RU2377009C1 - Weight-producing biologically active additive - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to compounds of weight-producing biologically active additives (BAA) in obesity by regulating carbohydrate metabolism in an organism, slowing-down carbohydrate absorption and suppressing appetite by imitating glucose action in blood. Said BAA contains the following components, wt: gamboge extract 100-200; fucus 50-150; gymnema extract 25-75; hoodia extract 25-75; Bromelain 10-30; succinic acid 10-30; papain 10-20; pyridoxine hydrochloride 0.5-1.5; riboflavin 0.45-1.35; thiamine mononitrate 0.5-1.0; chrome picolinate 0.1-0.3; potassium iodate 0.07-0.08; sodium molibdate 2H₂O 0.02-0.04; ammonium vanadate 0.02-0.026; an excipient - the rest up to 510.

EFFECT: normalised metabolic processes with simultaneous decrease of blood cholesterol.

3 tbl

Description

The invention relates to compositions of biologically active additives (BAA) that contribute to weight loss in obesity by regulating carbohydrate metabolism in the body, slowing down the absorption of carbohydrates and reducing appetite, simulating the effect of glucose in the blood.

The patent literature discloses many plant-based products used to reduce body weight in obesity.

From the patent RU 2271724, an amine microelement complex is known containing a dry extract of green tea, a dry extract of wheat and a dry extract of soy, which allows for the cleansing of the body and weight loss.

From patent RU 2316973 there is known a composition for preparing a slimming drink (fat-burning complex) containing, wt.%: Bromelain 2.0-4.0, chromium picolinate 0.0005-0.004, Garcinia Cambogia extract 0.2-0.35, L β-carnitine 1.5-3.0, cinnamon 0.1-0.6, turmeric 0.1-0.6, cardamom 0.1-0.6, ginger 0.1-0.6, ascorbic acid 1, 5-3.0, pectin 0.4-0.8. The invention allows to reduce body weight by 3-10% while providing the body with useful substances.

The closest composition of dietary supplements is disclosed in the application RU 2005130688. The known composition of dietary supplements is intended for persons controlling body weight, and contains the following components per tablet weighing 0.5 g, mg:

Jimnem Sylvester 20.0-30.0 Garcinia Cambogia (extract) 100.0-150.0 Rhodiola rosea (root) 20.0-30.0 Willow (bark extract) 10.0-15.0 Raspberry (leaf extract) 10.0-15.0 Lingonberry (leaf) 20.0-30.0 Blueberries (shoots) 20.0-30.0

Birch (leaf) 20.0-30.0 Hairbrush (grass) 20.0-30.0 Nettle (leaf) 20.0-30.0 Horsetail field (grass) 20.0-30.0 Highlander bird (grass) 20.0-30.0 Elecampane (root) 10.0-15.0 St. John's wort (grass) 10.0-15.0 Potassium iodate 0.010-0.015 Chromium Picolinate 0.010-0.015 Vitamin B ₆ 0.20-0.25 L-carnitine 4.0-6.0 Potassium chloride 5.0-7.5 Magnesium oxide 5.0-7.5 Vitamin C 20.0-30.0 L-glutamic acid 20.0-30.0 Excipients (starch / talc) Rest

The objective of the invention is to obtain a dietary supplement that effectively helps reduce body weight by regulating carbohydrate metabolism in the body, slowing down the absorption of carbohydrates and reducing appetite, simulating the effect of glucose in the blood, while reducing blood cholesterol, normalizing metabolic processes.

The problem is solved by the composition of dietary supplements containing garcinia extract, gimnema extract, pyridoxine hydrochloride, chromium picolinate, potassium iodate and a filler, in accordance with which it additionally contains fucus, hoodia extract, bromelain, succinic acid, papain, riboflavin, thiamine mononitrate and vanadium ammonium in the following ratio of components in wt. hours:

Garcinia Extract 100-200 Fucus 50-150 Gymnema Extract 25-75 Hoodia extract 25-75 Bromelain 10-30 succinic acid 10-30 Papain 10-20 Pyridoxine hydrochloride 0.5-1.5 Riboflavin 0.45-1.35 Thiamine mononitrate 0.5-1.0 Chromium Picolinate 0.1-0.3 Potassium iodate 0.07-0.08 Sodium molybdate · 2H ₂ O 0.02-0.04 Ammonium Vanadium Acid 0.02-0.026 Filler The rest is up to 510

As a filler, any suitable filler can be used, for example, a mixture of the following substances: lactose, lecithin, talc, calcium stearate, dye iron oxide black.

