WO2010088897A2

WO2010088897A2 - Plant extracts for regulating body weight

Info

Publication number: WO2010088897A2
Application number: PCT/DE2010/000139
Authority: WO
Inventors: Rudy Susilo
Original assignee: Evoria Gmbh
Priority date: 2009-02-04
Filing date: 2010-02-02
Publication date: 2010-08-12
Also published as: DE102009007780A1; WO2010088897A3

Abstract

The invention relates to the use of an extract or of extracts, of lipophilic extracts and hydrophilic extracts from the fruit of the plant Pandanus conoideus as dietary agents, slimming products, filling food and appetite suppressants, and for preventing and/or treating obesity as well as for regulating body weight.

Description

Plant extracts for the regulation of body weight

description

The invention relates to the use of an extract or extracts of lipophilic extracts as well as hydrophilic extracts of the fruit of the plant Pandanus conoideus as a dietetic, slimming, satiety and appetite suppressants and for the prevention and / or treatment of obesity and for the regulation of body weight.

Pandanus conoideus is an endemic plant species from Irian Jaya, Indonesia. The fruits of this plant are used by the locals as food, food supplement, animal feed, natural dye and as a remedy for various diseases such as worm diseases, blindness, skin diseases and as a wound treatment agent.

The traditional preparation takes place by long cooking of the red outer fruit layer and subsequent rubbing of the pulp to obtain a non-crusted porridge. The resulting oily porridge is used as a daily food or as a remedy.

The Pandanus conoideus is a gourd-like elongated fruit, which has a seedless white, light pulp inside, and around it is the red pulp, which also contains the seeds of the fruit. On the outside, the cylindrical, on average 1 m long, 7.5 kg heavy and with a diameter of 12 cm quite large fruit surrounded by a red shell.

Obesity is caused by metabolic disorders due to genetic causes or endocrine disorders as well as unhealthy lifestyle habits such as poor dietary habits, and lack of exercise.

Obesity is a major risk factor for heart disease such as

Myocardial infarction, atherosclerosis, heart failure and also for metabolic

Diseases such as diabetes and its sequelae. Obesity worsens the prognosis of such diseases. Therefore, early therapeutic and preventative treatment of obesity is of great importance

Importance. For the treatment of mild obesity diet therapies or exercise therapies are used so far, in severe obesity drug administration is used in combination with these therapies. In addition to the classical synthetic substances, plant extracts are also used as therapeutics for the treatment of obesity.

The extract from the succulent plant Hoodia gordonii, often called hoodia, is considered the latest discovery in obesity therapy. Extract from the dog-family (Apocynaceae) family is able to suppress hunger and appetite, so taking Hoodia may help reduce body weight.

Hoodia grows in semi-deserts in southern Africa in very salt-dry areas, preferably on sandy ground. The main distribution area is the Namibian Kalahari Desert.

Hoodia is unsuitable as a food because it is low nutritious. In addition, the plant smells of rotting flesh and attracts the flies, which is why it is also called the "carrion flower".

How Hoodia acts is so far unclear, only one steroid glycoside with the name P-57 should be responsible for the effect among other things (Maclean DB et al., Brain Res., 1020, 1-11, 2004). The substance can simulate the brain a sufficiently high blood sugar level and thus cause a feeling of satiety. However, with the use of Hoodia, circulatory disturbances were often observed in the first days of use.

The co-development between Unilever and Phytopharm was unilaterally terminated by Unilever in late 2008 due to insufficient safety in the use of Hoodia. The structural similarity of P-57 and the cardiac glycosides suggests that the use of Hoodia may only be ensured under close medical observation. The use of Hoodia to control body weight for the masses is therefore very limited.

Object of the present invention is a means for weight loss, ie a dietary, satiety or appetite suppressants and a means for Weight maintenance and a means to treat and prevent obesity.

This object is achieved by the technical teaching of the independent claims. Advantageous embodiments of the invention are specified in the dependent claims, the description and the examples.

Surprisingly, it has been found that the extracts of the species Pandanus conoideus act as satiety and appetite suppressants and can be used to reduce weight or to prevent weight gain and for the treatment and prophylaxis of obesity and even with prolonged use or at higher doses show no undesirable side effects.

There are different shapes and colors of the fruits of Pandanus conoideus, such as elongated red fruits, short red fruits, brown and yellow fruits. All of these fruits can be used for the purposes of the invention.

Surprisingly, it was found that the daily oral administration of pandanus extract reduces the voluntary food intake in rats. Pandanus extract can be used in the treatment of obesity by reducing the appetite. The effect occurs already 1 day after the application.

The compatibility is very good. There were no changes in the appearance, behavior and general condition of the animals. The biochemical blood analyzes as well as the histological examinations of the organs also showed no abnormalities.

