RU2709500C1 - Pharmaceutical composition for parenteral drip introduction - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to medicine, and concerns pharmaceutical compositions for parenteral drip introduction for treating time zone change syndrome.

EFFECT: well-selected, balanced qualitative and quantitative composition provides a dosage form suitable for treating desynchronization, the therapeutic effect of which is manifested rather quickly for 0,5–2 hours.

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Description

The invention relates to medicine and relates to pharmaceutical compositions for parenteral drip intended for the treatment of time zone change syndrome.

Time zone change syndrome, also called jet lag or desynchronization, is a temporary sleep problem that can affect anyone who travels quickly across multiple time zones. The human body has its own internal clock or circadian rhythms that signal the body when to stay awake and when to sleep. Jetlag occurs because the body’s internal clock is still synchronized with the original time zone, and not with the time zone in which the person appears. The more time zones intersect, the greater the likelihood that a person will encounter a change of time zones syndrome.

Jetlag can cause daytime fatigue, poor health, insomnia, problems with alertness, and gastrointestinal problems. The state of desynchronization is temporary, but it can significantly reduce the comfort of rest or business trip.

Time Zone Change Syndrome is usually temporary and usually does not require treatment. Symptoms often improve within a few days, although sometimes they last longer. However, with frequent travel, and the constant occurrence of desynchronization, drug therapy can be used.

Often, you can help the body recover by filling up the deficiency of vitamins and nutrients.

Most people lack the necessary vitamins and minerals. Moderate and even pronounced hypovitaminosis is present in no less than three quarters of the population. According to many, this can be fixed with the help of multivitamins. It should be noted that this approach helps only in part, since in well-known drugs there is no clear selection of the composition aimed at treating certain pathologies. In addition, most multivitamins are produced in the form of oral preparations, which affects the bioavailability of their vitamins.

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. To fill the deficiency of vitamins or minerals, it may take more than 6 months when using oral delivery, while infusions can correct the deficiencies within 1-3 months. 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, intended for the treatment of time zone change syndrome.

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 for desynchronization.

The object of the present invention is a pharmaceutical composition for parenteral drip, intended for the treatment of change of time zone syndrome, characterized in that it contains a complex of active substances, in the following ratio of components:

Thiamine disulfide phosphate 50 mg Fursultiamine hydrochloride 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Dexpanthenol 50 mg Pyridoxine hydrochloride 50 mg Biotin 1 mg Calcium folinate pentahydrate 10.8 mg Cyanocobalamin 500 mcg Glutathione 600 mg L-α-glycerophosphocholine 250 mg N-L-Acetyl-L-Cysteine 100 mg L-Taurine 250 mg Ubidecarenone 50 mg Magnesium Sulfate Hydrate 1.23 g Vitamin C 1000 mg Sodium chloride 0.9%, or Dextrose 5%, or Up to 500 ml Distilled water

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

Thiamine is a water soluble vitamin. In the human body, as a result of phosphorylation processes, it turns into cocarboxylase, which is a coenzyme of many enzyme reactions. Thiamine plays an important role in carbohydrate, protein and fat metabolism, as well as in the processes of nervous excitation in synapses. The forms of thiamine differ in bioavailability and stability, as well as in accumulation in various tissues, body fluids, penetration through the blood-brain barrier, and the rate of conversion to coenzyme form. Thiamine forms such as thiamine chloride hydrochloride and thiamine disulfide phosphate accumulate more intensively in the brain tissue.

Fursultiamine (thiamine tetrahydrofurfuryl disulfide) is a medicine and vitamin used to treat thiamine deficiency. Chemically, it is a disulfide derivative of thiamine and is similar in structure to allithiamine.

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.