The invention consists in the following.

The composition of the claimed additives, called "Complex HB 3", is intended to regulate carbohydrate metabolism in the body and slow down the absorption of carbohydrates. The components of the complex are able to reduce appetite by imitating the effect of glucose in the blood, so HB 3 is taken 30 minutes before meals.

The complex of HB 3 includes garcinia cambogia extract (Garcinia cambogia - Garcinia cambogia). The hydroxycitric acid (GOTs-citrine) contained in it provides a triple biochemical mechanism of physiological weight loss in the human body:

- reduces the formation of fatty acids and cholesterol;

- enhances the oxidation of fat present in adipocytes;

- regulates appetite.

The biochemical mechanism of this process is as follows: having a similar structure with citric acid, which is formed in the cells of our body, inhibits the activity of the enzyme citratlidase and thereby competitively inhibits the formation of acetyl-CoA, which, in turn, limits the further synthesis of fatty acids through malonyl CoA. At the same time, under the influence of GOTs-citrine, the carnitine acyltransferase enzyme is activated, due to which the formation of carnitine is activated and, accordingly, the transport of intracellular fatty acids in mitochondria and their oxidation in these subcellular formations are enhanced. The regulatory effect of GOTs-citrine on appetite is its indirect effect on the activity of hypothalamic neurons, which are responsible for hunger and satiety. By blocking the formation of fatty acids from carbohydrates, it maintains a concentration of glucose at which the hypothalamic neurons do not stimulate appetite.

The combination of hydroxycitric acid (GLA) with chromium picolinate gives an even greater effect, since chromium reduces appetite and, most importantly, suppresses cravings for sweet and flour foods. GLA and chromium together block the synthesis of fats, prevent the formation of excess cholesterol, improve metabolism and increase the energy balance of the body. Blocking the formation of adipose tissue leads to the burning of accumulated body fat. Chromium helps to normalize blood sugar, as it is a Co-factor of insulin. The activation of the metabolic process to a level that ensures intensive burning of fats, and the normalization of the functions of the hormonal system provides the right balance of GLA and chromium with iodine.

Fucus (Fucus finely bubbly - Fucus vesiculosus). Fucus contains a balanced set of chemical elements of organic nature. Fucus is one of the richest sources of iodine, it contains various polysaccharides (alginates, kelp, fucoidan, polyphenols and beckons).

Fucus active substances optimize thyroid function and metabolic processes in the body. Reduced thyroid function, impaired metabolism and an imbalance of sex hormones are causes of overweight. The components of brown algae are polysaccharides: alginates, laminarin, fucoidan favorably affect metabolic processes. Alginates are traps for water and ions. They are able to bind and excrete salts of heavy metals, radionuclides, regulate water-salt metabolism and plasma cholesterol. Swelling in the stomach, alginates normalize the digestion process, cleanse the intestines, cause a feeling of satiety.

Gimnema extract (Gymnema sylvestre - Gymnema sylvestre), which is part of HB 3, contains gimnemic acids. Gimnemic acid blocks the absorption of sugar in the digestive tract, regulates appetite, has a beneficial effect on insulin synthesis (gimnemic acid helps to restore pancreatic cells that produce insulin).

Gimnema extract is in the HB 3 complex in the form of phytosomes in order to increase the safety and bioavailability of the active components.

To obtain the phytosomal form, advanced technologies and experience have been used that allow you to save phytosomes with gymnema for a long time. The presence of undamaged phytosomes in a liquid medium with a pH similar to the contents of the intestine was proved in vitro using microscopy. The best preservation of the phytosomal form in comparison with a monoextract was proved by studying the hygroscopicity of these substances.

The composition of HB 3 includes hoodia extract (Hoodia - Hoodia Gordonii), which contains active components belonging to the group of steroid glycosides (triterpenoids). The main active component of the hoodia extract, called P-57, belonging to this group of compounds, was isolated. Hoodia extract contains polysaccharides, organic acids, minerals.

Hoodia extract effectively regulates appetite, since P-57 directly affects the hypothalamic structures of the brain, sending a signal about an adequate glucose level, which leads to a decrease in hunger, and the body switches to burning fat reserves to generate energy, and the person loses weight.

