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A Comparative Pharmacokinetic Study to Evaluate the Ability of a New Formulation to Enhance Curcuminoids Bioavailability

Not Applicable
Completed
Conditions
Healthy
Interventions
Dietary Supplement: TG
Dietary Supplement: STE
Dietary Supplement: NOV
Dietary Supplement: PHYT
Dietary Supplement: TEP
Registration Number
NCT03621865
Lead Sponsor
Givaudan France Naturals
Brief Summary

The rhizome of Curcuma longa (turmeric) is commonly used as a spice and for its medicinal properties traditionally in Asian countries. Turmeric extract usually contains 95% curcuminoids with a specific ratio (approximately 75-80% curcumin, 15-20% demethoxycurcumin (DMC), and 0-10% bisdemethoxycurcumin (BDMC)).

Curcuminoids have higher solubility in organic solvents than in water. As a consequence, curcuminoids have low aqueous solubility and poor gastrointestinal absorption. They also exhibit rapid metabolism and systemic elimination and are therefore known to have limited bioavailability, which limits the use of turmeric extract in general health care and as an adjunct in managing various diseases. In order to improve the bioavailability of curcumin, several approaches have been undertaken. The use of adjuvant like piperine that interferes with glucuronidation; liposomal curcumin, nanoparticles, phospholipid complex; and structural analogues of curcumin.

Recently, Naturex has developed a dried emulsion formulation using a turmeric extract mixed together with a quillaja extract, sunflower oil and arabic gum. This formulation is highly dispersible in water and should therefore improve the bioavailability of curcuminoids. The aim of this study is to assess the bioavailability of curcuminoids and their metabolites after oral intake of 4 turmeric extract-based formulations in comparison to a standard unformulated turmeric extract.

Detailed Description

The rhizome of Curcuma longa (turmeric) is commonly used as a spice and for its medicinal proprieties traditionally in Asian countries. Turmeric has been studying in different therapeutic areas. Antioxidant, anti-inflammatory (respiratory system, joints and digestive), antimutagenic, antimicrobial, neurological disease, hepatoprotective and anticancer properties are supported by in vitro and in vivo data.

Curcumin has been studied as the main bioactive component of turmeric associated to its potential health effect. However, besides curcumin, others components have been identified (demethoxycurcumin DMC and bisdemethoxycurcumin BDMC); this group of coumpounds are named together "curcuminoids". Curcuminoids are natural yellow-orange pigments and hydrophobic polyphenols derived from the rhizome of the herb Curcuma longa. They are commonly isolated from the spice and food-coloring agent turmeric. Extracts of turmeric generally contain 75-80% curcumin, 15-20% DMC, and 0-10% BDMC. Regarding the intrinsic property, curcuminoids have higher solubility in organic solvents than in water. As a consequence, curcuminoids have low aqueous solubility and poor gastrointestinal absorption. They also exhibit rapid metabolism and systemic elimination.

This leads to the conclusion that curcuminoids from turmeric extract have low bioavailability, which limits its use in general health care and as an adjunct in managing various diseases. In order to improve the bioavailability of curcumin, several approaches have been undertaken. The use of adjuvant like piperine that interferes with glucuronidation; liposomal curcumin, nanoparticles, phospholipid complex; and structural analogues of curcumin.

