RU2722728C1 - Kit for appetite control and body weight normalization and method of its application - Google Patents

Abstract

FIELD: food industry; chemistry; pharmaceutics.SUBSTANCE: invention relates to the field of food and chemical-pharmaceutical industry and concerns a set of biologically active substances complexes for appetite control and weight normalization. Kit comprises three products for oral administration. First said product is a complex of biologically active substances in the form of a single dosage form containing thylakoids and a dry extract of bitter orange fruits, standardized by p-Synephrine. Second product is a soft capsule containing ginger oil, olive oil and limonene. Third specified product in the form of a single dosage form contains dry extract of red pepper standardized by capsaicin. Method for controlling appetite and normalizing body weight involves oral intake of kit 2 or 3 times a day, wherein the first and second set products are taken simultaneously before or during meals, and after meal the third product of the kit is taken.EFFECT: invention promotes appetite reduction, a long period of satiety after meals, reduced sweet cravings, as well as facilitates monitoring of calorie content, tones up the body stimulating physical activity.3 cl, 4 ex

Description

The invention relates to the field of food and chemical-pharmaceutical industry and relates to a complex of biologically active substances for controlling appetite and normalizing weight.

The problem of well-being of overweight and obese people is now becoming more and more relevant, mass and socially significant. Modern society provokes inadvertent obesity among its citizens, contributing to the consumption of high-calorie foods with a high content of fat, and at the same time, thanks to technological progress, stimulating a sedentary lifestyle. These social and technological factors contribute to the increase in the prevalence of obesity in recent decades. Obesity is directly related to some of the most common diseases in modern society, including hypertension, coronary heart disease, arthritis, cholecystitis, cancer of the breast, prostate and colon.

As you know, more than thirty biologically active substances are involved in the process of regulating appetite and satiety: proopiomelanocortin, leptin, ghrelin, dopamine, serotonin, secretin, gastrin, information peptide, etc. About half of them are secreted by fat cells. When overweight, the number of fat cells grows very quickly. The more fat cells there are, the more control of appetite and satiety is violated. Thus, there is a significant need to develop methods and means of controlling appetite and, accordingly, preventing overweight and developing obesity.

There is a method of weight loss and appetite control by taking a biologically active supplement containing at least a source of catechins and at least 3% corosolic acid in day or night formulations. The additive may further include leaf extracts of green or black tea (WO 2007053929 (A1) - 2007-05-18).

Known composition for reducing human weight. The composition is presented in the form of a capsule containing an effective amount of capsaicin and / or its analogues, L-tyrosine, additional caffeine and / or its analogues, green tea extract containing catechin and caffeine, and embodiments that include calcium. Also described is a method of reducing and maintaining the weight of a person using the composition (US 2008008770 (A1) - 2008-01-10).

A functional food composition is known that contains probiotics and prebiotics. The composition may include a weight loss compound selected from the group consisting of thylakoid, thylakoid extracts, and combinations thereof. The composition may also include a substance from the group consisting of a proteinase II inhibitor, green coffee bean extract, chlorogenic acid, green tea leaf extract, polyphenols, ashwagandha extract, xanthan gum, chitosan, chromium picolinate, senna, ephedra, bitter orange, fucoxanthin extract white beans, vitamin D, human chorionic gonadotropin, resveratrol, capsaicin, chia, L-carnitine, banana leaf, red clover, ginger, almond, flax seeds, leucine (WO 2015017625 (A1), publ. 2015-02-05).

As the closest analogue, the solution according to EP 1578401 (A2) - 2005-09-28 can be indicated, according to which a method is disclosed that contributes to weight loss, thermogenesis, appetite suppression, muscle mass, increase metabolism and increase energy levels using dietary supplements. An example of the composition of such an additive may be a composition containing specific amounts: epigallocacetin gallate; caffeine; tyrosine; n-acetyl-1-tyrosine; theophylline; theobromine; methionine; gingerols from ginger; DMAE synephrine; proanthocyanidins; quercetin; fisetin; phenylethylamine; tyramine; octopamine; Vitamin C vitamin B6; pantothenic acid; about 5 to about 50 mg of magnesium; aminophylline; yohimbine; alkaloids and flavonoids.

The objective of the present invention is to develop an optimized comprehensive method for controlling appetite and weight in patients with obesity or a tendency to obesity.

