Abstract:The natural sweeteners erythritol and xylitol might be helpful to reduce sugar consumption and therefore prevent obesity and diabetes. The aim of the present study was to determine the absorption and metabolization into erythronate of different concentrations of erythritol and xylitol. Seventeen healthy lean participants received intragastric solutions of 10, 25, or 50 g erythritol or 7, 17, or 35 g xylitol on three study days in a randomized order. The study was double blinded with respect to the doses admini… Show more
“…The in vitro study by Maeng et al, 2019, examining the metabolism of erythritol in human and rat hepatocytes, reported that erythritol is stable and not metabolised. This is in contrast with the evidence emerging from the recent in vivo study by Bordier et al, 2022, from which metabolic transformation to erythronate, although limited, is shown. The Panel noted that the in vitro study used a much lower concentration of erythritol (41 uM) than that of the in vivo study.…”
Section: In Vitrocontrasting
confidence: 96%
“…The peak concentration in plasma was 240 μmol/L (29.3 mg/L) and the cumulative urinary excretion was 3.4 mmol, which corresponds to 41.5% of the dose ingested. Bordier et al (2022) performed a pharmacokinetic cross over study in 12 healthy volunteers receiving a bolus dose of 10, 25 or 50 g of erythritol dissolved in 300 mL tap water. Following ingestion, blood was taken and erythritol and erythronate were measured.…”
Section: In Vivo Studiesmentioning
confidence: 99%
“…For studies retrieved in the literature, only those evaluated as having low to moderate risk of bias (tier 1 or tier 2) were considered further in the assessment (n = 7) (Kim et al, 2011;Meyer-Gerspach et al, 2021;Teysseire et al, 2022Teysseire et al, , 2023Wölnerhanssen et al, , 2021.…”
Section: Studies Included In the Assessmentmentioning
confidence: 99%
“…Reference (authors, year, title, other info) Teysseire, F., Bordier, V., Budzinska, A., Weltens, N., Rehfeld, J. F., Holst, J. J., Hartmann, B., Beglinger, C., Van Oudenhove, L., Wölnerhanssen, B. K. and Meyer-Gerspach, A. C. (2022).…”
This opinion addresses the re-evaluation of erythritol (E 968) as food additive and an application for its exemption from the laxative warning label requirement as established under Regulation (EU) No 1169/2011. Erythritol is a polyol obtained by fermentation with Moniliella pollinis BC or Moniliella megachiliensis KW3-6, followed by purifications and drying. Erythritol is readily and dose-dependently absorbed in humans and can be metabolised to erythronate to a small extent. Erythritol is then excreted unchanged in the urine. It does not raise concerns regarding genotoxicity. The dataset evaluated consisted of human interventional studies. The Panel considered that erythritol has the potential to cause diarrhoea in humans, which was considered adverse because its potential association with electrolyte and water imbalance. The lower bound of the range of no observed adverse effect levels (NOAELs) for diarrhoea of 0.5 g/kg body weight (bw) was identified as reference point. The Panel considered appropriate to set a numerical acceptable daily intake (ADI) at the level of the reference point. An ADI of 0.5 g/kg bw per day was considered by the Panel to be protective for the immediate laxative effect as well as potential chronic effects, secondary to diarrhoea. The highest mean and 95th percentile chronic exposure was in children (742 mg/kg bw per day) and adolescents (1532 mg/kg bw per day). Acute exposure was maximally 3531 mg/kg bw per meal for children at the 99th percentile. Overall, the Panel considered both dietary exposure assessments an overestimation. The Panel concluded that the exposure estimates for both acute and chronic dietary exposure to erythritol (E 968) were above the ADI, indicating that individuals with high intake may be at risk of experiencing adverse effects after single and repeated exposure. Concerning the new application, the Panel concluded that the available data do not support the proposal for exemption.
