RU2721605C1 - Pharmaceutical composition for parenteral drop introduction - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to medicine and concerns a pharmaceutical composition for parenteral drop introduction intended for treating obesity.

EFFECT: well-chosen, balanced qualitative and quantitative composition provides creation of a dosage form suitable for effective body weight index reduction in a short period of time.

1 cl, 4 ex

Description

The invention relates to medicine and relates to a pharmaceutical composition for parenteral drip intended for the treatment of obesity.

The problem of obesity is global. According to recent data, about two billion people worldwide are overweight or obese. This is about 30% of the world's population.

Since 1980, obesity has doubled in 70 countries, and in many countries, childhood obesity has grown faster than among adults. The obesity epidemic is driven by many factors, including increased access to fast food, increased serving sizes, and a sedentary lifestyle.

The problem of obesity is associated with a decrease in the quality and overall life expectancy due to the frequent development of severe concomitant diseases. These include: type 2 diabetes mellitus, arterial hypertension, dyslipidemia, atherosclerosis and related diseases, reproductive dysfunction, gallstone disease, osteochondrosis.

The fight against excess weight, especially with arterial hypertension, is of great importance. In modern clinical practice, various approaches to the treatment of obesity are used, including psychotherapy, diets, pharmacotherapy, surgical treatment, physiotherapy exercises, etc. There are a large number of drugs that can reduce excess body weight, but to date, only sibutramine, orlistat and phentermine are officially recommended for the treatment of obesity as a means of choice.

It was unexpectedly discovered that it is possible to help the body in the fight against overweight by filling up the deficiency of vitamins and nutrients.

One of the ways to deliver bioactive substances to the human body is through intravenous infusion (dropper). Parenteral administration of medical solutions directly into the bloodstream, bypassing the gastrointestinal tract, provides several advantages, the main of which is the rapid and complete assimilation of nutrient and therapeutic substances from solutions. Oral supplements have less bioavailability due to the breakdown and loss of nutrients in the gastrointestinal tract. Active substances must first break down in the stomach, then must reach the small intestine to be absorbed, then metabolized by the liver, and then finally delivered to the tissue for use. During this process, many substances can be metabolized quite strongly, with only minimal amounts actually reaching the target tissue.

Infusion therapy is prescribed in all cases when local administration of the drug is necessary, quick correction of the state of the body or maintenance of its vital activity for a long time. The necessary quantities of drugs enter directly into the bloodstream, quickly get involved in metabolic processes and at the same time have minimal side effects, do not irritate the gastrointestinal mucosa.

Thus, the aim of the present invention is to provide an effective and safe dosage form for parenteral drip, with a clearly selected composition of vitamins and nutrients for the treatment of obesity.

The technical result consists in expanding the arsenal of funds for this purpose by creating a highly effective and fast-acting pharmaceutical composition for parenteral drip, which can be used in obesity.

The object of the present invention is a pharmaceutical

a composition for parenteral drip intended for the treatment of obesity, characterized in that it contains a complex of active substances, in the following ratio of components:

D-galactose 500 mg L-carnitine 500 mg L-Taurine 500 mg L-Ornithine Aspartate 250 mg L-methionine 192 mg L-tryptophan 64 mg L-Leucine 218 mg L-isoleucine 192 mg L-phenylalanine 128 mg L-Arginine Hydrochloride 200 mg L-lysine hydrochloride 241 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-glutamine 750 mg L-glycine 298 mg L-carnosine 102 mg N-L-Acetyl-L-Cysteine 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Hydroxocobalamin 500 mcg Sodium Chloride 0.9% or Distilled Water Up to 500 ml

The composition is selected in accordance with the objectives of the invention. Galactose is a member of the simple milk sugar class. It is an integral part of glycolipids and glycoproteins. Prevents diseases of the nervous system, regulates the functioning of the digestive organs, is important for creating cell membranes.

L-carnitine is a dipeptide consisting of two other essential amino acids: L-methionine and L-lysine. Promotes energy production and breakdown of fat. Helps maintain overall health by promoting the transfer of fatty acid groups to the mitochondrial membrane in order to produce cellular energy.

Taurine is a semi-essential amino acid that plays the role of a lipid / membrane stabilizer and supports various antioxidant defense systems of the body. The beneficial properties of taurine are mainly manifested as a result of interaction with other substances present in the body, while its direct effect is observed only at the cellular level. Taurine is widely studied as an antidiabetic agent due to its effect on organs usually affected by diabetics (kidneys, eyesight, nervous system), and as a means of controlling blood sugar levels, reducing some forms of foreign insulin resistance.