Thus, the present invention provides a means for reducing body weight or preventing weight gain. The pandanus extracts described herein, because of their high safety, are well-suited for wide-scale mass-use weight control applications. The extracts used according to the invention can be obtained in a known manner, for example

1) by the direct compression of the red pulp, from which an oily or oily product is obtained 2) by extraction of the red pulp with organic solvents, in particular lipophilic solvents, from which also an oily or oily product is obtained

3) by alcoholic extraction of the red pulp,

4) by alcoholic extraction of the kernels; 5) by direct compression or by the alcoholic extraction of the red pulp together with the kernels

6) by direct compression of the light inner fruit portion, whereby an aqueous juice is obtained or

7) by alcoholic extraction of the dried bright, inner fruit portion, whereby hydrophilic extracts are obtained.

These extracts may be used in pure form or prepared as a dietary supplement, alone or in combination as slimming products, satiety agents, appetite suppressants or weight maintenance agents, as well as weight loss. The term "dietary supplement" includes both medicines and dietary supplements.

Sattmers are agents that give the feeling of being full without actually consuming a satisfying amount of food, and appetite suppressants lower or suppress the appetite, the so-called "cravings," so that one generally has less desire to eat.

Such agents are available in a wide variety on the market, with the extent of known side effects being similar in scope. The traditional satiety or appetite suppressants sometimes lead to circulatory disorders, high cholesterol, high blood pressure, pulmonary hypertension, headaches and anxiety, just to name a few side effects. In addition, some appetite suppressants have a mood-enhancing effect and lead to dependencies, that a rapid increase in weight occurs when discontinuing the remedy.

Such partly drastic side effects could not be detected in the extracts of Pandanus conoid used according to the invention. The lack of harmful side effects are thus as surprising as the weight-reducing effect of the extracts of the present invention. Thus, the present invention relates to the use of extracts of Pandanus conoid for the manufacture of a dietary agent for use as an appetite suppressant, satiety, slimming or weight maintenance or weight loss agent. The means for

Weight maintenance is especially taken after a completed diet for a longer period of time, because it has been shown that the extracts counteract at a continuous intake in lower concentrations of a renewed weight gain after a diet.

Further, the present application discloses methods for obtaining the extracts such as a lipophilic extract from the red pulp of the fruits of the species Pandanus conoideus, by direct compression, ie cold pressing of the separated red pulp preferably without any chemical additives at temperatures preferably below 40 ⁰ or C is obtained by extraction of the separated comminuted red pulp with organic solvents at temperatures preferably below 4O ⁰ C. The extractions can in principle be carried out at temperatures between 4 ° C and 100 ⁰ C. Particularly preferred, however, is the cold pressing below 40 ⁰ C because on the one hand has been found that when cooking the red pulp in water or an organic solvent important bioactive substances such as tocopherols and other vitamins, phytosterols, etc. are destroyed. In addition, an extract prepared by cooking quickly becomes rancid. The preferred cold pressing surprisingly yields extracts, primarily oils, which are stable for at least one year and probably much longer. The previous stability data show a stability of two years of samples that have been stored for two years at 4 ° C year. The stability test will be continued and significantly longer stabilities are expected.

A temperature increase during the extraction process or the processing method of the red pulp above 40 ⁰ C surprisingly leads to a reduction in the stability and storage stability of the resulting extract. The longer the temperature during the extraction of the red pulp is above 40 ° C and the higher the temperature during the production process of the oil from the red pulp above 40 ⁰ C, the lower the stability of the extract. Thus, it is important in the to ensure that the extraction and processing conditions do not exceed a temperature of 60 ^° C., preferably 50 ^° C. and more preferably 40 ^° C., and ideally the entire extraction and oil extraction process is carried out at room temperature becomes.

Known methods of extracting the red pulp include cooking the red pulp, eventually with the addition of water, making a pulp, and skimming the oil floating on the pulp, resulting in oils that quickly turn rancid. This oil is used by the locals against any complaints, with a scientific basis for the effectiveness of the oil is missing.

The present invention now provides extracts for use as slimming aids or weight loss or weight maintenance agents, which may also be applied at high concentrations of up to 20 g per day and per person with an average body weight of 80 kg, without exhibiting harmful side effects , which were previously described as incompatible or even poisonous.

Hexane, heptane, cyclohexane, chloroform, methylene chloride, ethyl acetate, diethyl ether, petroleum ether, tert-butyl methyl ether, THF, methanol, ethanol, propanol, isopropanol, butanol, isobutanol, sec-butanol, acetone and mixtures are preferred for the extraction this solvent is used. After extraction, the solvent is preferably removed and recycled to reuse for further extractions. The concentrated oil contains the weight-affecting components of the extracted pulp.

