulations in cancer therapy, with the use of different types of nanodelivery systems. Mechanisms of action with a potential use in cancer therapy, negative effects, and the influence of resveratrol nanoformulations in different types of cancer are also highlighted. Finally, the toxicological features of nanoresveratrol are also discussed.
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  • 文章类型: Journal Article
    背景:铅(Pb)不是茶树生长的必需元素,但它是评价茶叶质量和安全性的重要指标。铅是对pH敏感的金属。探讨土壤酸化对土壤Pb的变化趋势和茶叶中Pb的富集系数对茶叶种植和茶叶质量安全控制具有重要意义。
    结果:中国安溪县364个茶园中有37.57%的人表现出土壤酸化,即土壤pH值<4.5。然而,土壤中总铅和茶叶中铅的含量均达到了中国规定的要求。土壤有效Pb含量和茶叶中Pb含量均与土壤pH值呈极显著负相关,随着土壤pH值的降低而增加。土壤有效Pb含量与土壤总Pb含量呈显著正相关。然而,土壤总Pb含量与土壤pH值无显著相关性。此外,土壤Pb生物有效性系数和茶叶Pb富集系数随土壤pH值的增加而降低。
    结论:安溪县超过三分之一的茶园已经酸化。pH值的降低导致土壤Pb含量的生物有效性系数和茶叶中Pb含量的富集系数增加。较低的土壤pH值导致茶树对Pb的吸收和积累增加,从而增加了茶叶中铅的含量。©2021年化学工业学会。
    BACKGROUND: Lead (Pb) is not an essential element for the growth of tea trees, but it is an important index for evaluating the quality and safety of tea. Lead is a sensitive metal to pH. Exploring the changing trend of soil Pb and enrichment coefficient of Pb in tea leaves affected by soil acidification is significant for tea planting and tea quality safety control.
    RESULTS: A percent of 37.57% of the 364 tea plantations in Anxi county of China showed soil acidification that is a soil pH value < 4.5. However, the total Pb content in the soil and Pb content of tea leaves met the requirements stipulated in China. The soil available Pb content and Pb content in tea leaves were both significantly negatively correlated with soil pH value, and increased with the decrease of soil pH value. The soil available Pb content had a significant positive correlation with soil total Pb content. However, the soil total Pb content had no significant correlation with soil pH value. Moreover, the soil Pb bio-availability coefficient and the Pb enrichment coefficient of tea leaves decreased with the increase of soil pH value.
    CONCLUSIONS: More than a third of tea plantations in Anxi county had been acidified. The decrease of pH value leads to an increase in the bio-availability coefficient of soil Pb content and the enrichment coefficient of Pb content in tea leaves. The lower soil pH value resulted in the increase of the absorption and accumulation of Pb by tea trees, thus an increase of Pb content in tea leaves. © 2021 Society of Chemical Industry.
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  • 文章类型: Journal Article
    生物炭在减少有毒重金属的生物利用度和最大程度地减少从污染土壤进入食物链的威胁方面获得了关注。这项研究的目的是评估啤酒污泥生物炭(BSB)作为土壤改良剂的潜在用途,以减少镉的生物有效性和甘蓝型油菜在盆栽实验中的吸收。在这个锅实验中,人工添加镉,适度肥沃,并使用了微碱性粉质壤土。生物炭是通过在500°C下热解啤酒厂污泥而产生的。将获得的生物炭用0.5mm的筛目尺寸筛分,并以4%(w/w)的比率施用在芸苔属植物生长的掺镉土壤上。向土壤中添加BSB可以显着降低土壤中镉的生物有效性及其在甘蓝型油菜茎中的积累,分别降低86%和93%,分别。此外,它使甘蓝型油菜可食部分的干重显着增加了228%。结果表明,BSB是镉固定化中非常有效的添加剂,反过来,显着(p值=0.00)促进蔬菜(甘蓝型油菜)生长。因此,BSB可用作镉污染的农业土壤补救措施和啤酒污泥的安全处置。
    Biochar has gained an attention in reducing the bio-availability of toxic heavy metals and minimize threat of entering into food chain from contaminated soil. This study was aimed at evaluating the potential use of brewery sludge biochar (BSB) as a soil amendment for reducing cadmium bio-availability and uptake by Brassica carinata in a pot experiment. In this pot experiment, artificially cadmium spiked, moderately fertile, and slightly basic silty-loam soil was used. The biochar was produced by pyrolyzing of the brewery sludge at 500 °C. The obtained biochar was sieved with 0.5 mm mesh size and applied at the rate of 4 % (w/w) on the Brassica carinata grown cadmium spiked soil. The additions of BSB to the soil contributed a significant reduction of the bio-availability of cadmium in the soil and its accumulation in the shoot of Brassica carinata by 86% and 93%, respectively. Besides, it remarkably increased the dry weight of the edible part of Brassica carinata by 228%. The results revealed that BSB is very effective additive in cadmium immobilization, in turn, significantly (p-value = 0.00) promoting vegetable (Brassica carinata) growth. Therefore, BSB can be used as agricultural soil remedy for cadmium contamination and as safe disposal of brewery sludge.
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  • 文章类型: Journal Article
    The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin (Am80-HP-β-CD) was prepared through a freeze-drying method at the mole ratio of 1:1 (Am80: HP-β-CD). Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) indicated the formation of Am80-HP-β-CD. In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80. An improved dissolution with approximately 97% drug release in 3 min was observed, in comparison with Am80 with approximately 60% release in 45 min. In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex. The decrease of tmax indicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster. In short, the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD. Therefore, using the inclusion technique is a promising method to improve the solubility of insoluble drugs.
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