Ornithine is an essential amino acid that is an important mediator in the urea production cycle, interacting with arginine and citrulline to free the body of ammonia, a byproduct of protein metabolism. Ornithine is converted to arginine, so it helps maintain normal levels of arginine in the body. Ornithine can also be converted to other amino acids, such as citrulline, proline and glutamate, as well as creatine, an important source of muscle energy.

A complex of 8 essential amino acids (L-methionine, L-leucine, L-isoleucine, L-phenylalanine, L-lysine, L-threonine, L-valine and L-histidine), which are involved in the formation of protein - the main building block of the body, collagen and elastin, contribute to the restoration of the skin and bone tissue and the rapid healing of wounds.

L-tryptophan is an essential amino acid, plays a critical role in the production of serotonin and melatonin, which support good mood, healthy sleep and the functioning of the immune system.

L-arginine is a conditionally essential amino acid, which is mainly involved in the metabolism and excretion of urea, as well as in the synthesis of DNA and protein. It is an important precursor of nitric oxide, which also plays a role in the expansion of blood vessels.

L-glutamine is a conditionally essential amino acid, the largest amount of which is in human muscle tissue. In the body, glutamine acts as the main carrier of nitrogen and is critical for maintaining a normal nitrogen balance. It provides a normal nitrogen balance. Helps maintain muscle strength as well as the health of the gastrointestinal tract and immune system.

Glycine is the smallest and simplest amino acid, which due to its properties is widely used for various purposes. Glycine is essential for the production of glutathione, DNA, creatine, bile, hemoglobin and most proteins. In addition, it contributes to the deposition of glycogen, thus creating more glucose for energy production. Glycine also plays the role of a calming neurotransmitter in the brain, providing transmission of nerve impulses. In addition, it is necessary to maintain normal sleep phases.

L-carnosine is a dipeptide found in the brain, heart, skin, muscles, kidneys and stomach that supports healthy aging and cell rejuvenation. L-carnosine optimizes the normal functioning of cells and fights against aging, neutralizing the activity of free radicals, thus acting as an antioxidant and acting, in particular, in the brain and nerve cells.

N-L-acetyl-L-cysteine is a stable form of L-cysteine. Sulfur-containing amino acid, which acts as a stabilizer in the formation of protein structures, as well as necessary for the formation of glutathione.

Flavin adenine dinucleotide is a coenzyme that takes part in many redox biochemical processes. Formed from riboflavin.

Nicotinamide adenine dinucleotide phosphate is a naturally occurring coenzyme of certain dehydrogenases, enzymes that catalyze redox reactions in living cells.

Hydroxocobalamin is the second most common form of vitamin B ₁₂ found in the blood. It is one of the forms that can be converted by the body into an active form. Also, it is hydroxocobalamin that is the most common form of B ₁₂ in natural products.

Sodium chloride 0.9% and distilled water are solvents commonly used in the technology of infusion dosage forms.

A clearly selected, balanced qualitative and quantitative composition of the proposed composition provides the creation of a dosage form suitable for the treatment of obesity, allowing for a short time to effectively reduce body mass index.

The proposed composition can be obtained as follows. Each ingredient in the composition is dissolved in 20 ml of sterile water for injection. Then all solutions are mixed and the solvent is added to the resulting mixture to obtain a volume of 500 ml. Thus, a product of the following composition is prepared for use:

D-galactose 500 mg L-carnitine 500 mg L-Taurine 500 mg L-Ornithine Aspartate 250 mg L-methionine 192 mg L-tryptophan 64 mg L-Leucine 218 mg L-isoleucine 192 mg L-phenylalanine 128 mg L-Arginine Hydrochloride 200 mg L-lysine hydrochloride 241 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-glutamine 750 mg L-glycine 298 mg L-carnosine 102 mg N-L-Acetyl-L-Cysteine 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Hydroxocobalamin 500 mcg Sodium Chloride 0.9% or Distilled Water Up to 500 ml

The drug of the present invention is administered to the patient infusion. The number of infusions, their frequency and rate of administration can be appropriately determined by the attending physician taking into account the symptoms of each patient, age and other indicators.

The possibility of carrying out the invention can be illustrated by the following specific examples of implementation.

Example 1

The patient, female, 32 years old. The patient complains of excessive food intake during the working day, an increase in the buttocks, thighs and the appearance of episodic stretch marks on them, as well as the appearance of signs of a second chin, shortness of breath, periodic tachycardia and an increase in blood pressure up to 140/90 mm. Hg, digestive disorders, flatulence, unstable stool, decreased muscle mass. On instrumental examination: body mass index - 33. Diagnosis - Metabolic syndrome, obesity, I degree.

Treatment - the claimed composition was prescribed drip three times a week for two weeks.

