RU2723950C1 - Pharmaceutical composition for parenteral drop introduction - Google Patents

Abstract

FIELD: pharmaceutics.SUBSTANCE: invention relates to the field of the pharmaceutical industry, specifically to a pharmaceutical composition for parenteral drop introduction for use in overexertion under intense loads, characterized by that it contains a complex of active substances in the following ratio of components, mg: sodium flavin adenine dinucleotide 40 mg; nicotinamide adenine dinucleotide phosphate 500 mg; folic acid 15 mg; calcium folinate pentahydrate 50 mg; cyanocobalamin 1 mg; methylcobalamin 500 mcg; glutathione 600–1,200 mg; α-lipoic (thioctic) acid 50 mg; β-D-fructose-1,6-diphosphate 5,000-10,000 mg; N,N-dimethylglycine 300 mg; ascorbic acid 2,000 mg; L-taurine 500 mg; L-carnitine 1,000 mg; inosine 400 mg; magnesium asparaginate 280 mg; potassium asparaginate 320 mg; calcium gluconate 500 mg; dextrose 5 % to 500 ml.EFFECT: invention provides a highly effective dosage form, which can be used in various conditions associated with physical overload and overexertion of separate organs and systems.1 cl, 2 ex

Description

The invention relates to medicine and relates to a pharmaceutical composition for parenteral drip, intended for use in case of overvoltage under intense loads.

Quick recovery is one of the most important problems for any professional athlete who is experiencing strong physical and mental stress.

Currently, many tools are offered to help professional athletes and people who are experiencing physical activity in general, to bear the intense physical stress that they experience during training and competition. Such products contain sugars (for example, sucrose, glucose, dextrose, fructose, maltose, maltodextrin) and are aimed at nourishing the body after loss of energy (or for consumption) during sports. The composition may also include electrolytes corresponding to body salts, which are usually lost during physical exertion, such as sodium, potassium, chlorides and inorganic phosphates. In addition, the formulations can be supplemented with vitamins, in particular vitamin C (ascorbic acid) and vitamin E (α-tocopherol), which act as antioxidants, as well as B vitamins (including B ₁ , B ₆ , etc.) as adjuvants in energy metabolism.

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 a number of advantages, the main of which is the rapid and complete absorption of nutrients 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 where 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, intended for use in case of overstrain under intense loads, including sports.

The technical result consists in expanding the arsenal of funds for this purpose by creating an integrated highly effective pharmaceutical composition for parenteral drip, which can be used in various conditions associated with physical overload and overstrain of individual organs and systems, in conditions requiring speed, endurance and high concentration attention.

The object of the present invention is a pharmaceutical composition for parenteral drip administration for use in case of overstrain under intense loads, characterized in that it contains a complex of active substances in the following ratio of components:

Sodium flavin adenine dinucleotide 40 mg Nicotinamide adenine dinucleotide phosphate 500 mg Folic acid 15 mg Calcium folinate pentahydrate 50 mg Cyanocobalamin 1 mg Methylcobalamin 500 mcg Glutathione 600-1200 mg α-lipoic (thioctic) acid 50 mg

β-D-fructose-1,6-diphosphate 5000-10000 mg

N, N-dimethylglycine 300 mg Vitamin C 2000 mg L-Taurine 500 mg L-carnitine 1000 mg Inosine 400 mg Magnesium asparaginate 280 mg Potassium asparaginate 320 mg Calcium gluconate 500 mg Dextrose 5% up to 500 ml.

The composition is selected in accordance with the objectives of the invention.

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.

Folic acid helps maintain a healthy level of homocysteine in methionine. At the same time, it plays an important role in the functioning of red blood cells and helps to maintain the health of the nervous system.

Calcium folinate is a reduced form of folic acid. In medicine, it is used to neutralize the toxic effects of folic acid antagonists.

Cyanocobalamin is involved in the transfer of metal fragments, the formation of choline, methionine, creatine, nucleic acids, the maturation of red blood cells, and contributes to the accumulation of compounds containing sulfhydryl groups in red blood cells. When cyanocobalamin enters the body, it is converted to methylcobalamin or adenosylcobalamin, which are two active forms of vitamin B ₁₂ in humans. Unlike cyanocobalamin, methylcobalamin is a natural form of vitamin B ₁₂ , which can be obtained from supplements, as well as from foods such as fish, meat, eggs and milk. Hydroxocobalamin is the second most common form 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.

Methylcobalamin is a natural form of vitamin B ₁₂ , a water-soluble nutrient that is necessary for the normal formation of red blood cells and contributes to the normal functioning of the immune system. And, like most B vitamins, it promotes normal energy metabolism, processes that release energy from food.