Another preferred extraction method is an alcohol and / or alcohol-water extraction of the pulp and kernels by first grinding the red pulp and seeds at temperatures below 4O ⁰ C, mixed with Alhokol and / or water mixture with stirring and then pressed and filtered. , Pulp and kernels can also be dried before grinding. The crushed kernels together with the remaining ground pulp are then treated analogously to the process for alcohol and / or alcohol-water extraction of the fresh material. Another method of the present application relates to the production of a hydrophilic extract of the separated core of the fruit of the species pandanus conoideus by crushing the seeds at temperatures below of preferably 40 ⁰ C, and extraction of the crushed seeds with a hydrophilic solvent at temperatures below of preferably 40 ⁰ C. Again, as with the other extractions, the extractions can be carried out at temperatures between 4 ° C and 100 ⁰ C in principle, but preferably temperatures of 60 ⁰ C and particularly preferably from 40 ⁰ C should not be exceeded.

The hydrophilic solvent used is preferably water, acetone, tetrahydrofuran (THF), methanol, ethanol, propanol, isopropanol, butanol or mixtures of these solvents, water, methanol and ethanol or mixtures of water, methanol and ethanol being preferred. After possibly multiple extraction and combination of the hydrophilic extracts, the solvent is removed again and used again. These steps should preferably be performed at temperatures below 40 ° C. The concentrated extract contains the weight-regulating components from the seeds of this fruit.

Another method of the present application relates to the preparation of a hydrophilic extract from the white pulp of the fruits of the species Pandanus conoid by direct compression of the separated white pulp with or without additives such as addition of antioxidants at temperatures preferably below 40 ⁰ C or by drying and comminution of the separated white pulp at temperatures below preferably 40 ⁰ C and subsequent extraction of the dried crushed white pulp by means of hydrophilic

Solvent.

The hydrophilic solvent used is preferably water, acetone, tetrahydrofuran (THF), methanol, ethanol, propanol, isopropanol, butanol or mixtures of these solvents, water, methanol and ethanol or mixtures of water, methanol and ethanol being preferred. After possibly multiple extraction of the white pulp and blending of the hydrophilic extracts, the solvent is removed again and can be reused. All extraction steps should preferably be carried out at temperatures below 40 ^° C. The concentrated Extract contains the pharmacologically active ingredients from the white pulp of Pandanus conoideus.

The fruit of Pandanus conoideus consists of an inner bright fruit and a red, nucleated and oily outer fruit. The present application discloses 7 possible extracts which can be obtained from this fruit. These extracts may be used alone or in combination, preferably as an aqueous solution, as an oil or as a solid.

To obtain the weight-controlling extracts, the fruits are cleaned and the red, outer fruit layer separated from the white, bright, inner fruit portion. The various extracts can be obtained in various ways, as disclosed, for example, in Examples 1-7.

All operations are preferably carried out at temperatures of 5-8O ⁰ C, more preferably at 10 ° C to 60 ⁰ C, more preferably at 15 - 45 ° C, even more preferably at 17 - 40 ⁰ C and particularly preferably at 19 ⁰ C - 38 ° C performed. It is further preferred if the operations are carried out at temperatures below 60 ⁰ C, preferably below 50 ° C and particularly preferably below 40 ⁰ C.

A simplified procedure for obtaining an extract from the red pulp is first to separate the red pulp from the kernels, then to crush and extract several times with an organic solvent. If ethanol is used for the extraction, then this alcoholic extract can be used directly as a dietary agent. This method is particularly suitable for the use of physiologically acceptable solvents and preferably for alcohols such as ethanol, isopropanol and especially for ethanol.

A preferred method for obtaining an extract from the red pulp together with the kernels is to first crush the red pulp together with the kernels and extract several times with an organic solvent. If ethanol is used for the extraction, then this alcoholic extract can be used directly as a dietary agent. This method is particularly suitable for the use of physiologically acceptable solvents and preferably for Alcohols such as ethanol, isopropanol and especially for ethanol. Of course, the extract can also be prepared from the dried red pulp together with the seeds by the same method.

A simplified method for obtaining an alcoholic extract from the light pulp is to dry the light white inner pulp, preferably in the air, then to crush it and extract it several times with a hydrophilic solvent. If ethanol or ethanol-water mixtures are used for the extraction, then this alcoholic extract can be used directly as a medicine.

Another possibility is to cold-press the inner bright pulp (preferably T <40 ° C). The resulting aqueous extract may optionally be supplemented with flavoring agents, colorants and / or preservatives and may be used as a dietetic in the present form. Of course, the aqueous extract may also be administered as a juice or dried and the resulting residue e.g. be formulated as a capsule or tablet or as a powder for incorporation into any other beverage such as milk, cocoa, tea, water or the like.

If the extraction of the separated and crushed kernels by means of ethanol, so this ethanolic extract can be used directly as a dietary agent.

Thus, the present application also relates in particular ethanolic extracts, which were obtained directly from the red, from the light or white pulp and from the cores directly under mild conditions (preferably T <40 ° C). The recovered alcoholic solution can be concentrated and can serve to prepare an ethanolic solution or a solid after drying, wherein the solid can be added as active component to conventional formulations.