The problem is solved by a set of products, which are complexes of biologically active substances, and by the method of its application in the method of controlling appetite and weight.

The kit (kit) according to the invention includes three products (components) and is intended to reduce appetite and normalize weight:

The first product (BMI-XS 1) is the part that should be used with meals.

The composition of BMI-XS 1 for oral administration includes:

- thylakoids from 1000 mg to 20,000 mg,

- dry extract of bitter orange fruit, standardized for p-synephrine with a content of p-synephrine from 0.5 to 200 mg, and optional

- dry extract of kudzu roots from 0.5 mg to 500 mg,

- dry extract of black tea, standardized for caffeine with a caffeine content of from 0.5 mg to 200 mg,

- dry extract of green tea, standardized for L-theanine with an L-theanine content of from 0.5 mg to 200 mg and for catechins with a catechin content of from 0.5 to 200 mg,

- Ceylon cinnamon extract standardized for phenolic acids with a phenolic acid content of 0.5 to 500 mg.

The content of active substances is presented based on one unit dosage form for administration of the composition.

Thylakoids are membrane-limited compartments within chloroplasts and cyanobacteria. Light-dependent photosynthesis reactions occur in thylakoids. Thylakoids slow down the digestion of fats due to reversible inhibition of lipase / colipase, stimulation of cholecystokinin, type 1 glucagin peptide, leptin and incretin, as well as inhibition of ghrelin, which causes a long-lasting feeling of satiety and satisfaction with a small amount of food, which can comfortably reduce caloric intake. Since thylakoid lipase blockade is reversible, thylakoid administration does not cause steatorrhea, a complication associated with irreversible lipase blockers. Thylakoids reduce cravings for sweets, as well as a combination of sweet and fatty (chocolate).

A dry spinach extract obtained from an aqueous extract of spinach leaves can be used as a source of thylakoid.

The extract of bitter orange fruit (orange), standardized for p-synephrine, is a dry extract obtained by the method of alcohol extraction of unripe fruits, peel of ripe fruits, followed by concentration and drying (https://wirud.ru/wp-content/uploads/2017 /03/citrus-aurantium.pdf). The standardized extract should contain at least 6% synephrine (or specifications 8%, 10% 30%, 98%). Bitter orange synephrine stimulates beta 3 adrenergic receptors, thereby enhancing the breakdown of white adipose tissue, promoting the conversion of beige adipose tissue into brown, enhances glycogenolysis and glycolysis, binds to NMUR 2 hypothalamic receptors, thereby reducing appetite, regulates the metabolism of fats and carbohydrates, promotes the breakdown of fats during physical exertion, enhances thermogenesis without causing hyperstimulation of the nervous and cardiovascular systems, and increases stress resistance.

Kudzu dry root extract (pueraria) is a source of isoflavones, glycosides and puerarin flavanoid. Examples of the extract are root extraction with a solvent such as water, water-alcohol solvents, ethanol 95%, methanol or propylene glycol with water, followed by concentration and drying (CN 101550133, CN 103224491, etc.). The use of kudzu extract improves glucose tolerance and reduces fasting glucose. Kudzu flavanoids reduce fat mass by lowering adiponectin, reduce food cravings, nicotine and alcohol, lower cholesterol, have hepatoprotective properties, inhibit alcoholic fatty degeneration of the liver, and prevent muscle loss by increasing the level of PGC-1 alpha (peroxisome activated receptor type 1 alpha proliferators), a regulator of muscle mass that protects against muscle atrophy, and phosphorylated AMPK (adenosine monophosphate activated protein kinase), a regulator of the nutrient state of cells, glucose transport into the cell, fatty acid oxidation and metabolic adaptation of skeletal muscles.

Dry extract of green tea, standardized for theanine and catechins, can be obtained, for example, from the crushed leaves of green unfermented tea Camellia sinensis, a genus of evergreen shrubs or trees of the tea family. In the manufacture of green tea, the leaves are heated to inactivate the enzymes, twisted, then dried to 50% humidity, then twisted again and then dried in the sun. To prepare a dry extract of Green Tea, the leaves are crushed, extracted with water, the resulting liquid extract is defended, purified and concentrated, then the thick extract is dried.

Dry caffeine standardized black tea extract can be obtained, for example, from ground black tea leaves by extraction with water, concentration and drying.