Glutathione is the most powerful natural antioxidant in all human cells. This tripeptide, consisting of glutamic acid, cysteine and glycine, helps detoxify the body and neutralize free radicals, supporting the immune system. It is known for its role in providing antioxidant protection to body tissues, including arteries, brain, heart, liver, lungs, and skin. Glutathione plays a significant role in the functioning of the body's immune system. Its antioxidant property makes it vital for white blood cells (lymphocytes), as it allows them to realize their potential during the oxygen-containing activity of the body's immune response.

Lipoic acid is a coenzyme involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids, and plays an important role in the energy balance of the body. By the nature of the biochemical action, thioctic acid is similar to B vitamins. It participates in the regulation of lipid and carbohydrate metabolism, has a lipotropic effect, affects cholesterol metabolism, improves liver function, has a detoxifying effect in case of poisoning with heavy metal salts and other intoxications.

β-D-fructose-1,6-diphosphate - is a natural hexose diphosphate. In its endogenous form, fructose-1,6-diphosphate is an intermediate link in glycolysis, which modulates various enzymatic reactions inside the cell, activating phosphofructokinase, pyruvate kinase and milk dehydrogenase. Parenteral administration of exogenous fructose-1,6-diphosphate has a pharmacological effect at the level of the cell membrane, exerting a glycometabolic and polarizing effect. It is used in the treatment of acute hypophosphatemia, for example, due to a blood transfusion or surgical intervention involving blood circulation outside the body, as well as in the form of parenteral nutrition in situations that are associated with the depletion of phosphates, such as chronic alcoholism, chronic respiratory failure, ischemic cardiomyopathy.

N, N-dimethylglycine supports methylation, metabolism of methionine, folic acid and modulation of the immune system. Dimethylglycine is also involved in maintaining healthy homocysteine levels and inhibits the accumulation of lactic acid in the body.

Ascorbic acid has a metabolic effect. Participates in the regulation of redox processes, carbohydrate metabolism, blood coagulation, tissue regeneration, in the synthesis of steroid hormones, increases the body's resistance to infections, reduces vascular permeability, reduces the need for vitamins B ₁ , B ₂ , A, E, folic acid, pantothenic acid.

L-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 insulin resistance.

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.

Inosine improves myocardial metabolism, has antihypoxic and antiarrhythmic effects. Increases myocardial energy balance. It has a protective effect on the kidneys in ischemic conditions during the operation. Participates in the exchange of glucose, increases the activity of a number of enzymes in the Krebs cycle. Stimulates nucleotide synthesis.

Magnesium and potassium salts of aspartic acid are necessary for the normal functioning of nerve and muscle cells, and also help regulate water balance.

Calcium gluconate regulates metabolic processes, replenishes the deficiency of calcium in the body, has a hemostatic, anti-allergic effect and reduces capillary permeability.

Dextrose 5% is a solvent 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 highly effective dosage form that can be used in various conditions associated with physical overload and overstrain of individual organs and systems. When using the claimed composition, endurance increases, blood supply to the heart improves, metabolism increases, the body recovers faster after exercise.

The inventive composition can be shown in various conditions associated with physical overload and overstrain of individual organs and systems, including diseases of the musculoskeletal system, such as diseases of the muscular system (myofibrosis) and diseases of the ligaments and joints (tendovaginitis, periarthrosis of the shoulder joint, shoulder epicondylosis, bone styloidosis, carpal tunnel syndrome, deforming arthrosis (osteoarthritis), occupational bursitis, etc.), as well as pathologies of the peripheral nervous system, such as autonomic-sensory polyneuropathy, compression neuropathies, coordinating neuroses. In addition, the composition can be used as a supplement in the treatment of asthenopia and phonastenia.

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 the solutions are mixed and the dextrose solution is added to the resulting mixture to obtain a volume of 500 ml. In this way, a product is ready for use.

The drug of the present invention is administered to the patient infusion. The number of infusions and their frequency can be appropriately determined by the attending physician taking into account the symptoms of each patient, age and other indicators. The drug is administered very slowly, about 60 drops per minute.

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

Example 1

Patient, female, 25 years old. The patient complains of increased fatigue, mild aching pains and sensations of tightening in the hands, decreased muscle strength of the upper extremities. The pains that occur at the beginning of the working day intensify and become "gnawing" by the end of the day. On palpation, soreness of the muscles of the hands and pain during tension are revealed.

Blood Lactate - 2.75 mmol / L.

Dynamometry: the right hand - 22.4 kg, the left hand - 20.4 kg.

Goniometry: joint extension (passive movement)

- interphalangeal I of the finger of the right hand - 60 °;

- proximal interphalangeal II-V fingers of the right hand - 65 °;

- metacarpophalangeal I of the finger of the right hand - 60 °;

- metacarpophalangeal II-V fingers of the right hand - 65 °;

- interphalangeal I of the finger of the left hand - 65 °;

- proximal interphalangeal II-V fingers of the left hand - 70 °;

- metacarpophalangeal of the I finger of the left hand - 70 °;

- metacarpophalangeal II-V fingers of the left hand - 75 °;

Electroneuromyography:

- immersion potentials of needle electrodes are stored for more than 10 s;

- distribution of a histogram of action potentials of motor units - the presence of shortened (less than 5 ms in 25% of the total) and elongated (more than 10 ms in 25% of the total) potentials;

a volley of electromyographic activity is recorded with transverse muscle palpation.

