Pharmacokinetic Study of Palmitoylethanolamide (PEA) Extract Formulations in Healthy Human Volunteers
试验速览
- 阶段
- 不适用
- 状态
- 已完成
- 发起方
- Tilman SA
- 入组人数
- 96
- 试验地点
- 2
- 主要终点
- Plasma pharmacokinetic parameters
研究概览
简要总结
PEA is an endocannabinoid-like lipid mediator with well-documented anti-inflammatory, analgesic, antimicrobial, immunomodulatory and neuroprotective effects. It is safe and well tolerated in animals and humans, offering therapeutic benefits in various conditions, including chronic pain, psychopathologies, and neurodegeneration. However, the endogenous levels of PEA may be insufficient in chronic inflammatory disorders, necessitating exogenous administration for therapeutic purposes PEA is a compound with poor solubility and poor bioavailability. Different formulations have been developed to increase the dispersion of PEA in water solution with the goal to increase the bioavailability while maintaining essential technical parameters such as bulk density and flowability. The goal of this study is to compare the bioavailability of different formulations containing PEA.
Conducting a pharmacokinetic study on PEA is crucial for optimizing its therapeutic use by understanding its absorption, distribution, metabolism, and excretion. This study provides essential information on bioavailability, dosage determination, administration frequency, duration of action, tissue distribution, metabolism, and safety. Knowledge of metabolic pathways and elimination routes helps identify potential drug interactions, ensuring safe elimination without toxicity or accumulation.
Establishing a correlation between pharmacokinetic parameters and pharmacodynamic effects is also vital for optimizing therapeutic outcomes. Additionally, pharmacokinetic data informs the development of formulations, to maintain consistent plasma concentrations over time. Investigation of PEA’s pharmacokinetic profile will also contribute to understanding its safety and tolerability, including potential drug interactions and adverse effects. In pharmacokinetic studies, healthy human trial participants are preferred to assess the active ingredient’s behavior accurately. Including both males and females is crucial to identify potential gender-based differences in absorption, distribution, metabolism, and excretion. This research aims to explore the pharmacokinetic profile of PEA extract in healthy human volunteers following acute oral administration under fasting conditions.
研究设计
- 研究类型
- Interventional
- 分配方式
- Computer generated randomization
- 盲法
- Open Label
入排标准
- 年龄范围
- 18.00 Year(s) 至 55.00 Year(s)（—）
- 性别
- All
入选标准
- •1.Healthy male and female human trial participants aged between 18 and 55 years(both inclusive) 2.Female trial participants must have a negative urine pregnancy test prior to the housing 3.Male and females agreeing to use the contraceptive pill or abstinence as a method of contraception during and 07 days after completion of the study 4.Trial participants with a BMI between 18.50-28.00 kgperm2 and body mass not less than 50.00 kg 5.Trial participants in normal health as determined by personal medical history, clinical examination including vital signs, and clinically acceptable results of laboratory examinations (including serological tests); 6.Trial participants having a normal or clinically not significant 12-lead electrocardiogram (ECG) recording 7.Trial participants having a normal or clinically not significant chest X-ray (PA view); 8.A negative alcohol breath test result before housing 9.Trial participant able to communicate effectively and provide written informed consent 10.Trial participants willing to adhere to the protocol requirements as evidenced by written informed consent approved by the ethics committee; 11.Trial participants that can provide adequate evidence of their identity 12.Availability of volunteers for the entire study duration 13.Ability to fast for at least 14.00 hours and consume standard meals.
排除标准
- •1.Known hypersensitivity to PEA or related product or any component of any interventions; 2.Incapable of understanding the informed consent information; 3.Clinically significant medical condition, such as, but not limited to, cardiovascular neurological, psychiatric, pulmonary, renal, immunological, endocrine (including uncontrolled diabetes or thyroid disease), or uncontrolled haematological abnormalities; 4.Any treatment which could bring about induction or inhibition of the hepatic microsomal enzyme system within one month of starting the study; 5.History or presence of alcoholism or drug abuse; 6.History or presence of asthma, urticaria, or other allergic reactions; 7.History or presence of gastric and/or duodenal ulceration; 8.History or presence of thyroid disease, adrenal dysfunction, or organic intracranial lesion; 9.History or presence of cancer; 10.Difficulty with donating blood; 11.Use of any prescribed medication (including herbal remedies) during the two weeks before the start of the study or OTC medicinal products (including herbal remedies) during the week before study initiation and throughout the study; 12.Use of medications such as benzodiazepines, anticonvulsants, or barbiturates for one month before the start of the study and throughout the study; 13.Smokers who smoke 9 or more cigarettes/day or inability to abstain during the study; 14.Trial participant consumed tobacco/tobacco-containing products, pan or pan masala, gutkha, and masala (containing beetle nut and tobacco) for at least 48.00 hours before initiation of the study and throughout the study; 15.Trial participant consumed caffeine and/or xanthine-containing foods or beverages (i.e., coffee, tea, chocolate, and caffeine-containing sodas, colas, etc.) and grapefruit juice and poppy-containing foods for at least 48.00 hours before initiation of the study and throughout the study; 16.Major illness during the 90 days before screening; 17.Participation in a drug research study within 90 days of screening; 18.Donation of blood within 90 days of screening;
- •Positive screening test result for any one or more of the following: HIV, Hepatitis B, Hepatitis C, and VDRL; 20.History or presence of easy bruising or bleeding; 21.Abnormal diet pattern for whatever reason (e.g., low sodium, fasting, and high protein diets) during the four weeks preceding the study; 22.Pregnant women and nursing mothers; 23.Male and females of childbearing potential unwilling to employ appropriate and reliable method of contraception during the study till 07 days after the completion of the study; 24.Male volunteers willing to donate sperm during the study till 07 days after the completion of the study.
- •25.Consumption of dietary supplements likely to provide constituents similar to the investigational product in last 3 days.
结局指标
主要结局
Plasma pharmacokinetic parameters
时间窗: TimePoints: | Predose: 45 min Before IP administration | Postdose: | 1)At 30 min After IP administration | 2)At 45 min After IP administration | 3)At 70 min After IP administration | 4)At 90 min After IP administration | 5)At 120 min After IP administration | 6)At 180 min After IP administration | 7)At 240 min After IP administration
次要结局
- 1.Screening, pre-dose, and post-dose vital signs.(2.Clinical examination, ECG, chest X-ray, clinical laboratory testing(hematology, blood chemistry, liver function test (LFT), kidney function test(KFT), and other enzyme tests and urinalysis).)