The HB 3 complex contains proteolytic and lipolytic enzymes:

1. Bromelain is a proteolytic, fat-burning enzyme isolated from pineapple. This is a powerful catalyst for the most important processes of carbohydrate and protein metabolism, contributes to the rapid breakdown of fats and their removal from the body. By splitting fats, bromelain prevents the formation of subcutaneous fat accumulations, an increase in blood fat. In this case, fat deposits are destroyed much faster. Bromelain increases enzymatic activity, helps in reducing the level of enzymes in the digestive juices, cleanses the body of toxins and toxins, improves digestion.

2. Papain is a plant proteolytic enzyme that helps normalize digestion. The papain enzyme metabolizes proteins to amino acids. Due to this, it prevents the subsidence of undigested food residues on the walls of the intestine. As a result of normalization of digestion, the body does not put off fat in the "problem areas". The enzyme is active in any part of the gastrointestinal tract.

The HB 3 complex contains trace elements - vanadium and molybdenum. They are co-factors of various enzymes. These trace elements, together with B vitamins, are involved in the exchange of glucose and other carbohydrates.

The composition of the HB 3 complex includes B vitamins (thiamine, riboflavin, pyridoxine). They act as cofactors of enzymes that catalyze carbohydrate metabolism.

Vitamin B1 (thiamine) is a water-soluble vitamin. The phosphorylated form of thiamine - thiamine pyrophosphate - is formed in the human body and is a precursor of enzymes that play a significant role in the metabolism of carbohydrates and, in particular, in the decarboxylation of pyruvic acid, keto acids.

Vitamin B1 is necessary for the oxidative decarboxylation of keto acids (pyruvic and lactic), the synthesis of acetylcholine, it is involved in carbohydrate metabolism and the associated energy, fat, protein, water-salt metabolism, and has a regulatory effect on trophism and the activity of the nervous system. With insufficient intake of thiamine, carbohydrate metabolism is disrupted, pyruvic acid and lactic acid accumulate in the tissues, the synthesis of acetylcholine is impaired, as a result of which the functions of a number of systems, primarily the nervous, cardiovascular and digestive ones, deteriorate.

Thiamine improves blood circulation and is involved in hematopoiesis. Thiamine optimizes cognitive activity and brain function. It has a positive effect on energy levels, growth, normal appetite, learning ability and is necessary for the tone of the muscles of the digestive tract, stomach and heart. Thiamine acts as an antioxidant, protecting the body from the damaging effects of aging, alcohol and tobacco.

Indications for the use of thiamine are metabolic disorders and diseases of the endocrine system (thyrotoxicosis, diabetes mellitus, obesity).

Vitamin B2 (riboflavin). The biologically active form of riboflavin is flavin adenine dinucleotide, which is synthesized in the human body in the kidneys, liver and other tissues. Another derivative of riboflavin is riboflavin-5-phosphoric acid. Thanks to them, the normal course of redox processes in the body is ensured.

Vitamin B2 intensifies metabolic processes, participating in the metabolism of proteins, fats and carbohydrates. Riboflavin is necessary for the formation of red blood cells and antibodies, for cell respiration and growth. It facilitates the absorption of oxygen by the cells of the skin, nails and hair. Vitamin B2 improves the condition of the organ of vision, taking, along with vitamin A, participation in the processes of dark adaptation, reduces eye fatigue and plays a big role in preventing cataracts. Riboflavin has a positive effect on the mucous membranes of the digestive tract, minimizing the negative effects of various toxins on the respiratory tract. It is necessary for the metabolism of tryptophan, which is converted into niacin in the body.

One of the most valuable qualities of riboflavin is its ability to accelerate the conversion of pyridoxine - vitamin B6 - into its active form in the body, promoting the absorption of pyridoxine.

The need for riboflavin increases with increased physical exertion, as well as when taking oral contraceptives. The systematic use of alcohol deforms the mechanism of assimilation of vitamin B2, therefore, in individuals who abuse alcohol, the need for riboflavin is increased.

Vitamin B6 (pyridoxine). The activity of vitamin B6 is possessed by a group of compounds derived from pyridine (pyridoxine (pyridoxol), pyridoxal and pyridoxamine), united under the general name "pyridoxine".