For example, a preferred extraction method for Pandanus conoid includes the following steps: 1) Separation of the fruit into bright, white inner flesh and into the red layer where the red flesh and seeds are. 2) cold pressing or extraction of the red layer with organic solvents to recover the oily fraction, and 3) Separation of the red layer into red pulp and seeds.

4) cold pressing of the red pulp to gain the oil fraction, and

5) extraction of the residue of the red pulp with alcohol (e.g., methanol, ethanol, propanol, iso-propanol, butanol); or

6) extraction of the oil directly from the red pulp with alcohol or other organic solvents,

7) extraction of the cores with hydrophilic solvents,

8) Cold white pulp cold presses to gain juice, or

9) optional extraction of white light pulp with hydrophilic solvents, and / or

10) Dry white pulp, and

11) subsequent extraction of white bright pulp with hydrophilic solvents.

Similar extraction methods can be described as follows and include at least some of the following steps: a) separation of the fruit into bright white inner pulp and red pulp together with the kernels, b) separation of the red pulp from the kernels, c) cold pressing or extraction with organic solvents (d) cold pressing of the red pulp, and (e) crushing and / or homogenisation of the red pulp, and (f) extraction of the juice from the red pulp and the minced or homogenised red pulp with alcohols or other organic lipophilic solvents and g) collection and concentration of the lipophilic extracts, or h) comminution of the cores and i) extraction of the comminuted cores with hydrophilic solvents, and j) collection and concentration of the hydrophilic extracts, or k) cold pressing of the white light internal pulp, or comminution and / or homogenization of the dried white bright pulp, and

I) Extraction of minced or homogenized dried white light pulp with hydrophilic solvents, and m) Collection and concentration of the hydrophilic extracts.

Also, the lipophilic fraction (the oil) from Pandanus conoideus can be used directly, without further processing for obesity or obesity or Freßsucht (dosage 1-2 tablespoons per day) or filled directly into softgel capsules.

An extract or extracts of Pandanus conoidus is / are preferably used to prepare a dietetic composition or dietary, appetite suppressant or satyminer containing the extract or extracts of Pandanus conoid together with at least one pharmacologically acceptable excipient, carrier and / or solvent.

The present application discloses methods by which various extracts can be obtained from the fruit of the plant Pandanus conoideus, depending on how the extraction is carried out. Of course it should be noted that red pulp and bright white pulp can also be extracted together and a prior separation is not mandatory. The same applies to the red pulp and the kernels. These pandanus extracts all show more or less weight reducing or weight regulating activity. Thus, it is preferred in the invention to mix or combine two or more extracts together and to treat obesity, to reduce weight on diet or to maintain weight, i. to prevent weight gain. Accordingly, it is preferable to mix an extract of the red pulp with an extract of the kernels and / or with an extract of the bright white pulp.

Similarly, an extract from the kernels with an extract of the bright white pulp and / or with the juice after cold pressing of bright white pulp and / or with an extract of the red pulp and / or with an extract from the after cold pressing of the red Fruit pulp obtained juice or the components of the juice are prepared after drying.

An extract of the white dried bright pulp and / or juice obtained by cold pressing of the white light pulp may be combined with an extract of the kernels and / or an extract the red pulp and / or with an oil obtained from the cold pressing of the red pulp or the constituents of the oil after it has been dried.

By such combinations, the spectrum of action of the combination of extracts or the dietary agent containing this combination of extracts widened and the activity can also be partially increased.

The preparation of extracts from the red pulp or from the separated kernels or from the red pulp together with the kernels or from the bright, inner portion of the fruit can also by extraction with supercritical fluids (carbon dioxide, propane, butane), preferably with

Carbon dioxide, with or without additional use of entrainers (methanol,

Ethanol). By means of the abovementioned fluids it is possible to obtain preferably lipophilic extracts, whereby by the simultaneous use of polar entraining agents also less lipophilic and more polar to hydrophilic

Extracts can be obtained. Thus, in the extraction of the red

Fruit pulp prefers no polar entrainers used, whereas the

Use of polar entrainers in the extraction of the cores and the inner bright pulp is preferred.

The extracts obtained by extraction with supercritical fluids (carbon dioxide, propane, butane), preferably carbon dioxide, may of course be used singly or in combination with one another, as well as in combination with the extracts not obtained by supercritical fluids. To extract the extracts, the following extraction methods are preferably used: ethanol-water extraction, hexane extraction and supercritical CO ₂ extraction.

The term extract is understood to mean both the liquid phase after a single extraction and the combined liquid phases of several extractions. In addition, the term extract is also the narrowed liquid

Phase in which the solvent has been partially, substantially or completely removed, so that extract may also mean a solid residue which has been obtained after removal of the solvent, preferably under reduced pressure and after drying of the solid ingredients such as a lyophilisate. The extracts described herein may be used alone or in combination with other extracts of the invention and / or in combination with other active ingredients, vitamins, trace elements, minerals as obtained or in the form of dietary formulations and compositions for obesity, obesity, weight gain for overweight or normal weight as well as against eating cravings and lack of satiety.

