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Examination of the Pharmacokinetics of Active Ingredients of Ginger in Humans

机译:生姜有效成分在人体中的药代动力学检查

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摘要

Ginger extracts have been studied in various clinical trials for different indications. However, the pharmacokinetics of the ginger active constituents in human biological matrices is not well investigated. This study aims to develop a LC-MS/MS method for simultaneous measurement of 6-, 8-, and 10-gingerols and 6-shogaol and study their pharmacokinetics in human plasma and colon tissues. A sensitive LC-MS/MS method was established and validated with a low limit of quantification of 2–5 ng/mL. The intra- and inter-day accuracy ranged from −7.3% to 10.4% and from −9.4% to 9.8%, respectively. The intra- and inter-day precision ranged from 0.9% to 10.9% and from 2.0% to 12.4%, respectively. The glucuronide and sulfate metabolites of 6-, 8-, and 10-gingerols and 6-shogaol in plasma and colon tissues were quantified after hydrolysis with β-glucuronidase and sulfatase. After oral dosing of 2.0 g ginger extracts in human, free 10-gingerol and 6-shogaol were detected in plasma with peak concentrations (9.5 ± 2.2 and 13.6 ± 6.9 ng/mL, respectively) at 1 h after oral administration, but no free 6-gingerol and 8-gingerol were detected in plasma from 0.25 to 24 h. The peak concentrations of glucuronide metabolites of 6-, 8-, and 10-gingerols and 6-shogaol were 0.47 ± 0.31, 0.17 ± 0.14, 0.37 ± 0.19, and 0.73 ± 0.54 μg/mL at 1 h, respectively. The peak concentrations of the sulfate metabolites of 6-, 8-, and 10-gingerols and 6-shogaol were 0.28 ± 0.15, 0.027 ± 0.018, 0.018 ± 0.006, and 0.047 ± 0.035 μg/mL at 1 h, respectively. Very low concentrations (2–3 ng/mL) of 10-gingerol glucuronide and sulfate were found in colon tissues. Pharmacokinetic analysis showed that half-lives of these four analytes and their metabolites were 1–3 h in human plasma. No accumulation was observed for 6-, 8-, and 10-gingerols and 6-shogaol and their metabolites in both plasma and colon tissues after multiple daily dosing.
机译:生姜提取物已在各种临床试验中针对不同的适应症进行了研究。然而,姜生物活性成分在人体生物基质中的药代动力学尚未得到很好的研究。这项研究的目的是开发一种同时测量6、8和10姜油酚和6寿果酚的LC-MS / MS方法,并研究它们在人血浆和结肠组织中的药代动力学。建立了灵敏的LC-MS / MS方法并以2-5 ng / mL的低定量下限进行了验证。日内和日间准确度分别为-7.3%至10.4%和-9.4%至9.8%。日内和日间精度分别为0.9%至10.9%和2.0%至12.4%。用β-葡萄糖醛酸苷酶和硫酸酯酶水解后,定量测定血浆和结肠组织中6-,8-和10-姜醇和6-shogaol的葡萄糖醛酸和硫酸盐代谢产物。口服2.0 g生姜提取物后,口服1小时后血浆中检出游离10-姜油和6-shogaol的峰值浓度(分别为9.5±2.2和13.6±6.9ng / mL),但没有游离在0.25至24小时内的血浆中检测到6-甘油和8-甘油。 6-,8-和10-甘油的葡萄糖醛酸苷代谢产物和6-shogaol的峰值浓度在1h分别为0.47±0.31、0.17±0.14、0.37±0.19和0.73±0.54μg/ mL。 6-,8-和10-姜醇和6-shogaol的硫酸盐代谢产物的峰值浓度在1 h分别为0.28±0.15、0.027±0.018、0.018±0.006和0.047±0.035μg/ mL。在结肠组织中发现了非常低的浓度(2–3 ng / mL)的10-姜油葡糖醛酸和硫酸盐。药代动力学分析表明,这四种分析物及其代谢产物的半衰期在人血浆中为1-3h。每天多次给药后,在血浆和结肠组织中均未观察到6-,8-和10-姜醇和6-shogaol及其代谢产物的蓄积。

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