Vitamin B6 plays an important role in the metabolism, is necessary for the normal functioning of the central and peripheral nervous system, and is involved in the synthesis of neurotransmitters. In phosphorylated form it provides processes of decarboxylation, transamination, deamination of amino acids, participates in the synthesis of protein, enzymes, hemoglobin, prostaglandins, metabolism of serotonin, catecholamines, glutamic acid, GABA, histamine, improves the use of unsaturated fatty acids, reduces cholesterol and lipids in the blood, improves myocardial contractility, promotes the conversion of folic acid into its active form, stimulates hematopoiesis.

With atherosclerosis, vitamin B6 improves lipid metabolism.

The need for pyridoxine increases with antidepressants and oral contraceptives, during stress and increased stress, as well as in people who consume alcohol and smokers.

Elevated levels of tryptophan, methionine, cysteine rich proteins, and intestinal infections also increase the need for pyridoxine.

There is evidence of the effectiveness of pyridoxine in atherosclerosis and diabetes mellitus (reduces the content of glycosylated hemoglobin), in addition, pyridoxine acts as a diuretic, helping to reduce high blood pressure, thereby protecting the cardiovascular system in several ways at once.

In a number of studies, pyridoxine has been shown to be effective in depression: it has a positive effect on the production of norepinephrine and serotonin.

The composition of the HB 3 complex includes succinic acid. Succinic acid is a natural substance (present in all organisms). It activates energy metabolism in the tissues, promotes the production of ATP (adenosine triphosphate), the main substance in the body that gives energy. Enhanced energy metabolism makes body cells less sensitive to glucose deficiency, which is especially important in the complex program for weight correction. Succinic acid stimulates many functions of the body, has exceptional regenerative power. Succinic acid enhances cellular respiration, promotes the absorption of oxygen by cells, tissues, organs. Neutralizes free radicals.

Thus, succinic acid is a stimulator of energy metabolism and a link in the chain of reactions for producing ATP. It enters the chain of citrate cycle reactions in the form of succinate and increases the overall metabolism.

The overall balance of the citrate cycle is that 2CO ₂ , 3 NADH + H ⁺ and one molecule of reduced ubiquinone (QH ₂ ) are formed from one acetyl residue. In this case, due to the reduced forms of coenzymes by oxidative phosphorylation, 9 are synthesized in the cell, and 10 ATP molecules are synthesized taking into account the transformation of one GTP molecule.

The filler for the inventive dietary supplement can be any acceptable filler that allows you to preserve the tablet form of the dietary supplement, for example, the filler may contain a mixture containing lactose, lecithin, talc, calcium stearate, dye iron oxide black, etc.

The enclosed dietary supplement is made as follows.

The technological scheme of manufacturing dietary supplements includes the preparation of raw materials; preparation of a mixture for encapsulation: dosing, sieving and mixing of raw materials; encapsulation and dust removal; department in terms of product appearance; packing, packaging and labeling.

Dosing of the components is carried out in the following sequence: garcinia extract 50%, fucus, liposomal mass with gimnema extract (2 parts by weight of extract and 1 parts by weight of lecithin), hoodia, bromelain 2400 GDU, succinic acid, papain.

Pyridoxine hydrochloride, riboflavin and thiamine mononitrate are pre-mixed separately with part of the lactose and sieved.

Chromium picolinate, potassium iodate, sodium molybdate · 2H ₂ O and ammonium vanadium are pre-ground in a mortar with lactose, then mixed with part of the lactose. Then, lactose, talc and calcium stearate are dosed. Black iron oxide dye (Spectracol) is pre-mixed with a five-fold amount of the already prepared mixture, sieved, ground and introduced into the total mixture.

The resulting mixture is sieved on a vibrating screen with a hole diameter of 1 mm and mixed in a V-shaped mixer. The mixture should be homogeneous, free from lumps and impurities. The mixture is encapsulated in 0.510 g and dedusted.

Table 1 shows examples of the compositions of the proposed dietary supplement.

