Evaluation of the Oral Bioavailability of a New Formulation of Pterostilbene Co-crystal in Comparison With Its Free Form in Healthy Volunteers: Crossover, Randomized and Simple Blind Study (BIOPTERO2)
试验速览
- 阶段
- 不适用
- 状态
- 已完成
- 发起方
- 入组人数
- 6
- 试验地点
- 2
- 主要终点
- Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels, both free and total.
研究概览
简要总结
The goal of this interventional study is to to evaluate the oral bioavailability of the crystallized form of pterostilbene (ccPT) compared to its commercial free base form (pterostilbene (PT) in healthy volunteers. The main question it aims to answer are:
• Do the crystallized forms of pterostilbene (ccPT) using two different encapsulation methods exhibit greater bioavailability than its commercial free base form (PT)?
Participants will attend to four visits: a preselection visit (V0), a visit for the first postprandial study (V1), a visit for the second postprandial study (V2) after one-week washing period and a visit for the third postprandial study (V3) after another one week washing period.
Researchers will analyze the three postprandial assays to determine which type of ccPT encapsulation provides the highest bioavailability compared to the commercial free base form (PT).
详细描述
The oxidative stress (OS) is a condition where pro-oxidative processes overwhelm cellular antioxidant defenses due to disruption in redox signaling. This results in the body's inability to eliminate reactive oxygen species (ROS) or repair damages, potentially leading to severe impacts on cells, tissues, and organs.
Pterostilbene (PT) is a stilbenoid found in various natural sources, emerging as an antioxidant with potential preventive and therapeutic properties in numerous diseases. Despite its promising properties, PT's low water solubility and bioavailability pose challenges.
Nutraceutical co-crystallization is a recent strategy to enhance solubility and oral bioavailability. It has been identified that a new pterostilbene:picolinic acid (1:1) co-crystal, significantly increasing solubility and oral bioavailability compared to commercial free base PT.
The study aims to evaluate oral bioavailability (AUC0-24h) of PT (free and total) from ccPT compared to commercial PT, using two different encapsulation methods. Secondary objectives include determining pharmacokinetic parameters such as AUCinf, relative oral bioavailability (Frel), Cmax, Tmax, and T1/2 for both free and total PT.
This randomized, crossover, single-blind clinical trial aims to provide insights into the effectiveness of the new ccPT formulation in enhancing PT's oral bioavailability compared to the commercial PT formulation.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Other
- 盲法
- Single (Outcomes Assessor)
入排标准
- 年龄范围
- 18 Years 至 65 Years（Adult, Older Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Men and women between 18 and 65 years of age.
- •Sign the informed consent form.
- •Know how to read, write and speak Spanish
排除标准
- •Take supplements or multivitamin supplements or phytotherapeutic products (especially infusions) that interfere with the treatment under study up to 30 days before the start of the study.
- •Be lacto-vegetarian, lacto-ovo-vegetarian, or vegan.
- •Present intolerances and/or food allergies related to pterostilbene or the excipients.
- •Be a smoker.
- •Having received antibiotic treatment up to 30 days before the start of the study.
- •Present values of body mass index ≤ 18kg/m^2 or ≥ 35 kg/m^
- •Present some chronic disease with clinical manifestations: coronary heart disease, cardiovascular disease, diabetes, celiac disease, Crohn's disease, chronic kidney disease, cancer, autoimmune diseases (such as fibromyalgia), respiratory and/or gastrointestinal diseases that may compromise the absorption of the compound.
- •Clinical history of anemia.
- •Being pregnant or intending to became pregnant.
- •Be in breastfeeding period.
- •Being unable to follow the study guidelines.
- •Participate in or have participated in a clinical trial or nutritional intervention study in the last 30 days before inclusion in the study.
结局指标
主要结局
Bioavailability of Pterostilbene calculated by area under the curve (AUC 0-24) of plasma pterostilbene levels, both free and total.
时间窗: At week 1, week 2 and week 3
Fasting pterostilbene levels in plasma will be determined by liquid chromatography coupled to mass spectrophotometry before consume the capsule with pterostilbene until 24 hours postprandially at 8 points after consuming the capsule (0.5 hours, 1 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours and 24 hours). Total PT will be quantified indirectly after hydrolysis of the conjugated glucuronide and sulfate metabolites to free PT in the presence of β-glucuronidase and arylsulfatase in the plasma samples.
次要结局
- Relative bioavailability of plasma pterostilbene levels (Frel).(At week 1, week 2 and week 3)
- Maximum plasma concentration (Cmax)(At week 1, week 2 and week 3)
- Time for maximum plasma concentration (Tmax)(At week 1, week 2 and week 3)
- Area under the curve (AUC 0-inf) of plasma pterostilbene levels, both free and total.(At week 1, week 2 and week 3)
- Half-life (T1/2).(At week 1, week 2 and week 3)