2 weeks after the infusion:

Pulse - 60 / min, respiratory rate - 18 / min, temperature 36.8, blood pressure 125/85 mm. Hg

General condition is satisfactory. Body mass index - 25. Symptoms of the metabolic syndrome of obesity are not observed. A slight fat deposition on the buttocks remains. The patient notes the presence of a positive mood, is active throughout the working day, also notes the normalization of appetite and a decrease in the amount of food taken per day.

Example 2

The patient, husband., 35 years old. The patient complains of excessive food intake due to constant stressful situations, an increase in the abdomen as an “apron” and the appearance of stretch marks on it, shortness of breath, periodic tachycardia, heartburn, snoring, decreased muscle mass, joint pain and an occasional increase in blood pressure to 150/90 mm Hg On instrumental examination: body mass index - 32. Diagnosis - Metabolic syndrome, obesity, I degree.

Treatment - the claimed composition was prescribed drip three times a week for two weeks.

2 weeks after the infusion:

Pulse - 66 / min, respiratory rate - 19 / min, temperature 36.7, blood pressure 130/80 mm. Hg

General condition is satisfactory. Body mass index - 26. Symptoms of the metabolic syndrome of obesity are not observed. A slight increase in the abdomen remains. The patient notes the presence of a positive mood, is active throughout the working day, also notes the normalization of appetite and a decrease in the amount of food taken per day.

Example 3

Patient, female, 43 years old. The patient complains of an increase in the amount and volume of food consumed during the day, with difficulty controlling food cravings, an increase in the buttocks, hips and the appearance of strong stretch marks on them, as well as the appearance of pronounced signs of a second chin and pseudo-gynecomastia, shortness of breath, aggravated by physical exertion, periodically expressed tachycardia and increased blood pressure up to 160/100 mm. Hg, digestive disorders, stool disorders, decreased muscle mass, periodic pain in the joints of the lower extremities. On instrumental examination: body mass index - 38. Diagnosis - Metabolic syndrome, obesity, II degree.

Treatment - the claimed composition was prescribed drip three times a week for two weeks.

2 weeks after the infusion:

Pulse - 62 / min, respiratory rate - 21 / min, temperature 36.9, blood pressure 135/85 mm. Hg

General condition is satisfactory. Body mass index - 32. Symptoms of the metabolic syndrome of obesity are much less pronounced. Partial fat deposits remain on the hips and buttocks. The patient notes the presence of a positive mood, is active throughout the working day, also notes the normalization of appetite and a decrease in the number of meals and the amount of food taken per day.

Example 4

Patient, male, 45 years old. The patient complains of an increase in the amount and volume of food consumed during the day, practically uncontrolled craving for food due to constant stressful situations, a significant increase in the abdomen as an “apron” and the appearance of strong stretch marks on it; shortness of breath, intensifying even with slight physical exertion, frequent tachycardia up to 90 beats / min and an increase in blood pressure to 180/150 mm. Hg, severe snoring and attacks of sleep apnea, decreased muscle mass, pain in the joints of the lower extremities. On instrumental examination: body mass index - 39. Diagnosis - Metabolic syndrome, obesity, II degree.

Treatment - the claimed composition was prescribed drip three times a week for two weeks.

2 weeks after the infusion:

Pulse - 68 / min, respiratory rate - 21 / min, temperature 36.4, blood pressure 135/85 mm. Hg

General condition is satisfactory. Body mass index - 34. Symptoms of the metabolic syndrome of obesity are less pronounced. Fat remains in the abdomen. The patient notes the presence of a positive mood, is active throughout the working day, also notes the normalization of appetite and a decrease in the number of meals and the amount of food taken per day.

Thus, the present invention provides a highly effective and fast-acting pharmaceutical composition for parenteral drip, which can be used to treat obesity.

Claims (2)

A pharmaceutical composition for parenteral drip intended for the treatment of obesity, characterized in that it contains a complex of active substances in the following ratio of components: D-galactose                                             500 mg L-carnitine                                             500 mg L-Taurine                                             500 mg L-Ornithine Aspartate                                 250 mg L-methionine                                             192 mg L-tryptophan                                               64 mg L-Leucine                                              218 mg L-isoleucine                                              192 mg L-phenylalanine                                   128 mg L-Arginine Hydrochloride                       200 mg L-lysine hydrochloride                       241 mg L-threonine                                                128 mg L-valine                                                192 mg L-histidine hydrochloride hydrate            100 mg L-glutamine                                                 750 mg L-glycine                                                 298 mg L-carnosine                                                 102 mg N-L-Acetyl-L-Cysteine                         100 mg Flavin adenine sodium dinucleotide  10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Hydroxocobalamin                                    500 mcg Sodium chloride 0.9% or Distilled water                     up to 500 ml