Study of the Bioavailability of Three Hesperidin Extracts.

NCT03984916 | Completed

• 1 other identifier: HESPERIDIN
• Study Type: interventional
• Target: 15
• Locations: 1 country
• Sites: 1

Brief Summary

The flavonoid hesperidin is present abundantly in citrus fruits and citrus juices. The results of numerous studies suggest that hesperidin perform several beneficial effects on health, including antitumor, antioxidant, anti-inflammatory, hypocholesterolemic and hypoglycemic effects as well as decreasing blood pressure. There are two isomers of hesperidin, -S and -R, being the predominant form in nature the isomer -S. However, currently commercialized hesperidin consists of a mixture of both isomers due to the extraction process of the hesperidin from natural sources. The presence of the rutin disaccharide conjugated to the hesperidin molecule is responsible that most of the ingested hesperidin is metabolized by bacteria in the colon through the enzymatic activity α-rhamnosidase, being this enzymatic activity the limiting step of the hydrolysis and absorption of hesperidin. It has been suggested that the low levels of this enzymatic activity in the gut microbiota is the cause of the low bioavailability of hesperidin and also, at least in part , of the high interindividual variability that exists in the absorption of this compound. The micronization process in order to decrease the size of the hesperidin particles is presented as a way to increase the bioavailability of hesperidin. Another way to increase the absorption of hesperidin that is proposed in this study is to increase the proportion of the isomer -S in the extracts of hesperidin, since being the isomer that mostly occurs in nature, the gut microbiota will have a greater capacity of metabolism for this isomer. On this basis the present hypothesis is posed: the administration of hesperidin formed mainly by the isomer -S and micronized, will present greater bioavailability than hesperidin formed by a mixture of the isomers -S and -R. In turn, the bioavailability of the hesperidin formed mainly by the isomer -S and micronized will present greater bioavailability than the mixture of the isomers -S and -R and micronized. The main objective of this study was to quantify the bioavailability of three extracts of hesperidin:

• Hesperidin extract with a mixture of the isomers -S and -R.
• Hesperidin extract with a mixture of the isomers -S and -R micronized.
• Hesperidin extract with the isomer -S micronized.

Conditions

Biological Availability

Keywords

hesperidin; orange extract

Outcome Measures

Primary Outcomes (1)

• Bioavailability of hesperidin calculated by urine hesperidin concentration

  Fasting hesperidin metabolites levels in urine will be determined before consuming the capsule with orange extract and in four fractions of time (0-3 hours; 3-6 hours; 6-9 hors and 9-24 hours) until 24 hours postprandially after consuming the capsule. The hesperidin levels in urine will be quantified with a Liquid Chromatography (LC)- Mass Spectrometry (MS) equipment.

  At week 2, week 3 and week 4.

Secondary Outcomes (7)

• Area Under The Curve (AUC) of plasma hesperidin levels.

  At week 2, week 3 and week 4.

• Maximum plasma concentration (Cmax).

  At week 2, week 3 and week 4.

• Time for maximum plasma concentration (Tmax).

  At week 2, week 3 and week 4.

• Half-life (T1/2).

  At week 2, week 3 and week 4.

• Hesperidin catabolites levels in plasma.

  At week 2, week 3 and week 4.

Study Arms (3)

Hesperidin Pharma

ACTIVE COMPARATOR

500 mg of sweet orange extract with a mixture of hesperidin isomers -S and -R. The approximate particle size is less than 100 µm for the 90% of the extract, and of 10 µm for 10% of the extract.

Dietary Supplement: Hesperidin Pharma

Hesperidin Pharma_M

ACTIVE COMPARATOR

500 mg of sweet orange extract with a mixture of hesperidin isomers -S and -R. The size of 90% of particles is less than 10 µm.

Dietary Supplement: Hesperidin Pharma_M

Cardiose

EXPERIMENTAL

500 mg of sweet orange extract with more than 90% of the isomer -S. The size of the 90% of particles is less than 10 µm.

Dietary Supplement: Cardiose

Interventions

Hesperidin Pharma DIETARY_SUPPLEMENT

Two capsules with 250 mg of sweet orange extract with a mixture of hesperidin isomers -S and -R.

Hesperidin Pharma

Hesperidin Pharma_M DIETARY_SUPPLEMENT

Two capsules with 250 mg of sweet orange extract each with a mixture of hesperidin isomers -S and -R and micronized.

Hesperidin Pharma_M

Cardiose DIETARY_SUPPLEMENT

Two capsules with 250 mg of sweet orange extract each with more than 90% of hesperidin as isomer -S and micronized.

Cardiose

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Men and women over 18 years of age.
• Firm the informed consent.

You may not qualify if:

• Take supplements or multivitamin supplements or phytotherapeutic products that interfere with the treatment under study up to 30 days before the start of the study.
• Present intolerances and / or food allergies related to hesperidin.
• Take antibiotics up to 30 days before the start of the study.
• Being pregnant or intending to become pregnant.
• Be in breastfeeding period.
• Be a smoker
• Be vegetarian.
• Present some chronic gastrointestinal disease.
• Present some chronic disease in clinical manifestation.

Sponsors & Collaborators

• Technological Centre of Nutrition and Health, Spain: lead
• Fundació Eurecat: collaborator
• Hospital Universitari Sant Joan de Reus: collaborator
• University Rovira i Virgili: collaborator

Study Sites (1)

Centro Tecnológico de Nutrición y Salud (Eurecat-Reus)

Reus, Tarragona, 43203, Spain

Location

Related Links

• Technological Centre of Nutrition and Health. Eurecat\_Reus.

Study Officials

• Rosa Solà, Dr

  Centro Tecnológico de Nutrición y Salud (Eurecat_Reus). Reus, Tarragona, Spain.

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Masking Details: The appearance of the interventions is identical, appearing in capsules of identical appearance and with a numerical code.
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 7, 2019
• First Posted: June 13, 2019
• Study Start: June 13, 2019
• Primary Completion: March 2, 2020
• Study Completion: March 2, 2020
• Last Updated: February 28, 2022

Record last verified: 2022-02

Data Sharing

• IPD Sharing: Will not share

Locations

ES (1)