Dexpanthenol makes up for pantothenic acid deficiency, has an anti-inflammatory effect, and stimulates regeneration processes. In the body forms an active metabolite - pantothenic acid, which is a substrate (the only indispensable component) stimulator of the synthesis of coenzyme A; the latter catalyzes acylation in the body, participates in almost all metabolic processes (the tricarboxylic acid cycle, the metabolism of carbohydrates, fats and fatty acids, phospholipids, proteins, etc.), provides the formation of corticosteroids, acetylation of choline with the formation of acetylcholine.

Pyridoxine (vitamin B6), is involved in metabolism; necessary for the normal functioning of the central and peripheral nervous system. Entering the body, it is phosphorylated, converted to pyridoxal-5-phosphate and is part of the enzymes involved in decarboxylation and transamination of amino acids. Participates in the exchange of tryptophan, methionine, cysteine, glutamine and other amino acids. It plays an important role in the exchange of histamine. Helps normalize lipid metabolism.

Biotin is part of the enzymes that regulate protein and fat balance, has a high activity. Participates in the synthesis of glucokinase, an enzyme that regulates carbohydrate metabolism. It is a coenzyme of various enzymes, including transcarboxylases. Participates in the synthesis of purine nucleotides. It is a source of sulfur, which takes part in the synthesis of collagen. With the participation of biotin, reactions of activation and transfer of CO ₂ proceed.

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 B12 in humans.

Glutathione is the most powerful natural antioxidant in all human cells, and is often referred to as the "main antioxidant" of the body. 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 for body tissues, including arteries, brain, heart, liver, lungs, and skin. Glutathione levels decrease with age. All cells in the human body are able to synthesize glutathione. But the highest concentration of glutathione is in the liver, making it critically important in the detoxification and elimination of free radicals. Free radicals are very reactive compounds that form in the body during normal metabolic functions; they can also enter the body from the external environment. The accumulation of these compounds can lead to oxidative stress, which occurs when the generation of free radicals in the body exceeds the body's ability to neutralize and eliminate them. Glutathione metabolically has many functions. As mentioned earlier, 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.

Alpha-glycerophosphocholine is a natural physiological precursor of acetylcholine, a neurotransmitter that is involved in memory and other cognitive functions. This is the most bioavailable form of choline, which is perfectly absorbed, becomes an integral part of the cell membranes of the brain and nerve tissues and crosses the blood-brain barrier.

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.

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.

Ubidecarenone transfers hydrogen ions, is a component of the respiratory chain. It increases the content of prostacyclin in the blood and reduces thromboxane. Helps to restore physical performance, increases the body's adaptive capabilities to increased loads, stressful effects and hypoxia.

Magnesium plays an important role in many enzymatic reactions of the body and plays a key role in neurochemical transmission and muscle excitability and, therefore, has been successfully used for seizures and other muscle-related problems. Magnesium acts peripherally, causing vasodilation - relaxing the walls of blood vessels, increasing blood flow, which can help reduce blood pressure, as well as the prevention and treatment of migraines.

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 B1, B2, A, E, folic acid, pantothenic acid.

Sodium chloride 0.9%, dextrose 5% 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 time zone change syndrome, the therapeutic effect of which is manifested quite quickly, within 0.5-2 hours.

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. In this way, a product is ready for use.

The infusion preparation of the present invention is symptomatically administered to a patient. Specific modes 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

Patient, female, 26 years old. Complaints - the patient after six hours of flight notes a slight fatigue, fatigue, periodic drowsiness, a little forgetfulness, irritability, sleep disturbance. Also, the patient complains of a lack of appetite. Diagnosis - Time Zone Change Syndrome, mild desynchronosis.

Treatment - a dropper of the following composition has been prescribed:

Thiamine disulfide phosphate 50 mg Fursultiamine hydrochloride 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Dexpanthenol 50 mg Pyridoxine hydrochloride 50 mg Biotin 1 mg Calcium folinate pentahydrate 10.8 mg Cyanocobalamin 500 mcg Glutathione 600 mg L-α-glycerophosphocholine 250 mg N-L-Acetyl-L-Cysteine 100 mg L-Taurine 250 mg Ubidecarenone 50 mg Magnesium Sulfate Hydrate 1.23 g Vitamin C 1000 mg Sodium chloride 0.9% Up to 500 ml

30 minutes after the infusion: General condition is satisfactory. Symptoms of a time zone change syndrome are not noted. The patient notes the presence of a positive mood, is active throughout the working day, also notes the normalization of appetite.