Caffeine, catechins and L-theanine extracts of black and green teas affect energy metabolism by activating the AMP kinase enzyme, helping to break down fats and reduce lipogenesis, reduce the absorption of fats and carbohydrates, thereby reducing calorie intake, regulate microbiota, which helps prevent obesity and maintains the desired weight after it is reduced.

Ceylon Cinnamon Extract - Ceylon cinnamon bark extract (Latin Cortex Cinnamomi zeylanici), standardized for phenolic acids, can be obtained by methods known in the art (e.g., CN 1014600660). Phenolic acids of Ceylon cinnamon reduce glucose levels and also increase the release of intestinal hormones that suppress hunger (UC peptide, glucagon-like peptide 1) and keep ghrelin levels low after meals.

These components in the indicated quantities can be presented in the following dosage (technological) forms:

1) a sachet, which is a mixture of all components obtained by simple mixing of the powdered extracts in the indicated amounts, followed by sprinkling the resulting mixture into separate individual packages (sachets, sticks, plastic or glass bottles).

For example, to make one sachet, you need to mix 3000 mg of spinach extract, 50 mg of bitter orange extract, 50 mg of kudzu extract, 10 mg of black tea extract, 10 mg of green tea extract and 100 mg of Ceylon cinnamon extract. Pour the resulting mixture into individual packaging.

The drug from sachets is used as follows:

- the powder is poured into the mouth and washed down with water or fruit juice without sugar (50-200 ml);

- Before use, the powder is poured into the required amount of water or fruit juice without sugar (50-200 ml), mixed and drunk.

2) gel for oral administration

The composition of the gel for oral administration is identical to the composition of the sachet.

The gel can be made as follows:

- powdered extracts in appropriate quantities are mixed into a homogeneous mass. After mixing, drinking water, thickeners and gelling binders, such as agar, gelatin, pectin, etc., are added to the composition.

- the resulting mass is packaged in an appropriate container (plastic or glass bottles, jars, tubes, etc.)

3) coated or uncoated tablets

The composition (qualitative and quantitative) of the tablets is identical to the composition of the sachet and gel. There are several tablet manufacturing technologies. The main stages of the process are described, for example, in the manual http://www.pharmspravka.ru/farmatsevticheskie-vorosyi-i-otvetyi/study/tverdye-lekarstvennye-formy-tabletki-texnologiya-izgotovleniya.html

4) hard capsules

The composition (qualitative and quantitative) of the capsules is identical to the composition of sachets, gel and tablets. The production technology of filled hard gelatin capsules is described, for example, in the manual https://infopedia.su/17x7b75.html

The second product (BMI-XS 2) is a capsule with ginger oil and D-limonene. Accepted simultaneously with the first component.

The BMI-XS 2 component may include the following components:

- olive oil - from 10 to 500 mg;

- ginger oil - from 5 to 200 mg;

- D-limonene - from 1 to 200 mg.

Since the last listed components are oils, a single dosage form is selected for production - soft gelatin capsules.

For example, the composition of one capsule may be as follows:

- olive oil - 200 mg;

- ginger oil - 25 mg;

- D-limonene - 5 mg.

The technology for the production of soft gelatin capsules is described, for example, in the manual https://nauchforum.ru/journal/stud/64/49384

Accepted simultaneously with the first component.

The third product (BMI-XS 3) is a dry red pepper extract standardized for capsaicin with a capsaicin content of 1 to 200 mg.

The extract can be obtained by water extraction of crushed fruits or seeds, followed by freezing using a cryogenic freezer and grinding using a freeze dryer (KR 20190089447 (A), 2019-07-31). This component of the BMI-XS complex can be produced, for example, in the form of a hard gelatin capsule.

Mechanism of action: activates the sympathetic nervous system, enhances lipid metabolism and activates thermogenesis, promotes the conversion of white fat into brown. It accelerates the onset and prolongs the feeling of fullness, which reduces the need for food. Reduces body fat in the abdomen and thighs. The product may also be in the form of tablets, simple or coated tablets.

The kit includes standardized extracts, that is, containing a guaranteed and quantitatively determined amount of active substances. Standardization includes a special quality control process at each stage of extract production and mainly chemical analysis using reliable analysis techniques (mainly various chromatography techniques).