Table 1 No. Name of components Content, mg per 1 tablet 0.510 g Composition 1 Composition 2 Composition 3 Garcinia extract 50% 150 one hundred one Hydroxycitric Acid 75 200 Fucus one hundred 150 2 Iodine content 0,03 fifty 3 Gimnema extract 25% fifty 75 Gimnemic Acid 12.5 25 Lean extract fifty 25 four Triterpene Saponins 0.1 75 5 Bromelain 2400 GDU twenty thirty 10 6 succinic acid twenty 10 thirty 7 Papain fifteen 10 twenty 8 Pyridoxine hydrochloride one 1,5 0.5 9 Riboflavin 0.9 1.35 0.45 10 Thiamine mononitrate 0.75 0.5 1,0 Chromium Picolinate 0.2 0.3 eleven Chromium 0,025 0.1 12 Potassium iodate 0,076 0,07 0.08 Iodine 0,045 13 Sodium molybdate · 2H ₂ O 0,03 0.04 0.02 Molybdenum 0.012 fourteen Ammonium Vanadium Acid 0,023 0.02 Vanadium 0.01 0,026 fifteen Lactose 47,021 57.22 35,824 16 Talc fifteen 10 twenty 17 Calcium stearate 5 3 8 eighteen Lecithin 25 thirty twenty 19 Dye Iron Oxide Black 10 7 fifteen

The proposed dietary supplement - the “NV 3” complex - was developed for use in the weight correction program “HR END CONTROL” (HELS AND BODY CONTROL) - “Н & В CONTROL” (HEALTH & BODI CONTROL) manufactured by LLC Artlife, Tomsk, which consists of five separate complexes, each of which has its own focus, and together they have a multicomponent effect on the body.

The aim of the study was to determine the effect of the Weight & Body Control weight correction program, including each of the complexes, on the anthropometric, laboratory and clinical parameters of patients with varying degrees of obesity.

Under observation were 20 patients with obesity of varying degrees. Of these, 8 men (40%) and 12 women (60%). The average age of the patients was 41.2 ± 2.0 years (from 27 to 61 years). The age of men is from 27 to 52 years, the average is 39.75 ± 2.7 years. The age of women is from 28 to 61 years, the average is 42.2 ± 2.9 years.

HSBC 3 (Health & Body Control) - HB 3 (Health & Body control) - take 1 capsule during breakfast and afternoon snack. The recommended time of admission is 8-10 hours in the morning and 17 hours of the day.

As a result of taking the weight control program of the intake of “H & B Control” (Health & Body control) in combination with diet therapy (for 3-4 weeks the patient was offered a low-calorie diet in accordance with standard diets) in patients with obesity, a positive dynamics was revealed by anthropometric, clinical and laboratory indicators.

A study of the dynamics of body weight in patients over a 45-day course of the program did not reveal significant differences in the indicators, but there was a persistent tendency to decrease in body weight in all patients (in 100% of cases). In 70% of patients, weight loss was more than 2.6 kg. The average decrease in body weight was 3.65 kg, the maximum decrease in body weight was 10 kg.

The direction of the impact of the proposed dietary supplement HBC 3 (Health & Body Control) - HB 3 (Health & Body control) on the regulation of carbohydrate metabolism illustrates a decrease in the average group index of glucose in the blood of patients from 5.3 to 5.0 mmol / l (table 2 )

table 2 Estimated indicator Average The significance level of differences, Wilcoxon test Before the beginning After programs graduation programs Glucose, mmol / L 5.3 ± 0.08 5.0 ± 0.08 0.05

According to the identified tendency to decrease the level of blood triglycerides in patients and a significant decrease in total cholesterol in subjects before and after taking the program “HR & B Control” (Health & Body control), a month and a half course allows us to begin to normalize the change in the main links of metabolic regulation, the violation of which lies in basis of obesity and metabolic syndrome (table 3).

Table 3 Estimated indicator Average The significance level of differences, Wilcoxon test Prior to the program After the end of the program Total cholesterol, mol / l 5.8 ± 0.14 5.6 ± 0.15 = 0.05 Triglycerides, μmol / L 1.1 ± 0.04 1.0 ± 0.03 > 0.05

Claims (1)

A weight loss dietary supplement containing garcinia extract, gimnema extract, pyridoxine hydrochloride, chromium picolinate, potassium iodate and an excipient, characterized in that it additionally contains fucus, hoodia extract, bromelain, succinic acid, papain, riboflavonite, thiamine , sodium molybdate 2H ₂ O and vanadium ammonium in the following components in parts by weight:
garcinia extract 100-200 fucus 50-150 gimnema extract 25-75 hoodia extract 25-75 bromelain 10-30 succinic acid 10-30 papain 10-20 pyridoxine hydrochloride 0.5-1.5 riboflavin 0.45-1.35 thiamine mononitrate 0.5-1.0 chromium picolinate 0.1-0.3 potassium iodate 0.07-0.08 sodium molybdate 2H ₂ O 0.02-0.04 vanadium acid ammonium 0.02-0.026 filler the rest is up to 510