评价药物动力学和生物利用度更高的剂量Tocotrienols美联储人类健康。
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库雷希AA,汗哒,Silswal N,萨利姆年代,库雷希N
评价药物动力学和生物利用度更高的剂量Tocotrienols美联储人类健康。
中国Exp Cardiolog。2016年4月,7 (4)。doi: 10.4172 / 2155 - 9880.1000434。Epub 2016年4月28日。
- PubMed ID
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27493840 (在PubMed]
- 文摘
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背景:Tocotrienols已经知道低血清脂质参数低于500毫克/天,而增加脂质参数的高剂量750毫克/天。delta-Tocotrienol有小说浓度抑制和激活的炎症性质。因此,抑制(消炎)财产的tocotrienols低剂量对心血管疾病很有用,然而,激活(炎性)财产使用高剂量找到有效治疗各种癌症。我们最近描述等离子体生物利用度的125 mg / d, 250 mg / d和500毫克/天的剂量delta-tocotrienol美联储在健康主题,显示剂量依赖性增加曲线下的面积(AUC)和最大浓度(Cmax)。因此,在当前的研究中,高剂量的tocotrienols用于分析其影响血浆药代动力学参数。目的:评估的安全性和生物利用度更高的剂量(750毫克和1000毫克)annatto-based tocotrienols健康主题。所有四个同分异构体(α、β、γ、δ-)的母育酚(tocotrienols和天然维生素e)出现在等离子体的主题进行了量化和分析各种药代动力学参数。研究设计:一个非盲、随机研究进行分析的药物动力学和生物利用度delta-tocotrienol美联储在6健康的主题。所有科目(3 /剂量)被随机分配到每个剂量750毫克和1000毫克。收集血液样本(0,1,2,4,6,8 h间隔和同分异构体的α,β,γ- delta-tocotrienols,天然维生素e在等离子体被高效液相色谱量化。 RESULTS: Oral administration of 750 and 1000 mg/d of tocotrienols resulted in dose-dependent increases in plasmas (ng/ml) AUCt0-t8 6621, 7450; AUCt0-infinity 8688, 9633; AUMC t0-infinity 52497, 57199; MRT 6.04, 5.93; Cmax 1444, 1592 (P<0.05), respectively, of delta-tocotrienol isomer. Moreover, both doses also resulted in plasmas Tmax 3.33-4 h; elimination half-life (t1/2 h) 2.74, 2.68; time of clearance (Cl-T, l/h) 0.086, 0.078; volume of distribution (Vd/f, mg/h) 0.34, 0.30; and elimination rate constant (ke; h(-1)) 0.25, 0.17, respectively of delta- tocotrienol isomer. Similar results of these parameters were reported for gamma-tocotrienol, beta- tocotrienol, alpha-tocotrienol, delta-tocopherol, gamma-tocopherol, and beta-tocopherol, except for alpha- tocopherol. CONCLUSIONS: This study has described pharmacokinetics using higher doses of 750 mg/d and 1000 mg/d of delta-tocotrienol. These results confirmed earlier findings that Tmax was 3-4 h for all isomers of tocotrienols and tocopherols except for alpha-tocopherol (6 h). These higher doses of tocotrienols were found safe in humans and may be useful for treatments of various types of cancer, diabetes, and Alzheimer's disease.
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- 药物