Recently, Naturex has developed a dried emulsion formulation using a turmeric extract mixed together with a quillaja extract, sunflower oil and arabic gum. This formulation is highly dispersible in water and should therefore improve the bioavailability of curcuminoids. The aim of this study is to assess the bioavailability of curcuminoids and their metabolites after oral intake of 4 turmeric extract-based formulations in comparison to a standard unformulated turmeric extract.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
30
Inclusion Criteria
  • Age between 18 and 45 years (limits included),
  • BMI between 19 and 25 kg/m² (limits included),
  • Weight stable within ±3kg in the last three months,
  • With routine blood chemistry values within the normal range
  • For women: Non menopausal with the same reliable contraception since at least 3 cycles before the beginning of the study and agreeing to keep it during the entire duration of the study (condom with spermicidal gel and estrogen/progestin combination contraception accepted) or menopausal without or with hormone replacement therapy (estrogenic replacement therapy begun from less than 3 months excluded),
  • Non smoking or with tobacco consumption ≤ 5 cigarettes / day and agreeing not to smoke during all experimental sessions (V1 to V5),
  • Agreeing not to consume food, drink and condiment containing curcumin, turmeric (curcuma longa Linn.) or curry for 1 week prior to and throughout the entire study,
  • Good general and mental health with in the opinion of the investigator: no clinically significant and relevant abnormalities of medical history or physical examination,
  • Able and willing to participate to the study by complying with the protocol procedures as evidenced by his dated and signed informed consent form,
  • Affiliated with a social security scheme,
  • Agreeing to be registered on the volunteers in biomedical research file
Exclusion Criteria
  • Suffering from a metabolic or endocrine disorder such as diabetes, uncontrolled or controlled thyroidal trouble or other metabolic disorder,
  • Suffering from a severe chronic disease (e.g. cancer, HIV, renal failure, ongoing hepatic or biliary disorders, chronic inflammatory digestive disease, arthritis or other chronic respiratory trouble, etc.) or gastrointestinal disorders found to be inconsistent with the conduct of the study by the investigator (e.g. celiac disease),
  • Suffering from liver diseases
  • Current disease states that are contraindicated to subjects with dietary supplementation: chronic diarrhea, constipation or abdominal pain, Inflammatory bowel diseases (Crohn's disease or ulcerative colitis), Cirrhosis, chronic laxatives use...,
  • Suffering from Irritable Bowel Syndrome (IBS) diagnosed by a medical doctor and treated with chronic medication,
  • Having medical history of current pathology which could affect the study results or expose the subject to an additional risk according to the investigator,
  • Recent gastroenteritis or food borne illness such as confirmed food poisoning (less than 1 month),
  • Who made a blood donation in the 3 months before the V0 visit or intending to make it within 3 months ahead,
  • With a low venous capital not allowing to perform kinetic of blood samples according to the investigator's opinion,
  • With a known or suspected food allergy or intolerance or hypersensitivity to any of the study products' ingredient and/or of the standard meals (gluten intolerance, celiac disease, etc....)
  • Pregnant or lactating women or intending to become pregnant within 3 months ahead,
  • Exhibiting alcohol or drug dependence
  • On any chronic drug treatment (for example anticoagulant, antihypertensive treatment, treatment thyroid, asthma treatment, anxiolytic, antidepressant, lipid-lowering treatment, corticosteroids, phlebotonic, veino-tonic, drug with impact on blood circulation ...) excepting oral and local contraceptives,
  • Currently taking (and during the past 3 months) any supplementation from botanical origins
  • Having consumed curcumin-containing food supplements (curcumin, turmeric and curry) or foods (curcumin, turmeric, E100, and curry) defined as at least 3 times per week and for 2 weeks prior to testing
  • Currently taking (and during the past 3 months) any prebiotics or probiotics supplementation from food or from dietary supplements
  • With significant change in food habits or in physical activity in the 3 months before the V0 visit or not agreeing to keep them unchanged throughout the study,
  • Trying to lose weight with a current or planned in the next 3 months specific diet (hyper or hypocaloric, vegan, vegetarian...) or exercice regimen
  • With a personal history of anorexia nervosa, bulimia or significant eating disorders according to the investigator,
  • Consuming more than 3 standard drinks of alcoholic beverage daily for men or 2 daily for women or not agreeing to keep his alcohol consumption habits unchanged throughout the study,
  • Having a lifestyle deemed incompatible with the study according to the investigator including high level physical activity (defined as more than 10 hours of significant physical activity a week, walking excluded),
  • Taking part in another clinical trial or being in the exclusion period of a previous clinical trial,
  • Having received, during the last 12 months, indemnities for clinical trial higher or equal to 4500 Euros,
  • Under legal protection (guardianship, wardship) or deprived from his rights following administrative or judicial decision,
  • Presenting a psychological or linguistic incapability to sign the informed consent,
  • Impossible to contact in case of emergency.

After V0 biological analyses the subject will be considered as non-eligible to the study on the following criteria:

  • Control record (Glycaemia, GGT, ASAT, ALAT, Urea, Creatinine and Complete blood count) with clinically significant abnormality according to the investigator

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
subject sequence 2NOVsubject allocation sequence 2. IIntervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 3TEPsubject allocation sequence 3. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 4TEPsubject allocation sequence 4. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 5TEPsubject allocation sequence 5. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 6TGsubject allocation sequence 6. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 6PHYTsubject allocation sequence 6. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 1TGsubject allocation sequence 1. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 1NOVsubject allocation sequence 1. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 1PHYTsubject allocation sequence 1. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 2TGsubject allocation sequence 2. IIntervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 1STEsubject allocation sequence 1. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 2TEPsubject allocation sequence 2. IIntervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 4PHYTsubject allocation sequence 4. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 5NOVsubject allocation sequence 5. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 8NOVsubject allocation sequence 8. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 8PHYTsubject allocation sequence 8. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 8TEPsubject allocation sequence 8. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 6TEPsubject allocation sequence 6. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 1TEPsubject allocation sequence 1. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 3PHYTsubject allocation sequence 3. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 2STEsubject allocation sequence 2. IIntervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 2PHYTsubject allocation sequence 2. IIntervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 3TGsubject allocation sequence 3. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 4TGsubject allocation sequence 4. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 5PHYTsubject allocation sequence 5. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 6STEsubject allocation sequence 6. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 9PHYTsubject allocation sequence 9. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 7STEsubject allocation sequence 7. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 3STEsubject allocation sequence 3. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 3NOVsubject allocation sequence 3. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 4STEsubject allocation sequence 4. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 5TGsubject allocation sequence 5. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 5STEsubject allocation sequence 5. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 7TEPsubject allocation sequence 7. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 9STEsubject allocation sequence 9. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 10PHYTsubject allocation sequence 10. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 4NOVsubject allocation sequence 4. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 6NOVsubject allocation sequence 6. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 7TGsubject allocation sequence 7. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 7NOVsubject allocation sequence 7. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 8TGsubject allocation sequence 8. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 8STEsubject allocation sequence 8. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 9TEPsubject allocation sequence 9. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 10TGsubject allocation sequence 10. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 7PHYTsubject allocation sequence 7. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 9NOVsubject allocation sequence 9. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 10STEsubject allocation sequence 10. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 9TGsubject allocation sequence 9. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 10NOVsubject allocation sequence 10. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
subject sequence 10TEPsubject allocation sequence 10. Intervention: The subject will receive the five products (TG, STE, NOV, PHYT or TEP) in a certain order.
Primary Outcome Measures
NameTimeMethod
Dose-normalized AUC of total curcuminoids plasmatic concentrationfrom 0 to 24 hours

