A Phase I, Randomized, Crossover, Double-blind, Pharmacokinetic Study of Berberine Released From Cyclodextrin in Healthy Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 尚未招募
- 发起方
- 入组人数
- 16
- 试验地点
- 5
- 主要终点
- The area under the plasma concentration versus time curve (AUC, expressed in ng x h/mL) of berberine incorporated in gamma-cyclodextrin
研究概览
简要总结
In this study, we will evaluate the relative bioavailability of Berberine (BB) from capsules containing Indian Barberry (Berberis aristate DC.) Bark and Root Extract in the blood plasma of healthy subjects after oral administration of:
A. Capsules containing Berberine and GCD (BBA Berberine MetX™ Ultra Absorption, 250 mg) B. Capsules containing Berberine (BB, Berberine MetX™, 500 mg) - (reference product).
详细描述
Study Background
A growing body of evidence suggests that gamma-cyclodextrin (GCD) can increase the clinical efficacy of water-insoluble biologically active compounds with low bioavailability. GCD is the most bio adaptable and helpful to increase the absorption of many drugs, including Berberine from Indian Barberry (Berberis aristate DC.) Bark and Root Extract by forming inclusion complexes or GCD/drug conjugates.
Berberine has been recommended in traditional practice and recognized by modern science to support healthy blood sugar†, cholesterol and triglyceride levels, and overall metabolic health. But despite these findings, standard Berberine can still be difficult for the body to absorb and use effectively.
It's estimated that only about five percent of any given dosage of Berberine makes it into the bloodstream, so finding a way to enhance absorption is key to the full advantage of its benefits.
Hypothesis: gamma-cyclodextrin increases absorption and bioavailability of Berberine from Berberine MetX™ Ultra Absorption capsules.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Treatment
- 盲法
- Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)
入排标准
- 年龄范围
- 18 Years 至 60 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy volunteers, as determined by medical history, physical examination, and clinical laboratory testing,
- •Willingness to stay in the unit overnight for the duration of the study,
- •Provide a signed written informed consent.
排除标准
- •overweight (BMI >35 kg/m2),
- •pregnancy,
- •lactation,
- •drug abuse,
- •use of dietary supplements or any form of medication (with the exception of oral contraceptives),
- •heavy smokers, or ex-smokers with a remote history (> one pack/day),
- •frequent alcohol consumption (>20 g ethanol/d),
- •adherence to a restrictive dietary regimen,
- •physical activity of more than 5 h/wk,
- •respiratory tract infections, or suspicion thereof in the last 14 days before dosing,
- •history or presence of disease in the kidneys and heart, lungs, liver, gastrointestinal tract, endocrine organs or other conditions such as metabolic disease known to interfere with the absorption, distribution, metabolism, and excretion of drugs,
- •malignancy,
- •autoimmune disorders such as (but not limited to) lupus erythematosus, multiple sclerosis, rheumatoid arthritis, or sarcoidosis,
- •any other disease or condition, which, in the opinion of the Investigator, would make the subject unsuitable for this study,
- •currently taking medications known to be CYP2C9 inducers (i.e., carbamazepine and rifampicin).
结局指标
主要结局
The area under the plasma concentration versus time curve (AUC, expressed in ng x h/mL) of berberine incorporated in gamma-cyclodextrin
时间窗: 0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72 and 96 hours, post-dose
The changes from the baseline the concentration (ng/ml) of berberine in blood plasma obtained after oral administration of the experimental product BBA.
The area under the plasma concentration versus time curve (AUC, expressed in ng x h/mL) of berberine
时间窗: 0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72 and 96 hours, post-dose
The changes from the baseline the concentration (ng/ml) of berberine in blood plasma obtained after oral administration of the active comparator BB.
次要结局
- The absorption rate constants (Ka, h-1) of berberine(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72 and 96 hours, post-dose)
- Maximum plasma concentration (Cmax, ng/ml) of Berberine incorporated in gamma-cyclodextrin(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72, and 96 hours, post-dose)
- Time to reach maximum plasma concentration, Tmax (h) of berberine incorporated in gamma-cyclodextrin(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72, and 96 hours, post-dose)
- Time to reach maximum plasma concentration, Tmax (h) of berberine(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72, and 96 hours, post-dose)
- Mean absorption time MAT (h) of berberine incorporated in gamma-cyclodextrin(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72, and 96 hours, post-dose)
- The absorption rate constants (Ka, h-1) of berberine incorporated in gamma-cyclodextrin(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72 and 96 hours, post-dose)
- Maximum plasma concentration (Cmax, ng/ml) of Berberine(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72, and 96 hours, post-dose)
- Mean absorption time MAT (h) of berberine(0.5, 0.75, 1, 2, 4, 6, 12, 24, 48, 72, and 96 hours, post-dose)