The dietary or dietetic composition containing an extract or several extracts of Pandanus conoidus can be prepared in a known manner with the usual solid or liquid carriers or diluents and the commonly used pharmaceutical excipients according to the desired mode of administration with a suitable dosage. Such dosage forms are for example tablets,

Mini-tablets, microtablets, film-coated tablets, coated tablets, dragees, capsules, microcapsules, micropellets and pellets, pills, granules, powders, solutions, drops, juices, suspensions, suppositories, enemas, emulsions, dispersions, creams, gels, ointments, syrups or depot forms.

Such preparations are useful inter alia for intravenous, intraperitoneal, intramuscular, subcutaneous, oral, rectal, transdermal, topical, intradermal, intragastric, intracutaneous, intranasal, intrabuccal, percutaneous or sublingual administration, with oral administration being of course preferred.

Corresponding tablets can be prepared, for example, by mixing the extract (s) with known excipients, for example inert diluents such as dextrose, sugar, sorbitol, mannitol, polyvinylpyrrolidone, disintegrants such as corn starch or alginic acid, binders such as starch or gelatin, lubricants such as magnesium stearate or talc and / or or agents for achieving a depot effect and for achieving a controlled release, such as methyl / ethyl acrylate derivatives (Eudragit), carboxypolymethylene,

Carboxymethyl cellulose, hydroxypropylmethyl cellulose, cellulose acetate phthalate or polyvinyl acetate. The tablets can also consist of several layers.

Coated tablets can accordingly be produced by coating cores produced analogously to the tablets with agents customarily used in tablet coatings, for example polyvinylpyrrolidone or Eudragit, shellac, gum arabic, talc, titanium dioxide or sugar. It can also the Drageum cover consist of several layers, with the above mentioned in the tablets excipients can be used.

Solutions or suspensions with the extract may additionally taste-improving agents such as saccharin, cyclamate or sugar as well

Flavorings such as vanillin or orange extract contain. You can also

Suspension adjuvants such as sodium carboxymethylcellulose or

Preservatives such as p-hydroxybenzoates included. Containing the extract

Capsules can be prepared, for example, by mixing the active ingredient with an inert carrier such as lactose or sorbitol and encapsulating it in gelatin capsules.

The oily or oily extract can also be processed directly into soft gelatin capsules.

Suitable suppositories can be prepared, for example, by mixing with suitable carriers such as neutral fats or polyethylene glycol or derivatives thereof.

The lipophilic fraction and / or the extracts may also be administered as enema (rectal instillation).

For example, lactose, starch, sorbitol, sucrose, cellulose, magnesium stearate, dicalcium phosphates, calcium sulfates, talc, mannitol, ethyl alcohol and the like can be used as pharmacologically acceptable carriers. Powders and tablets may consist of 5 to 95% of such a carrier.

Furthermore, disintegrating agents, dyes, flavorings and / or binders may be added to the dietetic compositions.

It is also preferable to provide the extracts and dietary agents with vitamins such as vitamin A, vitamin C (ascorbic acid), vitamin D, vitamin H, vitamin K, vitamin E, vitamin B, vitamin B 2, vitamin B 3, vitamin B 8, vitamin B 2, vitamin B 2, thiamine, riboflavin, Niacin, pyridoxine and folic acid.

Furthermore, trace elements, iron, magnesium, calcium, iodine or other substances may be added to the extracts and dietary agents, which may not be sufficiently supplied to the body in a diet. Liquid formulations include solutions, suspensions, sprays and emulsions.

For the preparation of suppositories low-melting waxes, fatty acid esters and glycerides are preferably used.

Capsules are made, for example, from methylcellulose, polyvinyl alcohols or denatured gelatin or starch.

Starch, sodium carboxymethyl starch, natural and synthetic gums such as locust bean gum, karaya, guar, tragacanth and agar, and cellulose derivatives such as methyl cellulose, sodium carboxymethyl cellulose, microcrystalline cellulose and alginates, clays and bentonites can be used as disintegrants. These ingredients can be used in amounts of 2 to 30 wt .-%.

As a binder, sugar, starch from grain, rice or potatoes, natural sugars, natural as well as synthetic gums such as acacia or guar gum, gelatin, tragacanth, alginic acid, sodium alginate, ammonium calcium alginate, methyl cellulose, carboxymethyl cellulose,

Polyethylene glycol, waxes, sodium carboxymethylcellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone and inorganic compounds such as magnesium-aluminum-silicates are added. The binders can be added in amounts of 1 to 30 wt .-%.

As lubricants, stearates such as magnesium stearate, calcium stearate, potassium stearate, stearic acid, refractory waxes, as well as water-soluble lubricants such as sodium chloride, sodium benzoate, sodium acetate, sodium oleate, polyethylene glycol and amino acids such as leucine can be used. Such lubricants can be used in amounts of 0.05 to 15 wt .-%.

