WO2001013930A1

WO2001013930A1 - Dietetic use of cynara cardunculus and silybum marianum oils

Info

Publication number: WO2001013930A1
Application number: PCT/FR1999/002046
Authority: WO
Inventors: Jean Julia
Original assignee: Jean Julia
Priority date: 1999-08-26
Filing date: 1999-08-26
Publication date: 2001-03-01
Also published as: AU5425999A; EP1176973A1

Abstract

. The invention concerns a soluble encapsulated dietetic composition for oral or rectal administration. The invention is characterised in that said composition contains oil produced by cold mixing and pressing, under high pressure, of unhulled seeds of Cynara Carbunculus or of Silybum Marianum, in a proportion between 0.5 % and 100 %. In a preferred embodiment, each capsule comprises 500 mg of Cynara Carbunculus or Silybum Marianum oil. In such case, the composition may be administered to n adult being treated in doses of two to three capsules per day. Advantageously, the capsules are packaged in lots of 30, 60, 90 and 120 capsules, each lot generally corresponding to a standard treatment.

Description

DIETETIC USE OF CYNARA CARDUNCULUS OILS AND

OF SILYBUM MARIANUM.

The present invention relates to a composition for dietary use based on Cynara Cardunculus oil or Silybum Mananum. It also relates to an oil extraction process suitable for the manufacture of a composition for dietetic use.

Certain subjects of the thistle family are known for their efficiency with regard to certain ailments. This is how Cnicus Benedictus exerts its effects on digestion and fever, teasel (Dipsacus Silvestris) on eczema and acne, Cynara Cardunculus and Silybum Marianum on the liver, varicose veins and hemorrhoids.

It has been demonstrated, as described in French patent 2,716,371, that the use in cosmetic products of the oil produced by cold pressing, under high pressure, seeds of Cynara Cardunculus, gave result in good results in the skin and hair areas.

As a follow-up to the work undertaken on Cynara Cardunculus oil, a systematic study of the applications of this oil revealed surprising results in the field of dietetics. Equivalent results were obtained by applying a Silybum Marianum oil. Consequently, the present invention relates to a composition based on Cynara Cardunculus oil or Silibum Marianum suitable for application in dietetics.

A composition for dietetic use is proposed, packaged in a soluble capsule which can be administered orally or rectally, containing oil produced by kneading and cold pressing, under high pressure, of

Cynara Cardunculus or Sylibum Marianum unshelled, in a proportion of 0.5% to 100%.

A study on the composition of such an oil has shown that the latter contains, expressed as silybin, silymarin at a high dose (276 mg per liter, or 300 mg per kilogram). This silymarin is directly bioavailable, which is not the case, for example, of silymarin extracted chemically from the milk thistle ball. According to studies carried out on silymarin, the latter has membrane compatibility with the cell. Its action at the hepatic level is reflected in particular by a protective action with respect to the hepatic lesions produced by the toxins, due to the membrane affinity reducing the membrane passage, and by a regenerative action of the liver, due to the increase in the multiplication of liver cells it causes.

In addition, the oil produced by kneading and cold pressing, under high pressure, of unhulled Cynara Cardunculus or Sylibum Marianum seeds contains, as will be described in more detail below, a large amount of acid. linoleic and oleic acid, all essential amino acids, phytosterols contained in unsaponifiables, vitamin E and beta-carotene bioavailable. The action of these elements works in synergy, and produces an unexpected dietetic effect.

Entering in proportion from 0.5% to 100% in a composition for dietetic use as a food supplement, this oil is indicated in particular in the following cases:

-hepatic degeneration produced by hepatitis, cirrhosis or abuse of alcohol, tobacco, or very aggressive pharmacological treatments; -stress; - fatigue and convalescence;

-dermatitis, eczema and situations of excessive drying of the skin;

-dysmenorrhea and amenorrhea; -mastites; -fertility problems;

-prevention of the appearance of tumors; - dieting; -hypercholestérolémie. One can think, considering the studies carried out on the oil produced by mixing and cold pressing, under high pressure, of seeds of Cynara

Unhulled Cardunculus or Sylibum Marianum, as the actions of a composition for dietetic use containing from 0.5% to 100% of this oil are the following:

-increase in the level of prostaglandins PGE1 involved in the process of coagulation and platelet aggregation and the balance of the skin;

-increased production of growth hormone;

-increased production of prolactin and lutein and follicular hormone necessary in the process of the menstrual cycle. -maintaining the integrity of the mitochondrial membrane;

-increase in the protein synthesis of hepatic mitochondria and regeneration of the hepatic parenchyma;

- adaptation of free radicals;

-protection against oxidation of cells responsible for the destruction of cancer cells.