Technical result:

The present complex is aimed at optimizing the functioning of the appetite control system, energy metabolism and fat formation: intestinal enzymes, the process of absorption of fats, control of fluctuations in glucose concentration, the signaling system of the brain, controlling hunger / satiety, formation and breakdown of brown and white fat.

The complex more effectively helps to reduce appetite, a long period of satiety after eating, reduce cravings for sweets. It facilitates calorie control, tones the body, stimulating physical activity.

Only the intake of the first component of the effect set cannot be, since thylakoids will be inactive. When taking only the second component of the effect, there can be no effect, since the substances necessary to achieve the expected effect will not be introduced into the body.

If you take only the BMI-XS1 and BMI-XS2 complex without the BMI-XS3 composition, the effect will not be complete, since the "fat burning" system will not be activated, since the latter is aimed at enhancing lipid metabolism, and the former at reducing lipid uptake.

A method of appetite control is the oral administration of the components of the kit (set) 2 or 3 times a day before or during and after meals: before or during meals, a combination of BMI-XS 1 components and a capsule with BMI-XS 2 oil are drunk, and after eating BMI-XS 3.

The preferred regimen for taking the BMI-XS-2 kit is once a day:

1 reception: before or during a meal in the morning, the composition BMI-XS-1 (in the form of a sachet, capsule, tablet or gel) and an additional capsule with BMI-XS-2 oils. After eating in the morning, 1 capsule or tablet of the composition BMI-XS-3.

2 doses: before meals or during meals in the afternoon (for example, lunch or afternoon snack) BMI-XS-1 (in the form of a sachet, capsule, tablet or gel) and an additional capsule with BMI-XS-2 oils. After a meal in the afternoon (for example, lunch or afternoon snack), 1 capsule or tablet of the composition BMI-XS-3.

The invention can be illustrated by the following examples.

Example 1

Male 42 years old, programmer, height 180 cm, weight 95 kg. Leads a sedentary lifestyle. Five years ago I bought a car, now I go to work by car. Over the past 4 years, he gained 10 kg, in connection with which the current BMI is 29, waist - 103 cm, the ratio of waist to height - 0.57. Glucose, cholesterol are normal, triglycerides are moderately elevated, otherwise the blood count is normal. He has no chronic diseases. I began to pay attention that even with a little physical exertion, shortness of breath appears, it is difficult to perform some routine actions (for example, tying shoelaces on boots). He decided to limit the use of sweet and starchy foods, but followed the decision for about a week. He began to take BMI-XS: before eating in the morning, the composition BMI-XS-1 in the form of a sachet and a capsule with BMI-XS-2 oils. After a meal in the morning, 1 capsule with the composition BMI-XS-3. In the first two days, the appetite decreased sharply, then returned to its normal level, but noticed that it practically did not want to eat sweets, it was much easier to refuse flour and to observe the correct diet. He began to walk more: he walked 2 times a week for 20 minutes. After 1 month, the weight decreased by 6 kg, BMI - 27, the waist volume decreased by 4 cm (99 cm, the ratio of waist to height - 0.55). He noted that he feels awake, shortness of breath during physical exertion disappeared, he became much less tired at work. Continues to take BMI-XS.

Example 2

Woman 32 years old, manager, height 172 cm, weight 95 kg, BMI - 32, waist 104 cm, the ratio of waist to height 0.60. It eats irregularly, often follows strict diets, but never manages to "hold out" for more than 10 days. Several times I lost 3-4 kg during the diet, but then the weight quickly recovered, and often added 2-3 kg. Every time, seeing that the weight is growing, he feels despair. Periodically attends classes in fitness clubs, for the first two or three times drives himself to exhaustion, then gives up physical exercises in general. In the indicators of blood tests, there is a moderate increase in triglycerides and a slight increase in fasting glucose, there is a violation of glucose tolerance. I began to take BMI-XS: before meals in the morning, the composition BMI-XS-1 in capsule form and an additional capsule with BMI-XS-2 oils. After eating in the morning, 1 capsule of the composition BMI-XS-3. Starting from the first days of admission, she noted that it became easier to control appetite, the portions of food that cause satiety decreased, easily rejected sweets. After a week, I gave myself a little physical exertion (I rode a bicycle for 30 minutes a day), my mood improved significantly, and stopped weighing daily. After a month of taking BMI-XS, the weight decreased by 5 kg, the waist volume decreased to 99. The blood counts returned to normal. Overall well-being has improved significantly, a belief has appeared that can cope with the problem of weight. Continues to take BMI-XS and lead a healthy lifestyle.