The dietary and dietary formulations are used as slimming aids, appetite suppressants and satiety in diets and for the treatment of obesity, obesity and avidity and can also be used prophylactically due to their good tolerability and the lack of side effects and the lack of addiction. Such prophylactic uses of the extracts and dietary agents include in particular one Continuous use of the extracts or dietary products after a successful diet or weight loss diet to prevent regaining weight and avoid the yo-yo effect. Jojo's effect is the observation that after a diet with weight loss at the end of the diet a stronger weight gain is observed, which in turn leads to a more extensive diet and one can not maintain the weight achieved after a diet.

The dosage of the extracts can be chosen in a wide range because of undetectable side effects or toxicity.

In animal studies with rats, the dosage was 10 mg - 5,000 mg / kg body weight (body weight), preferably 50-2000 mg / kg body weight and especially preferably 100-1,000 mg / kg body weight.

In humans, the usual dosage is 10 mg - 20,000 mg / kg body weight (body weight), preferably 100-15,000 mg / kg body weight and especially preferably 500-5,000 mg / kg body weight. Per application is preferably an amount of 10 mg - 20 000 mg extract or diet containing 10 mg - 20 000 mg extract and more preferably an amount of 100 mg - 15,000 mg extract or diet containing 100 mg - 15,000 mg extract and particularly preferably diet containing 500 mg - 5,000 mg extract administered. Usually, 1 to 10, preferably 3 to 6, doses are administered per day.

Brief Description:

Figure 1 shows the effects of pandanus extract on body weight

The experiment was carried out in young rats with an average body weight of 280, due to

Grow about 5 g per day. FIG. 1 shows that no further increase in weight occurs more than one day after administration of the pandanus extract.

FIG. 2 shows influences of the pandanus extract on the organs of the rats using the example of liver, kidney and spleen

Figure 3 shows the course of weight gain in rats in the growth phase on the one hand with administration of pandanus extract and on the other after stopping the administration of pandanus extract Examples

Example 1: Recovery of cold pressed oil

The red, nucleated fruit layer is preferably stirred with added water in a blender to separate the red pulp from the kernels. The recovered, red Fruchtfleischbrei be pressed. After centrifugation and filtration, a clear, red, viscous oil (cold pressed virgin oil, extract 1) is obtained. The cores are washed with water and dried at a temperature of at most 40 ⁰ C in a drying oven and stored for further processing.

Example 2:

Extraction of the Oil by Extraction with Organic Solvent The red pulp, obtained as above, is washed with a lipophilic solvent, e.g. Hexane, pentane, cyclohexane, petroleum ether, heptane, tert-butyl methyl ether extracted. After drying (dehydration), centrifugation and filtration to obtain the red, viscous oil.

Example 3: Recovery of the alcohol extracts

The red pulp slurry obtained as above is extracted with a polar solvent such as an alcohol, ether, acetone, THF, ethyl acetate, and preferably methanol or ethanol. After evaporation of the solvent gives the alcoholic extract.

Example 4:

Obtaining the alcohol extracts from the cores

The cores obtained as described above are crushed and extracted with 50% methanol-water. After evaporation of the solvent to obtain the extract of the cores (nuclear extract). Example 5:

Extraction of the dried red fruit layer extract including the cores by extraction with organic solvents

The red fruit portion together with the cores is dried at below 40 ⁰ C in a drying oven. The water content of the dried material should be below 12%. The dry material is crushed and extracted with organic solvents such as methanol, ethanol, acetone, isopropyl alcohol or hexane, preferably with ethanol. A dark red, viscous oily product (oleosum) is obtained.

Such extraction can of course also be carried out with fresh fruit material.

Example 6:

Obtaining the aqueous juice from the white / light inner fruit layer. From the white layer, i. the inner bright pulp content is obtained by direct compression an aqueous phase. Stabilizers such as e.g. Ascorbic acid or other antioxidants may be added to the juice to prevent oxidation by atmospheric oxygen. The juice can be used directly or dried for later use.

Example 7:

Extraction of alcohol extracts from the inner, light fruit The white, bright fruit is cut into slices of approx. 4x4x2 cm and dried in a drying oven. The pieces are crushed and extracted with 50% methanol-water or 50% ethanol-water.

Example 8:

Extracting the extract from the red pulp with supercritical carbon dioxide (Tk = 31 ⁰ C ₁ Pk = 73.9 bar) In the extraction container, the red fruit pulp is mixed with the liquid carbon dioxide (90 bar, 8 kg CO ₂ / h over 4 h). The loaded with plant ingredients solvent is pumped by means of a pump in the separation vessel. On the way there, the pressure is reduced to subcritical by means of a throttle valve Conditions relaxed. The solubility decreases and the dissolved lipophilic substances precipitate. In the separation vessel, the lipophilic substances (oil fraction) are separated from the gas. The gas is recompressed to the fluid and reused. By adding various concentrations of entrainers (eg methanol or ethanol), medium-polar as well as polar substances can be gently extracted.