“…The in vitro study by Maeng et al, 2019, examining the metabolism of erythritol in human and rat hepatocytes, reported that erythritol is stable and not metabolised. This is in contrast with the evidence emerging from the recent in vivo study by Bordier et al, 2022, from which metabolic transformation to erythronate, although limited, is shown. The Panel noted that the in vitro study used a much lower concentration of erythritol (41 uM) than that of the in vivo study.…”
Section: In Vitrocontrasting
confidence: 96%
“…The peak concentration in plasma was 240 μmol/L (29.3 mg/L) and the cumulative urinary excretion was 3.4 mmol, which corresponds to 41.5% of the dose ingested. Bordier et al (2022) performed a pharmacokinetic cross over study in 12 healthy volunteers receiving a bolus dose of 10, 25 or 50 g of erythritol dissolved in 300 mL tap water. Following ingestion, blood was taken and erythritol and erythronate were measured.…”
Section: In Vivo Studiesmentioning
confidence: 99%
“…For studies retrieved in the literature, only those evaluated as having low to moderate risk of bias (tier 1 or tier 2) were considered further in the assessment (n = 7) (Kim et al, 2011;Meyer-Gerspach et al, 2021;Teysseire et al, 2022Teysseire et al, , 2023Wölnerhanssen et al, , 2021.…”
Section: Studies Included In the Assessmentmentioning
confidence: 99%
“…Reference (authors, year, title, other info) Teysseire, F., Bordier, V., Budzinska, A., Weltens, N., Rehfeld, J. F., Holst, J. J., Hartmann, B., Beglinger, C., Van Oudenhove, L., Wölnerhanssen, B. K. and Meyer-Gerspach, A. C. (2022).…”
This opinion addresses the re-evaluation of erythritol (E 968) as food additive and an application for its exemption from the laxative warning label requirement as established under Regulation (EU) No 1169/2011. Erythritol is a polyol obtained by fermentation with Moniliella pollinis BC or Moniliella megachiliensis KW3-6, followed by purifications and drying. Erythritol is readily and dose-dependently absorbed in humans and can be metabolised to erythronate to a small extent. Erythritol is then excreted unchanged in the urine. It does not raise concerns regarding genotoxicity. The dataset evaluated consisted of human interventional studies. The Panel considered that erythritol has the potential to cause diarrhoea in humans, which was considered adverse because its potential association with electrolyte and water imbalance. The lower bound of the range of no observed adverse effect levels (NOAELs) for diarrhoea of 0.5 g/kg body weight (bw) was identified as reference point. The Panel considered appropriate to set a numerical acceptable daily intake (ADI) at the level of the reference point. An ADI of 0.5 g/kg bw per day was considered by the Panel to be protective for the immediate laxative effect as well as potential chronic effects, secondary to diarrhoea. The highest mean and 95th percentile chronic exposure was in children (742 mg/kg bw per day) and adolescents (1532 mg/kg bw per day). Acute exposure was maximally 3531 mg/kg bw per meal for children at the 99th percentile. Overall, the Panel considered both dietary exposure assessments an overestimation. The Panel concluded that the exposure estimates for both acute and chronic dietary exposure to erythritol (E 968) were above the ADI, indicating that individuals with high intake may be at risk of experiencing adverse effects after single and repeated exposure. Concerning the new application, the Panel concluded that the available data do not support the proposal for exemption.
“…Some studies have revealed that xylitol is absorbed in the range of 49–95 % in the small intestine via passive diffusion and a slow absorption rate; however, xylitol was not found in plasma samples after two hours of ingestion. Xylitol can be excreted via the kidneys and fermented by beneficial bacteria [74] . On the other hand, citric acid can be absorbed in the gut or destroyed by bacteria and enzymes [75] .…”
Carvedilol is used to treat chronic hypertension, chronic stable angina pectoris and concomitant treatment heart failure and class II of the Biopharmaceutics Classification System (low solubility and poor bioavailability). This drug is only formulated as tablets, and liquid oral formulations are not available on the market. In this work, several aqueous eutectic mixtures formed by xylitol, citric acid, sorbitol and glucose (HBD) and choline chloride as HBA have been used to improve the solubility. Additionally, SwissADME was used to obtain physicochemical and pharmacokinetic parameters to further knowledge on the ADME (absorption, distribution, metabolism and excretion) parameters for carvedilol.The results reveal that the solubility of carvedilol increases as the content of water decreases, and the mixture formed by citric acid and choline chloride (CACh10) was the most soluble. The stability study shows that carvedilol in DES is stable during the test time, as the maximum and minimum concentration losses were 19.0 % and 0.2 %, respectively. These results help advance the green and sustainable development of new medicines in the liquid state.
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