Pharmacokinetic study of Noni fruit extract.
Pharmacokinetic study of Noni fruit extract.
复制标题
诺丽果提取物的药代动力学研究。
DOI：
10.1080/19390210802519671
复制
发表时间：
2008
影响因子：
2.5
通讯作者：
Fielding,RobertM
中科院分区：
文献类型：
--
作者：
Issell,BrianF;Franke,Adrian;Fielding,RobertM
许多不同的产品含有诺丽（巴戟天大溪地）水果提取物销往世界各地的健康恢复和维护。尽管有一家大型企业推动了诺丽的普及，但产品缺乏标准化，也没有科学证据证明诺丽的临床疗效和安全性。也没有证据表明最佳治疗剂量或给药间隔。在最初的志愿者中，东莨菪碱被确定为诺丽暴露的生物活性标志物，也是产品标准化和药代动力学研究的候选者。随后，9名健康志愿者（每组3名）口服含诺丽全果冻干胶囊，剂量为1，500 mg（3 × 500 mg）、2，000 mg（4 × 500 mg）和2，500 mg（5 × 500 mg）。在给药前和给药后0.5、1、2、4和8 h采集每例受试者的血浆和尿液样本。东莨菪内酯的浓度通过具有PDA的HPLC（在200-700 nm下扫描）和MS检测来测定。东莨菪内酯在摄入诺丽后迅速进入血浆，在给药后至少8小时内维持在0.5至5 ng/mL的水平。东莨菪碱的生物利用度似乎较低，具有显著的受试者间变异性。我们的结论是东莨菪碱可以作为一个相对特定的标记诺丽暴露在血液中，特别是在尿液中，当其药代动力学被认为是适当的。
Many different products containing Noni (Morinda citrifolia) fruit extracts are sold throughout the world for health restoration and maintenance. Despite a large business enterprise fueling Noni's popularity, there is a lack of standardization of products and no scientific evidence of Noni's clinical efficacy and safety. There is also no evidence to indicate an optimal therapeutic dose or dosing interval. In an initial volunteer, scopoletin was identified as a bioactive marker of Noni exposure and a candidate for product standardization and pharmacokinetic studies. Subsequently, capsules containing the whole freeze-dried fruit of Noni were orally administered to nine healthy volunteers (3 per group) at doses of 1,500 mg (3 × 500 mg), 2,000 mg (4 × 500 mg) and 2,500 mg (5 × 500 mg). Plasma and urine samples were obtained from each subject prior to dosing and at 0.5, 1, 2, 4 and 8 h after dosing. Concentrations of scopoletin were determined by HPLC with PDA (scanning at 200–700 nm) and MS detection. Scopoletin rapidly enters the plasma after Noni ingestion, maintaining levels in the range of 0.5 to 5 ng/mL for at least 8 h after dosing. Scopoletin bioavailability appears to be low, with significant intersubject variability. We conclude that scopoletin can be used as a relatively specific marker of Noni exposure in the blood and particularly in urine when its pharmacokinetics is considered appropriately.