Example 9: Preparation of the extracts

After thoroughly washing the fruit with water, the outer red layer is separated from the inner white layer. From the red layer, the pulp portion is separated from the kernels by shaking and / or rubbing.

The red pulp portion is homogenized, pressed and centrifuged. After centrifugation, the oil phase is separated (extract 1). The residue is extracted first with n-hexane (extract 2) and then with methanol (extract 3).

The kernels are crushed and extracted with 50% methanol (extract 4).

From the white layer, an aqueous phase (extract 5) is obtained by direct compression. The residue after compression is dried and extracted with 50% methanol (extract 6).

All operations are carried out under 40 ⁰ C.

Example 10 Preparation of a Ready to Drink Granules for Appetite Inhibition

Pandanus extract 15 g

Microcrystalline cellulose 25 g

Aerosil 8 g

Walocel CRT 8g

Magnesium stearate 4 g

Icing sugar 28 g

Ethanol ad 100 g Flavors and aromas such as orange flavor, passion fruit flavor can be added.

All ingredients are mixed and stirred to homogeneity. The granules are passed through a sieve.

To prepare a drinking solution, 5 g of the granules are stirred into 100 ml of water. The aqueous suspension is ready to drink.

Of course, the granules can also be stirred into yoghurt or milk and taken.

Example 11: Preparation of enteric-coated granules with sustained release for appetite inhibition

Production of pellets:

Pandanus extract 10 g

Aerosil 10 g

Lactose 120 g

The binder solution consists of 7% polyvinylpyrrolidone solution in 600 ml

Water.

The sugar cores are moistened with the binder solution and the mixture of

Pandanus extract / Aerosil is applied to the pellets. The granules are dried and sieved. Pellets are obtained with granule size of 0.5-1 mm.

The pellets are now coated with Eudragit.

Coating of the pellets with Eudragit L 30:

Pellets 100 g

Eudragit L 30 60 g

Talc 10 g triethyl citrate 2 g

Water 50 g Talc and triethyl citrate are homogenized in water for 20 minutes. The suspension is added to the Eudragit dispersion with stirring. The dispersion is stirred until the spraying process is complete.

The pellets are filled in sachet to 5-10 g per serving. The pellets can be mixed with yoghurt or fruit juices or suspended and taken in this way.

Example 12:

Production of pandanus extract in soft gelatin capsules

The extract can be formulated in an amount of 300 mg to 1000 mg in soft gelatin capsules.

Example 13:

Production of fitness scales for weight control

Pandanus extract 50 g

Oatmeal 100 g

Protein powder 50 g

Egg white / egg white 50 g

Milk 200 g

Raisins 20 g

The ingredients are mixed and stirred to homogeneity, poured into the mold and heated at 18O ⁰ C for about 30 minutes in the oven. There are 10 bar pieces, each bar piece contains 5 g of pandanus extract.

Example 14A:

Carrying out an animal experiment on rats

Wistar rats were treated with pandanus extract 500 mg / kg body weight for 5 days (n = 3). The oral administration of the extract was administered daily by means of a probe. The animals in the control group were treated with physiological saline. It can clearly be seen in FIG. 1 that the average body weight of the animals in the pandanus extract group changes slightly in the treatment period (day 1 = 280 g, Day 5 = 279 g), while the average body weight of the animals in the control group increased steadily. The difference is significant (p = 0.006, paired t-test) (see Figure 1).

Example 14B:

Wistar rats were treated with pandanus extract 500 mg / kg body weight for 5 days (n = 3). The oral administration of the extract was administered daily by means of a probe. The animals in the control group were treated with physiological saline.

Fig. 2 shows that the relative organ weights (liver, spleen, and kidney weights relative to body weight) in the pandanus extract group have no differences in the two groups as compared with the control group.

Studies of liver and inflammatory parameters such as bilirubin, lactate dehydrogenase, aspartate-amino-transferase, alanine-amino-transferase, alkaline phosphatase showed no significant changes compared to the control rats.

These results indicate the good tolerability of the extract. The good tolerability of the extract or other preparations from the pandanus fruits can also be taken from the wide use of the fruit (raw or cooked). Such preparations are taken up to 20 g (oily preparation) or 100 g (mushy preparation) daily in Indonesia. Serious adverse effects have not been observed so far.

Example 14C:

Control of body weight with Pandanus extract:

Wistar rats were orally treated with pandanus extract 635 mg / kg body weight for 6 days (n = 5). The oral administration of the extract was administered daily by means of a probe. On day 7, treatment with pandanus extract was stopped. The change in body weight of the animals was further observed until day 11.

FIG. 3 clearly shows the course of the body weight with the administration of pandanus extract in comparison with the course of the body weight at break-off the treatment. It can be clearly seen that the average body weight of the animals changed only slightly with the administration of pandanus extract. However, after interruption of treatment, body weight steadily increases until the end of the observation period on day 11.