According to another aspect of the present invention, each capsule comprises from 250 to 500 mg of Cynara Cardunculus or Sylibum Marianum oil. Each capsule will therefore comprise from 0.075 to 0.15 mg of directly bio-available silymarin. Of course, each capsule may also contain any product known in the field of food supplements which can be combined with Cynara Cardunculus or Silybum Marianum oil.

In a currently preferred embodiment, the composition for dietetic use is administered to an adult in cure by dose of two to three capsules per day, each capsule comprising 500 mg of pure oil.

Thus, the daily dose administered to an adult of Cynara Cardunculus or Sylibum Marianum oil will vary between 1000 mg and 1500 mg. In particular, the daily requirements for vitamin E and essential fatty acids will be covered. Advantageously, the capsules are packaged in batches of 30 to 120 capsules, each batch generally corresponding to a standard treatment. Currently, in view of the treatments envisaged, lots of 30, 60, 90 and 120 capsules are preferred.

Of course, the duration of the cure will however depend on the case of indication of the composition. Similarly, depending on the nature of the treatment, the daily dose may be increased.

The toxicity of the oil has been studied, demonstrating that massive doses would be necessary for the body to eventually have any intolerance. No toxic effect appears possible at the recommended doses. A clinical study was carried out on a group of 50 people over a period of 12 months. Part of the group served as a reference, and the rest were treated with capsules containing 500 mg of pure oil, two capsules each morning. Half of the group was treated with Silybum Marianum oil, the rest with Cynara Cardunculus oil. Positive effects were seen in all of the individuals treated. These results are reflected in particular by a feeling of well-being and form with easier digestion, an improvement in liver functions and a convincing decrease in cholesterol levels after analysis.

Other studies, concerning only Cynara Cardunculus oil, have given the following results:

-In a case of fatigue, weariness, lack of business perceived at the change of season, a daily treatment of two capsules dosed with 500 mg of pure oil for one month was undertaken. An improvement was noticed after 15 days of treatment. -In a case of cyclic fatigue, post pondrial drowsiness with flatulence, weakness of the pancreatic and hepatic functions, a daily treatment of three capsules dosed with 500 mg of pure oil for two months was undertaken, associated with a food adjustment. Rapid improvement occurred within two weeks. The return of hepatopancreatic functions has been observed. No recurrence occurred eight months later.

-In a case of digestive heaviness, especially with fatty products, with gastroesophageal reflux, and lack of intellectual dynamism, treatment daily of three capsules dosed at 500 mg of pure oil for three months was undertaken, associated with a food adjustment. Improvement occurred within a month.

The oils of Cynara Cardunculus and Silybum Marianum can be advantageously combined with other food supplements or phytotherapy products depending on the targeted cases. For example, they can be associated with plants with cholesterol-lowering aims.

According to another aspect of the invention, there is provided a process for extracting Cynara Cardunculus or Sylibum Marianum oil for composition for dietetic use, characterized in that it comprises a step of harvesting seeds of Cynara Cardunculus or Sylibum Marianum, carried out with an axial combine harvester, and an extraction step by first pressing without heating said seeds.

Harvesting with an axial combine harvester prevents seeds from being damaged. The extraction is carried out without heating so that the oil has the desired properties.

Advantageously, during the extraction step, the press temperature is less than 50 °.

A preferred embodiment of the present invention is described in the following.

Cynara Cardunculus are cultivated. It is a plant native to the Mediterranean basin. It was cultivated as a vegetable under the name of Cardon or Carde. It is actually the botanical ancestor of the artichoke. It is perennial, stays in place for 10 or 15 years and has an aerial development of between 1, 50 and 3 meters. The plant is cultivated like a sunflower, the culture is completely mechanized. Harvesting is done with a conventional axial combine harvester so as not to damage the seeds. Oilseed yields are in the order of 1.5 to 2 tonnes per hectare in normally carried out cultivation. These seeds have an oil content of 16 to 18% for the first culture cycle and 22 to 26% for the following. This gives rise, in the case of extraction by cold pressure, to a percentage of 12 to 14% of virgin oil during the first cycle, and from 15 to 18% for the following. The oil extraction is done exclusively by first pressing without heating the unhulled seeds. The temperature does not exceed that due to friction of metal parts, the maximum of which is of the order of

40 ° to 50 °. The grain crushing and oil extraction protocols are those described in the specifications for organic farming.

The oil thus obtained is packaged in soluble capsules. Each capsule contains 250 to 500 mg of pure Cynara Cardunculus oil. Of course, each capsule may also contain any product known in the field of food supplements which it is desirable for it to be combined with Cynara Cardunculus oil in view of the composition of the latter, which will now be described.