Example 3

A man of 36 years, a sociologist, height 169 cm, weight 95 kg, BMI - 33, waist - 110 cm, the ratio of waist to height 0.65. Leads an active lifestyle, communicates a lot with people, the regime of the day is chaotic, and the diet is extremely irregular. He was always inclined to be overweight, but after stress 4 years ago he began to quickly gain weight. He attributed this to the fact that he began to experience insurmountable hunger at night, woke up from this feeling, ate a large amount of food and only after that could fall asleep, in the morning and the whole first half of the day, the food was disgusting. Currently, she feels constant fatigue, gets tired even from insignificant physical activity, it has become difficult to concentrate, she is almost constantly experiencing unreasonable anxiety. The sleep is restless, superficial, often nightmare dreams. Blood counts show a moderate increase in triglycerides. I began to take BMI-XS: at lunch, BMI-XS-1 in the form of a gel and a capsule with BMI-XS-2 oils. After a meal, 1 capsule of BMI-XS-3. In the first four days I did not notice a change in diet, then I got the feeling that night hunger had decreased, I could tolerate it, I had breakfast with pleasure in the morning. By the end of the third week, sleep became calmer, there were no nightmares. At the end of the month, the diet began to approach regular, episodes of nocturnal food intake were sporadic. Fatigue disappeared, anxiety decreased significantly. Weight decreased slightly (2 kg), but there was confidence that he could control his diet. Continues to take BMI-XS.

Example 4

Woman 46 years old, housewife, height 165 cm, weight 78 kg, BMI - 29, waist -90 cm, the ratio of waist to height - 0.54. I was always slender, but 1 year ago I tried to quit smoking several times (I smoked 20 cigarettes a day from 20 years old), I didn’t smoke for the last time for 4 months, during that time I gained 7 kg, my appetite increased sharply, almost constantly chewed something to soften cravings for nicotine. The indicators of blood tests unchanged. I began to take BMI-XS: before meals in the afternoon, before an afternoon snack, BMI-XS-1 in the form of a sachet and a capsule with BMI-XS-2 oils. After eating, 1 tablet of the composition BMI-XS-3.

During the first week, appetite decreased, although she continued to have a snack between meals. Two weeks later, I noticed that the craving for nicotine was significantly reduced, and I had to snack less often. By the end of the month, snacking episodes became sporadic, craving for nicotine was negligible. Continues to take BMI-XS.

In total, a study to determine the effect of the claimed complex on weight loss and on appetite was conducted on 46 volunteers - 35 women and 11 overweight men. The study showed that taking the claimed complex had a beneficial effect on weight, BMI, and appetite. The feeling of fullness was maintained for a longer time than in the control group that took only BMI-XS-1.

Claims (14)

1. A kit to reduce appetite and normalize weight, characterized in that it includes three products for oral administration, where the first product is a complex of biologically active substances in the form of a unit dosage form containing: - thylakoids from 1000 to 20,000 mg, - dry extract of bitter orange fruits, standardized for p-synephrine, with a content of p-synephrine from 0.5 to 200 mg per form, the second specified product is a soft capsule containing: - olive oil from 10 to 500 mg; - ginger oil from 5 to 200 mg; - D-limonene from 1 to 200 mg, and the third product in a unit dosage form contains dry capsicum standardized red pepper extract with a capsaicin content of 1 to 200 mg per form. 2. The kit according to claim 1, characterized in that the first specified product further comprises: - dry extract of kudzu roots from 0.5 to 500 mg; - dry extract of black tea, standardized for caffeine, with a caffeine content of from 0.5 to 200 mg per form; - dry extract of green tea, standardized for L-theanine, with an L-theanine content of 0.5 to 200 mg per form, and for catechins, with a catechin content of 0.5 to 200 mg per form; - Ceylon cinnamon extract standardized for phenolic acids with a phenolic acid content of 0.5 to 500 mg per form. 3. A method of controlling appetite and normalizing body weight, characterized in that the products of the kit according to claim 1 or 2 are taken orally 2 or 3 times a day, where the first and second products of the kit are taken simultaneously before or during meals, and after meals third set product.