The results show that the pandanus extract is effective to regulate body weight.

BeispieM5:

Influences of pandanus extract on food intake in humans

Subjects: 3 healthy subjects between 30-50 years, body mass index 22-30, clinically normal. Design: An application study with cross over design and a one week washout phase, single blind.

Dose: 2 capsules with 400 mg pandanus extract (daily dose 800 mg extract) or 2 placebo capsules

The Pandanus preparation and placebo capsules

Each capsule contains 800 mg of granules with the following composition:

Pandanus extract 400 mg, cellulose 40 mg, Aerosil 296 mg, magnesium stearate 24 mg, starch 40 mg.

The capsules are coated with Eudragit FS 30 D to ensure a targeted release in the small intestine.

The placebo capsules contain starch.

Conducting the application observation

First dosage (dosage A)

- The first dose of 2 capsules (verum or placebo) was given 1 hour before breakfast. The subjects were fasting, the last food intake was at least 8 hours before breakfast.

- Breakfast should be taken within 20 minutes

- Surveys were conducted at 0 and 1 hour and 3 hours after feeding, respectively (questionnaire with 5-step Scores: 1 = very hungry, 2 = hungry, 3 = little hungry, 4 = full, 5 = very full).

Ratings: Changes in the number of points in the survey.

Second dosage (dosage B)

- The second dose of the drugs (verum or placebo) was given 1 hour before lunch.

- Lunch should be taken within 20 minutes. - Surveys were conducted at 0 and 1 hour and 3 hours after feeding (questionnaire with 5-step scores: 1 = very hungry, 2 = hungry, 3 = little hungry, 4 = full, 5 = very full)

Ratings: Changes in the number of points in the survey.

Results

Table 1 shows the changes in the scores of individual subjects after taking pandanus capsules or placebo capsules.

Tab. 1 and Tab. 2 show that, in general, the intake of pandanus extract in comparison to placebo intake increases satiety. The feeling of hunger after fasting for 10 hours is apparently less after taking pandanus capsules compared to placebo.

The effects appear to be greater after the second dose of pandanus capsules (Dosage B) compared to the effects of Dosage A. This could be caused by the subsequent release of the capsules in the small intestine (transport time from ingestion to reaching the small intestine may vary depending on the stomach filling take up to several hours). Due to the later release in the small intestine area higher concentrations of pandanus extract in the small intestine after the second dose compared to the first dose can be achieved.

These results indicate that pandanus extract can suppress hunger and reduce food intake. The effect is particularly evident when the pandanus capsules are taken before a meal. Pandanus extract may therefore be of assistance in the

Body weight regulation can be used. Table 1: Score of individual subjects

Subject 1 Subject 2 Subject 3 Mean

Table 2: Time course of the average score (mean)

(1 = very hungry, 2 = hungry, 3 = little hungry, 4 = full, 5 = very full)

Dosage A

T-O T-1-h T-3-h

Placebo (medium) 1, 6 3.3 2 Verum (medium) 2.6 4 3.3

Dosage B

T-O T-1-h T-3-h

Placebo (medium) 1, 6 2.6 1, 6 Verum (medium) 3.6 4 3.3

Claims

claims

Use of an extract derived from the species Pandanus conoideus for the manufacture of a dietary supplement for use as

Appetite suppressant and satiety and for the treatment and prophylaxis of

Obesity, obesity, obesity or predation and to

Prevention of a new weight gain after completed diet.

2. Use according to claim 1, wherein the extract is obtained from the red outer pulp and / or from the white light inner pulp and / or from the cores.

3. Use according to claim 2, wherein the extract is obtained from the red outer pulp together with the kernels or only from the red pulp by direct compression without any chemical additives.

4. Use according to claim 2, wherein the extract of the red outer pulp together with the kernels or only from the red pulp by extraction with organic solvents methanol, ethanol, propanol,

Isopropanol, acetone, ethyl acetate, hexane is recovered.

5. Use according to claim 2, wherein the extract from the cores is a hydrophilic extract obtained by separation and comminution of the cores and extraction of the comminuted cores with a hydrophilic solvent.

6. Use according to claim 2, wherein the extract from the white bright inner pulp is a hydrophilic extract obtained by direct compression of the separated white bright inner pulp or by drying and comminution of the separated white bright inner pulp and subsequent extraction of the dried crushed white bright internal pulp is obtained with a hydrophilic solvent.

7. Use according to claim 5 or 6, wherein for the extraction of water, ethyl acetate, methanol, ethanol, propanol, isopropanol, THF, acetone or mixtures thereof are used.

8. Use according to claim 2, wherein the extract is obtained from the red outer pulp and / or from the white light inner pulp and / or from the cores by means of supercritical fluids.

9. Dietetic containing an extract or extracts of the species Pandanus conoideus.

10. A dietary preparation according to claim 9 further containing at least one pharmacologically acceptable excipient, carrier and / or solvent.