To Test the Efficacy of Novel Berberine Emulsification by TPGS or Quillaja Extract on the Absorption of Berberine Compared to Berberine Powder in Humans
试验速览
- 阶段
- 不适用
- 状态
- 已完成
- 入组人数
- 32
- 试验地点
- 2
- 主要终点
- AUC:the area under the concentration-time curve
研究概览
简要总结
Berberine from medicinal plants has therapeutic activities against multiple chronic diseases. But its absorption rate is very low. The objective of this study is to test if adding TPGS or Quillaja extract as an emulsifier enhance the absorption of berberine in human.
详细描述
Berberine is widely used as an herbal medicine and many health benefits. These well-documented in the literature including lowering blood lipids and glucose, having anti-inflammatory and anti-tumor activity, preventing and delaying neurodegenerative diseases (Alzheimer, Parkinson and Huntington disease) and preventing obesity. However, the absorption rate of berberine is very low. The study team believes adding TPGS or Quillaja extract as an emulsifier enhance the absorption of berberine in human.
The bioavailability of berberine is extremely low. Only 0.5% of orally ingested berberine are absorbed in small intestine and about 0.36% can enter the systemic circulation. About 56% of ingested berberine was not absorbed and additional 43.5% is lost due to metabolism in small intestine.
Vitamin E TPGS (a water-soluble form of vitamin E) is a food additive approved by FDA. It has the potential to increase the absorption of drugs and dietary supplements. TPGS is an effective inhibitor of P-glycoproteins that are responsible for decreased absorption rate of many drugs including berberine. TPGS has the potential be a safe and effective adsorption enhancer for berberine and other bioactive botanicals.
Quillaja extract is a natural GRAS (generally recognized as safe) food-grade surfactant/emulsifier ingredient rich in saponins and sapogenins. It is purified from the Quillaja Saponaria Molina tree which is native to Chile. Quillaja extract is an approved ingredient for use in Food and Beverages by FDA under Title 21 CFR 172.51. It is an approved food additive in the European Union under code E 999. Quillaja extract is an attractive alternative emulsifier for berberine formulation because it meets consumers' demand for natural ingredient. Quillaja extract provides additional benefits of anti-inflammation and cholesterol lowering to dietary supplement. Some early study before 2000 suggested that Quillaja saponin DS-1 promote the absorption of insulin and aminoglycoside antibiotics via the ocular and nasal route by reducing permeability of epithelial barrier. However, it is not known whether quillaja affect absorption of berberine in vivo or in human.
Specific Aims:
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
- Single (Participant)
入排标准
- 年龄范围
- 21 Years 至 50 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Normal BMI (20-27)
排除标准
- •Pregnancy
- •Gastro-intestinal conditions
- •Diabetics,
- •Alcohol and substance abuse history,
- •Allergy to berberine,
- •Current berberine use,
- •Use of H2 blockers, proton pump inhibitors, blood sugar-lowering agents, or statins
结局指标
主要结局
AUC:the area under the concentration-time curve
时间窗: Pre-dose, Hour 0.5, Hour 1, Hour 2, Hour 3, Hour 4, Hour 6, Hour 8 and Hour 12
To determine change in bioavailability of orally ingested berberine in human volunteers by increasing the area under the concentration-time curve (AUC).
Cmax: maximum plasma concentration
时间窗: Pre-dose, Hour 0.5, Hour 1, Hour 2, Hour 3, Hour 4, Hour 6, Hour 8 and Hour 12
To determine change in bioavailability of orally ingested berberine in human volunteers by increasing its plasma concentration peak concentration (Cmax).
Tmax: the time point of maximum plasma concentration
时间窗: Pre-dose, Hour 0.5, Hour 1, Hour 2, Hour 3, Hour 4, Hour 6, Hour 8 and Hour 12
To determine change in bioavailability of orally ingested berberine in human volunteers by increasing its the time point of maximum plasma concentration (Tmax).
次要结局
- Changes in concentrations of berberine metabolites.(Pre-dose, Hour 0.5, Hour 1, Hour 2, Hour 3, Hour 4, Hour 6, Hour 8 and Hour 12)