Increasing the Oral Bioavailability of 6-prenylnaringenin by Micellar Solubilization
试验速览
- 阶段
- 不适用
- 状态
- 已完成
- 入组人数
- 6
- 试验地点
- 4
- 主要终点
- Mean area under the curve (AUC) of plasma concentration vs. time of total 6-PN [nmol/L*h]
研究概览
简要总结
Micellar encapsulation will be tested to increase the oral bioavailability in humans of 6-prenylnaringenin (6-PN) from hops (Humulus lupulus). The study follows a single dose (250 mg 6-PN), placebo controlled, randomized, double-blind, three armed crossover study design with ≥2-week washout periods. Plasma, urine and PBMC samples will be collected at intervals up to 24 h after intake of the native compound, the micellar formulation or placebo. The safety, pharmacokinetics and impact of oral prenylflavonoids on PBMC survival will be investigated.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Basic Science
- 盲法
- Double (Participant, Investigator)
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy volunteers with blood chemistry values within normal ranges
- •Age: 18-45 years
- •BMI: 19-25 kg/m2
排除标准
- •Pregnancy or lactation
- •Alcohol and/or drug abuse
- •Use of dietary supplements or any medications, except contraceptives
- •Any known malignant, metabolic and endocrine diseases
- •Previous cardiac infarction
- •Participation in a clinical trial within the past 6 weeks prior to recruitment
- •Physical activity of more than 5 h/wk
研究组 & 干预措施
Placebo
Mannitol and silicon dioxide
干预措施: Placebo (Dietary Supplement)
Native 6-prenylnaringenin
250 mg native 6-PN plus mannitol and silicon dioxide
干预措施: Native 6-prenylnaringenin (Dietary Supplement)
Micellar 6-prenylnaringenin
250 mg 6-PN in a micellar formulation with Tween-80 as adjuvant
干预措施: Micellar 6-prenylnaringenin (Dietary Supplement)
结局指标
主要结局
Mean area under the curve (AUC) of plasma concentration vs. time of total 6-PN [nmol/L*h]
时间窗: 0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Mean maximum plasma concentration (Cmax) of total 6-PN [nmol/L]
时间窗: 0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration
时间窗: 0 h, 6 h, and 24 h post dose
Time to reach maximum plasma concentration (Tmax) of total 6-PN [h]
时间窗: 0 h, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h and 24 h post dose
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
Cell viability of PBMCs after 6-PN administration
时间窗: 0 h, 6 h, and 24 h post dose
Cumulative urinary excretion of total 6-PN [nmol/g creatinine]
时间窗: 0 h - 24 h post dose
Total 6-PN determined after deconjugation with beta-glucuronidase/sulphatase
次要结局
- Serum HDL cholesterol [mg/dL](0 h, 4 h, 24h post-dose)
- Serum glucose [mg/dL](0 h, 4 h, 24h post-dose)
- Serum uric acid [mg/dL](0 h, 4 h, 24h post-dose)
- Serum alanine transaminase activity [U/L](0 h, 4 h, 24h post-dose)
- Serum aspartate transaminase activity [U/L](0 h, 4 h, 24h post-dose)
- Serum creatinine [mg/dL](0 h, 4 h, 24h post-dose)
- Serum gamma-glutamyl transferase activity [U/L](0 h, 4 h, 24h post-dose)
- Serum bilirubin(0 h, 4 h, 24h post-dose)
- Serum LDL cholesterol [mg/dL](0 h, 4 h, 24h post-dose)
- Serum total cholesterol [mg/dL](0 h, 4 h, 24h post-dose)
- LDL/HDL cholesterol ratio(0 h, 4 h, 24h post-dose)
- Mean corpuscular hemoglobin concentration [g/dL](0 h, 24 h post-dose)
- Hematocrit [%](0 h, 24 h post-dose)
- Erythrocytes [/pL](0 h, 24 h post-dose)
- Serum alkaline phosphatase activity [U/L](0 h, 4 h, 24h post-dose)
- Serum triacylglycerols [mg/dL](0 h, 4 h, 24h post-dose)
- Mean corpuscular hemoglobin [pg](0 h, 24 h post-dose)
- Leucocytes [/nL](0 h, 24 h post-dose)
- Glomerular filtration rate [mL/min](0 h, 4 h, 24h post-dose)
- Hemoglobin [g/dL](0 h, 24 h post-dose)
- Mean corpuscular volume [fL](0 h, 24 h post-dose)
- Thrombocytes [/nL](0 h, 24 h post-dose)