The primary endpoint is the dose-normalized AUC of total curcuminoids (sum of curcumin, DMC, BDMC and their metabolites) plasmatic concentration from 0 to 24 hours (AUC0-24h/dose) (expressed in µg.h/mL/mg). The dose-normalized AUC is the AUC normalized to curcuminoids intake by dividing the observed AUC by the corresponding curcuminoids dosage of each administration The following time-points are considered: T0, T15, T30, T45, T60, T90, T120, T240, T60, T480, T24H. T-10 will be considered as baseline value (T0) for AUC calculation. The primary comparison is Turmipure Gold 300 mg vs Standard turmeric 1500 mg powder extract.

Secondary Outcome Measures
NameTimeMethod
AUC of total curcuminoids plasmatic concentrationfrom 0 to infinity

AUC of total curcuminoids plasmatic concentration from 0 to infinity (AUC0-infinity, expressed in µg.h/mL);

Time to peak of total curcuminoids plasmatic concentrations24hours

Time to peak of total curcuminoids plasmatic concentration in plasma (Tmax, expressed in minutes)

Time to peak of curcuminoids separately (curcumin, DMC, BDMC) plasmatic concentrations24hours

Time to peak of plasmatic concentrations curcuminoids separately (curcumin, DMC, BDMC) in plasma (Tmax, expressed in minutes);

Time to peak of curcuminoids metabolites plasmatic concentrations24hours

Time to peak of plasmatic concentrations curcuminoids metabolites in plasma (Tmax, expressed in minutes);

AUC of curcuminoids separately (curcumin, DMC, BDMC) plasmatic concentrationsfrom 0 to infinity

AUC of curcuminoids separately (curcumin, DMC, BDMC) plasmatic concentrations from 0 to infinity (AUC0-infinity, expressed in µg.h/mL);

AUC of curcuminoids metabolites plasmatic concentrationsfrom 0 to infinity

AUC of curcuminoidsmetabolites plasmatic concentrations from 0 to infinity (AUC0-infinity, expressed in µg.h/mL);

AUC of total curcuminoids plasmatic concentration normalized to curcuminoids intakefrom 0 to infinity

AUC of total curcuminoids plasmatic concentration from 0 to infinity normalized to curcuminoids intake (AUC0-infinity/dose, expressed in µg.h/mL/mg);

Peak of total curcuminoids plasmatic concentration normalized to curcuminoids intake24hours

Peak of total curcuminoids plasmatic concentration normalized to curcuminoids intake (Cmax/dose, expressed in µg/mL/mg);

Peak of total curcuminoids plasmatic concentration24hours

Peak of total curcuminoids plasmatic concentration (Cmax, expressed in µg/mL);

Peak of curcuminoids separately plasmatic concentrations24hours

Peak of curcuminoids separately plasmatic concentrations (Cmax, expressed in µg/mL);

Peak of curcuminoids metabolites plasmatic concentrations24hours

Peak of curcuminoids metabolites plasmatic concentrations (Cmax, expressed in µg/mL);

Half-life of total curcuminoids in plasma24hours

Half-life of total curcuminoids in plasma (t1/2, expressed in minutes);

Half-life of curcuminoids separately (curcumin, DMC, BDMC) in plasma24hours

Half-life of curcuminoids separately (curcumin, DMC, BDMC) in plasma (t1/2, expressed in minutes);

Half-life of curcuminoids metabolites in plasma24hours

Half-life of curcuminoids metabolites in plasma (t1/2, expressed in minutes);

Terminal elimination rate constant of total curcuminoids in plasma (λz)24hours

Terminal elimination rate constant of total curcuminoids in plasma (λz);

Terminal elimination rate constant curcuminoids separately (curcumin, DMC, BDMC) in plasma (λz)24hours

Terminal elimination rate constant curcuminoids separately (curcumin, DMC, BDMC) in plasma (λz);

Terminal elimination rate constant curcuminoids metabolites in plasma (λz)24hours

Terminal elimination rate constant curcuminoids metabolites in plasma (λz);

Relative bioavailabilityfrom 0 to 24 hours

Relative bioavailability from 0 to 24 hours defined as the ratio of dose-normalized AUC0-24h of total curcuminoids for the different tested formulation to the dose-normalized AUC0-24h obtained for the reference product (turmeric extract 95% curcuminoids).

Trial Locations

Locations (1)

Biofortis Mérieux NutriSciences

🇫🇷

Saint-Herblain, France

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