The oil of Cynara Cardunculus, obtained by the process according to the invention contains in particular the following elements. Fatty acids.

Myristic acid 0.12%

Palmitic acid 11, 12%

Stearic Acid 2.75%

Oleic Acid 21.15% Linoleic Acid 63.10%

Peanut Acid 0.30%

Γ-Linolenic acid 0.05%

Α-Linolenic acid 0.33%

Ester fractions. β-Sistosterol 43.1% δ-7 Stigmastereol 26.7%

Stigmastereol 13.1%

Amino acids per 100 grams.

Aspartic acid 1800 mg

Threonine 790 mg Serine 880 mg

Glutamic acid 2380 mg

Praline 3370 mg

Glycine 6610 mg Alanine 2760 mg

Total cystine 190 mg

Valine 760 m

Methionine 180 mg

Isoleucine 400 mg Leucine 850 mg

Tyrosine 150 mg

Phenyllalanine 510 mg

Lysine 910 mg

Histidine 170 mg Arginine 1980 mg

Tryptophan 50 mg

Other components.

Silymarin 276 mg / l β-Carotene 4 mg / l

Vitamin E 270 mg / l

As for essential fatty acids, the oil contains a large amount of linoleic and oleic acid. It contains 65% polyunsaturated fatty acids and 22% monounsaturated fatty acids. It is ideally dosed to have a major effect in a role of precursor of prostaglandins.

The essential fatty acids contained in the oil are also involved in the structure of cell membranes.

As far as amino acids are concerned, all the essential amino acids are present in Cynara Cardunculus oil. They have in particular a role of vectors, transmitters. They are also involved in the hormonal domain, at the cell level, at the immune level, and are detoxicants.

With regard to the esters contained in the unsaponifiables, the phytosterols contained in the oil of Cynara Cardunculus are correctly dosed and distributed within the unsaponifiables. We know in particular that they contribute to the fight against the deposit of cholesterol in particular in the cardiovascular system. Research has shown that taking phytosterols significantly lowers blood cholesterol levels. They also bring increased protection to the cell. In addition, these substances have an important effect as substitutes for natural estrogens in postmenopausal or pre-menopausal women.

As for vitamin E, it is contained in large quantities in Cynara Cardunculus oil in the natural form RRR-d-alpha tocopherol. This natural form has twice the bioavailability of the synthetic form of vitamin E. Vitamin E acts as an antioxidant, protecting circulating lipids and lipids from cell membranes from oxidation.

The oil also contains beta-carotene which is in particular the precursor of vitamin A in the body. Regarding the sylimarine contained in Cynara oil

Cardunculus, it is directly bio-available, which is not the case, for example, of silymarin extracted chemically from the ball of the achene of milk thistle. According to studies carried out on silymarin, the latter has membrane compatibility with the cell. Its action at the hepatic level is reflected in particular by a protective action with respect to the hepatic lesions produced by the toxins, due to the membrane affinity reducing the membrane passage, and by a regenerative action of the liver, due to the increase in the multiplication of liver cells it causes. It promotes the increase in protein synthesis of liver mitochondhes inducing accelerated regeneration of the liver parenchyma. All these components have common fields of action on the human organism. Their actions operate in synergy and their effects are thereby increased compared to what they would be individually.

Claims

1. Composition for dietetic use, characterized in that, packaged in a soluble capsule which can be administered orally or rectally, it contains oil produced by kneading and cold pressing, under high pressure, of seeds of Cynara Cardunculus or of Sylibum Marianum not shelled, in a proportion of 0.5% to 100%.

2. Composition for dietary use according to claim 1 characterized in that each capsule comprises from 250 to 500 mg of Cynara Cardunculus or Sylibum Marianum oil.

3. Composition for dietary use according to claim 1 characterized in that each capsule comprises 500 mg of Cynara Cardunculus oil or Sylibum Marianum.

4. Composition for dietetic use according to claim 3, characterized in that it is administered to an adult in cure per dose of two to three capsules per day.

5. Composition for dietetic use according to claim 4, characterized in that said capsules are packaged in batches of 30 to 120 capsules, each batch generally corresponding to a standard treatment.

6. Method for extracting Cynara Cardunculus or Sylibum Marianum oil for composition for dietetic use according to any one of the preceding claims, characterized in that it comprises a step of harvesting seeds of Cynara Cardunculus or Sylibum Marianum , carried out with an axial combine harvester, and a step of extraction by first pressing without heating said seeds.

7. Method of extracting Cynara Cardunculus oil or

Sylibum Marianum according to claim 5, characterized in that, during the extraction step, the press temperature is less than 50.