Example 2

Patient, husband., 28 years old. Complaints - The patient after nine hours of flight notes severe fatigue, fatigue, constant drowsiness, slight forgetfulness, irritability, and insomnia. The patient also complains of a lack of appetite. Diagnosis - Time zone change syndrome, desynchronosis of moderate severity.

Treatment - a dropper of the following composition has been prescribed:

Thiamine disulfide phosphate 50 mg Fursultiamine hydrochloride 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Dexpanthenol 50 mg Pyridoxine hydrochloride 50 mg Biotin 1 mg Calcium folinate pentahydrate 10.8 mg Cyanocobalamin 500 mcg Glutathione 600 mg L-α-glycerophosphocholine 250 mg N-L-Acetyl-L-Cysteine 100 mg L-Taurine 250 mg Ubidecarenone 50 mg Magnesium Sulfate Hydrate 1.23 g Vitamin C 1000 mg Dextrose 5% Up to 500 ml

45 minutes after the infusion: General condition is satisfactory. Symptoms of a time zone change syndrome are not noted. The patient notes the presence of a positive mood, is active throughout the working day, also notes the normalization of appetite and digestive function of the body.

Example 3

The patient, husband., 33 years old. Complaints - The patient after twelve hours of flight noted pronounced disorientation in time, severe fatigue, fatigue even with little physical exertion, constant drowsiness, tinnitus, severe irritability and insomnia. The patient also complains of severe discomfort in the abdomen. Diagnosis: Time zone change syndrome, severe desynchronosis.

Treatment - a dropper of the following composition has been prescribed:

Thiamine disulfide phosphate 50 mg Fursultiamine hydrochloride 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Dexpanthenol 50 mg Pyridoxine hydrochloride 50 mg Biotin 1 mg Calcium folinate pentahydrate 10.8 mg Cyanocobalamin 500 mcg Glutathione 600 mg L-α-glycerophosphocholine 250 mg N-L-Acetyl-L-Cysteine 100 mg L-Taurine 250 mg Ubidecarenone 50 mg Magnesium Sulfate Hydrate 1.23 g Vitamin C 1000 mg Distilled water Up to 500 ml

90 minutes after the infusion: General condition is satisfactory. Symptoms of the time zone change syndrome are practically not observed, a slight fatigue is observed. The patient is oriented in time and space, notes the presence of a positive mood, takes an active part in resolving work issues. There is no discomfort in the abdomen; appetite is slightly reduced.

Thus, the present invention provides a highly effective and fast-acting pharmaceutical composition for parenteral drip administration, which can be used with time zone change syndrome.

Claims (2)

A pharmaceutical composition for parenteral drip, intended for the treatment of time zone change syndrome, characterized in that it contains a complex of active substances, in the following ratio of components: Thiamine disulfide phosphate 50 mg Fursultiamine hydrochloride 100 mg Flavin adenine sodium dinucleotide 10 mg Nicotinamide adenine dinucleotide phosphate 100 mg Dexpanthenol 50 mg Pyridoxine hydrochloride 50 mg Biotin 1 mg Calcium folinate pentahydrate 10.8 mg Cyanocobalamin 500 mcg Glutathione 600 mg L-α-glycerophosphocholine 250 mg N-L-Acetyl-L-Cysteine 100 mg L-Taurine 250 mg Ubidecarenone 50 mg Magnesium Sulfate Hydrate 1.23 g Vitamin C 1000 mg Sodium chloride 0.9%, or Dextrose 5%, or Up to 500 ml Distilled water