Frank Thomas, Stintzing Florian Conrad, Carle Reinhold, Bitsch Irmgard, Quaas Daniela, Strass Gabriele, Bitsch Roland, Netzel Michael
Solvay Pharmaceuticals GmbH, Hans-Boeckler-Allee 20, D-30173 Hannover, Germany.
Pharmacol Res. 2005 Oct;52(4):290-7. doi: 10.1016/j.phrs.2005.04.005.
The aim of the present pilot study was to characterise the renal elimination of betalains after consumption of red beet juice (RBJ). Six healthy, non-smoking female volunteers were given a single oral dose of either 500 mL of a commercial RBJ containing 362.7 mg of betalains and 500 mL of tap water, respectively, in a sequential manner. Urine was collected in intervals up to 24 h post-dose. Renal excretion of betalains was determined spectrophotometrically and quantified as betanin-equivalents. In addition, the identity of individual compounds was confirmed by HPLC coupled with diode-array detection and positive ion electrospray mass spectrometry, respectively. The amount (mean+/-S.D.) of intact betalains (betanin and isobetanin) recovered in urine was 1001+/-273 microg corresponding to 0.28+/-0.08% of the administered dose. Maximum excretion rates were observed after a median tmax,R of 3.0 h (range 2.5-8.0 h) amounting to 91.7+/-30.1 microg/h. The terminal elimination rate constant (lambdaz) and the corresponding half-life were 0.097+/-0.021 h(-1) and 7.43+/-1.47 h, respectively. Using the lambdaz estimates obtained the expected total betalain amount excreted in urine was 1228+/-291 microg. Based on the results obtained it is assumed that either the bioavailability of the betalains is low or that renal clearance is a minor route of systemic elimination for these compounds. The urinary excretion rates of unmetabolised betalains were fast and appeared to be monoexponential suggesting a one-compartment model. In order to get a more complete picture of the pharmacokinetics and health-promoting properties of red beet betalains, quantitative data on betalain bioavailability should include measurements of unchanged compounds and their corresponding metabolites in plasma, urine and bile.
本初步研究的目的是描述饮用红甜菜汁(RBJ)后甜菜红素的肾脏排泄情况。六名健康、不吸烟的女性志愿者,分别依次单次口服500 mL含有362.7 mg甜菜红素的市售RBJ和500 mL自来水。给药后间隔收集尿液直至24小时。采用分光光度法测定甜菜红素的肾脏排泄量,并以甜菜红苷当量进行定量。此外,分别通过高效液相色谱结合二极管阵列检测和正离子电喷雾质谱法确认各化合物的身份。尿液中回收的完整甜菜红素(甜菜红苷和异甜菜红苷)量(均值±标准差)为1001±273 μg,相当于给药剂量的0.28±0.08%。中位达峰时间tmax,R为3.0小时(范围2.5 - 8.0小时)后观察到最大排泄率,为91.7±30.1 μg/小时。终末消除速率常数(λz)和相应的半衰期分别为0.097±0.021 h-1和7.43±1.47小时。根据获得的λz估计值,尿液中预期排泄的总甜菜红素量为1228±291 μg。基于所得结果,推测要么甜菜红素的生物利用度较低,要么肾脏清除是这些化合物全身消除的次要途径。未代谢甜菜红素的尿排泄率较快,且似乎呈单指数形式,提示为单室模型。为了更全面地了解红甜菜甜菜红素的药代动力学和促进健康特性,甜菜红素生物利用度的定量数据应包括血浆、尿液和胆汁中未变化化合物及其相应代谢物的测量。