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罗汉果醇是七种罗汉果皂苷和赛门苷I的苷元,因其具有抗白血病和糖尿病的活性,日益受到关注。本文采用超高效液相色谱-四极杆飞行时间质谱(UHPLC-Q-TOF/MS)法鉴定了大鼠灌胃给予100 mg·kg~(-1)罗汉果醇后血浆主要代谢产物,并建立液相色谱-串联质谱(LC-MS/MS)法测定血浆中主要成分浓度,以评价其药代动力学。大鼠灌胃给予罗汉果醇后,血浆以原形药物为主,检测到13种代谢产物,主要为单氧化和脱氢代谢产物。定量分析时,为提高灵敏度,采用锂加合离子作为前体离子。测定大鼠血浆中罗汉果醇线性范围为5.00~1 000 ng·m L~(-1)。质控样品的日内、日间精密度(RSD)小于9.3%,准确度(RE)在-4.5%~2.9%之间。大鼠灌胃给予罗汉果醇后,吸收迅速,达峰时间大约为1.67 h,血浆清除半衰期约2.34 h,绝对生物利用度仅为3.5%。
Mangosteen is an aglycone of seven kinds of mogroside and saegtin I, and attracts more and more attention because of its anti-leukemia and diabetic activity. In this paper, the main metabolites of rat plasma after oral administration of 100 mg · kg -1 Luo Hanuo alcohol were identified by UHPLC-Q-TOF / MS and established Liquid chromatography-tandem mass spectrometry (LC-MS / MS) was used to determine the concentration of major components in plasma to evaluate its pharmacokinetics. After gavage of mogrosides in rats, the plasma mainly consisted of prototype drugs, and 13 kinds of metabolites were detected, mainly mono-oxidation and dehydrogenation metabolites. For quantitative analysis, lithium adduct ions are used as precursor ions for increased sensitivity. The linear range of loganin in rat plasma was 5.00 ~ 1 000 ng · m L -1. The quality control samples had a day-to-day precision of less than 9.3% and a precision (RE) of -4.5% -2.9%. After oral administration of Luo Hanuo alcohol, the rats rapidly absorbed peak time of 1.67 h and plasma clearance half-life of 2.34 h with an absolute bioavailability of only 3.5%.