Ultrasound of the muscles of the hands:

- the presence of thin hyperechoic strips parallel to the long axis of the muscle, on a hypoechoic background.

Diagnosis - Myofascial syndrome, stage I-II.

Treatment - the claimed composition was prescribed drip for five days.

Sodium flavin adenine dinucleotide 40 mg Nicotinamide adenine dinucleotide phosphate 500 mg Folic acid 15 mg Calcium folinate pentahydrate 50 mg Cyanocobalamin 1 mg Methylcobalamin 500 mcg Glutathione 600 mg α-lipoic (thioctic) acid 50 mg

β-D-fructose-1,6-diphosphate 5000 mg

N, N-dimethylglycine 300 mg Vitamin C 2000 mg L-Taurine 500 mg L-carnitine 1000 mg Inosine 400 mg Magnesium asparaginate 280 mg Potassium asparaginate 320 mg Calcium gluconate 500 mg Dextrose 5% up to 500 ml.

5 days after the infusion:

Pulse - 62 / min, respiratory rate - 19 / min, temperature 36.7, blood pressure - 125/80 mm Hg The general condition is satisfactory. Fatigue and pain in the hands of the patient are not noted. There is a positive trend in the return of muscle strength of the upper limbs, a positive mood, activity throughout the day.

Blood Lactate - 1.80 mmol / L.

Dynamometry: right hand - 25.2 kg, left hand - 24.1 kg.

Example 2

The patient, husband., 22 years old. After an intensive training process, the patient notes severe fatigue, fatigue, irritability, and sleep disturbance. The patient also complains of a decrease in blood pressure, pain in the muscles of the upper and lower extremities and a lack of appetite.

Blood lactate - 3.25 mmol / L.

PWC ₁₇₀ test (according to Karpman) - 1145 kgm / min.

Cooper test - 2.4 km.

Novakki test: load power - 4 W / kg, operating time - 2 min.

Ergospirometry:

Diagnosis - Chronic physical exertion syndrome. Muscle pain syndrome. Lactic acidosis, type B.

Treatment - the claimed composition was prescribed drip for three days.

Sodium flavin adenine dinucleotide 40 mg Nicotinamide adenine dinucleotide phosphate 500 mg Folic acid 15 mg Calcium folinate pentahydrate 50 mg Cyanocobalamin 1 mg Methylcobalamin 500 mcg Glutathione 1200 mg α-lipoic (thioctic) acid 50 mg

β-D-fructose-1,6-diphosphate 10,000 mg

N, N-dimethylglycine 300 mg Vitamin C 2000 mg L-Taurine 500 mg L-carnitine 1000 mg Inosine 400 mg Magnesium asparaginate 280 mg Potassium asparaginate 320 mg Calcium gluconate 500 mg Dextrose 5% up to 500 ml.

3 days after the infusion:

Pulse - 52 / min, respiratory rate - 17 / min, temperature 36.4, blood pressure 115/75 mm Hg General condition is good. Symptoms of chronic physical stress syndrome are not noted. No muscle pain. The patient notes the presence of a positive mood, is active throughout the training process, also notes the normalization of appetite.

Survey indicators.

Blood lactate - 2.20 mmol / L.

Test PWC ₁₇₀ (according to Karpman) - 1910 kgm / min.

Cooper Test - 3.2 km.

Novakki test: load power - 6 W / kg, operating time - 1 min.

Ergospirometry:

Thus, the present invention provides a highly effective pharmaceutical composition for parenteral drip, which can be used in various conditions associated with physical overload and overstrain of individual organs and systems, in conditions requiring speed, endurance and a high concentration of attention.

Claims (2)

A pharmaceutical composition for parenteral drip administration for use in case of overstrain under intense loads, characterized in that it contains a complex of active substances, in the following ratio of components: Sodium flavin adenine dinucleotide 40 mg Nicotinamide adenine dinucleotide phosphate 500 mg Folic acid 15 mg Calcium folinate pentahydrate 50 mg Cyanocobalamin 1 mg Methylcobalamin 500 mcg Glutathione 600-1200 mg α-lipoic (thioctic) acid 50 mg β-D-fructose-1,6-diphosphate 5000-10000 mg N, N-dimethylglycine 300 mg Vitamin C 2000 mg L-Taurine 500 mg L-carnitine 1000 mg Inosine 400 mg Magnesium asparaginate 280 mg Potassium asparaginate 320 mg Calcium gluconate 500 mg Dextrose 5% up to 500 ml