RU2709502C1 - Pharmaceutical composition for parenteral drip introduction - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for parenteral drip introduction for treating non-infectious dermatological diseases.

EFFECT: well-chosen, balanced qualitative and quantitative composition provides creating a dosage form suitable for treating various pathological skin conditions, the therapeutic effect of which is manifested rather quickly for several days.

1 cl, 4 ex

Description

The invention relates to medicine and relates to a pharmaceutical composition for parenteral drip, intended for the treatment of dermatological diseases of non-infectious origin.

The skin is the largest organ of the human body and it, like other organs, is subject to various pathologies. In addition to external negative manifestations, many types of skin pathologies cause discomfort and are very painful. Pathological changes in the skin can be caused by various infections, can occur against the background of inflammation, and can also be hereditary. The main approaches in the treatment of skin diseases are the use of oral or local dosage forms.

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 drugs 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 dermatological diseases of non-infectious origin.

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 various dermatological diseases of non-infectious origin.

The object of the present invention is a pharmaceutical composition for parenteral drip, intended for the treatment of dermatological diseases of non-infectious origin, characterized in that it contains a complex of active substances in the following ratio of components:

Riboflavin sodium phosphate or Sodium flavin adenine dinucleotide 10-30 mg Nicotinic acid or 20-100 mg Nicotinamide adenine dinucleotide phosphate Dexpanthenol 100-250 mg Pyridoxine Hydrochloride or Pyridoxal Phosphate Hydrate 30 mg Biotin 1-2 mg α-lipoic (thioctic) acid 25-50 mg Tranexamic acid 100-250 mg Glutathione 600-2400 mg Monoammonium glycyrrhizinate (in terms of glycyrrhizic acid) 53-106 (40-80) mg Magnesium Sulfate Hydrate 1.23 g L-methionine 292 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 240.6 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-cysteine hydrochloride 120 mg L-glycine 698 mg Ubidecarenone 50 mg Vitamin C 750-2000 mg Sodium chloride 0.9% or dextrose 5% or Distilled water up to 500 mg

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

Riboflavin, also known as vitamin B2, is an important nutrient that helps in the formation of ATP, the main form of energy storage by the body. It is also a cofactor in the production of glutathione, an important antioxidant in the body. Flavin adenine dinucleotide is a coenzyme that takes part in many redox biochemical processes. Formed from riboflavin.

Niacin plays a significant role in the activity of various enzymes involved in the metabolism of carbohydrates and fats, as well as for the functioning of the nervous and digestive systems, the production of sex hormones and cholesterol, and skin health. Nicotinamide adenine dinucleotide phosphate is a naturally occurring coenzyme of certain dehydrogenases, enzymes that catalyze redox reactions in living cells.

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.

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.

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.

Alpha Lipoic Acid (ALA) is a fatty acid that acts as a vitamin, although it is not classified as such. As a coenzyme, ALA plays an important role in glucose metabolism, which produces energy in cells. ALA also has antioxidant properties and, therefore, is necessary to control free radicals. Since this acid is soluble in both water and fat, it is sometimes called the “universal antioxidant” - it supports the body’s defense against free radicals, processes antioxidant nutrients such as vitamin C and vitamin E, and helps maintain healthy blood sugar levels ( when used as part of a diet).

Tranexamic acid inhibits the action of the plasmin activator and plasminogen, has a hemostatic effect in bleeding associated with increased fibrinolysis, as well as anti-allergic and anti-inflammatory effects by suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions.

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. Metabolically, glutathione 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.

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.

Glycyrrhizic acid has an anti-inflammatory effect, reducing the level of alanine aminotransferase and aspartate aminotransferase in the blood, antioxidant properties - reduces the formation of oxygen free radicals, helps to reduce the degree of fibrosis.

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, promotes the restoration of 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.

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.

Cysteine is an essential amino acid. It can be synthesized in a mammalian organism from serine with the participation of methionine as a source of sulfur, as well as ATP and vitamin B6. In some microorganisms, a source of sulfur for the synthesis of cysteine may be hydrogen sulfide. Cysteine promotes digestion by participating in transamination processes. Helps neutralize certain toxic substances and protects the body from the damaging effects of radiation.

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.

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 Bl, B2, A, E, folic acid, pantothenic acid. Compensates the increased needs of the body for vitamin C for diseases accompanied by fever.

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 various dermatological diseases of non-infectious origin, the therapeutic effect of which is manifested quickly enough, within a few days. The patient does not need to take oral medications for several months. In most cases, significant changes in the course of the disease are detected after the first infusion.

The inventive composition can be shown in the following types of skin pathologies - allergic dermatitis, toxidermia, eczema, atopic dermatitis, urticaria, erythema, acne, rosacea, as well as other non-infectious skin pathologies.

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 ready for use is obtained.

The infusion preparation of the present invention is administered to the patient for 1 to 5 days. 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, husband., 27 years old. Complaints of severe skin itching on the upper and lower extremities, the lateral surface of the neck and in the gluteal region. Itching is accompanied by a rash in the form of blisters of a pinkish-brown hue, which rise above the surface of the skin and disappear when pressed on them. The patient also complains of dry skin, increased irritability and insomnia. Diagnosis - Allergic pigmented urticaria.

Treatment - a dropper of the following composition was prescribed for 3 days:

Riboflavin Sodium Phosphate 20 mg A nicotinic acid 50 mg Dexpanthenol 100 mg Pyridoxine hydrochloride 30 mg Biotin 1 mg α-lipoic (thioctic) acid 25 mg Tranexamic acid 100 mg Glutathione 600 mg Monoammonium glycyrrhizinate (in terms of glycyrrhizic acid) 53 (40) mg Magnesium Sulfate Hydrate 1.23 g L-methionine 292 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 240.6 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-cysteine hydrochloride 120 mg L-glycine 698 mg Ubidecarenone 50 mg Vitamin C 1000 mg Dextrose 5% up to 500 ml

3 days after the infusion: the general condition is satisfactory. Attacks of skin itching are not noted. The skin of the upper, lower extremities and the gluteal region turned pale and acquired a normal light shade. Blisters and their formation are not noted. Irritability and sleep disturbances are not observed. There is a slight weakness.

Example 2

The patient, female, 24 years old. Complaints of intolerable skin itching in the elbow and knee bends, on the side of the neck, armpits, in the inguinal region, on the face and hands. Itching is accompanied by redness, dry skin, a feeling of tightening, peeling. Occasionally, isolated papules with serous fluid are noted in the affected areas. There is also slight cracking of the skin and small areas of hyperkeratosis on the hands. Also complaints of increased irritability and insomnia. The diagnosis is allergic contact dermatitis.

Treatment - a dropper of the following composition was prescribed for 3 days:

Riboflavin Sodium Phosphate 10 mg A nicotinic acid 50 mg Dexpanthenol 100 mg Pyridoxine hydrochloride 30 mg Biotin 1 mg α-lipoic (thioctic) acid 25 mg Tranexamic acid 100 mg Glutathione 1200 mg Monoammonium glycyrrhizinate (in terms of glycyrrhizic acid) 53 (40) mg Magnesium Sulfate Hydrate 1.23 g L-methionine 292 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 240.6 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-cysteine hydrochloride 120 mg L-glycine 698 mg Ubidecarenone 50 mg Vitamin C 1000 mg Sodium chloride 0.9% up to 500 ml

3 days after the infusion: the general condition is satisfactory. Attacks of skin itching are not noted. The skin of the face and upper limbs turned pale and acquired a pinkish tint. The formation of new papules is not noted. Irritability and sleep disturbances are not observed. There is a slight weakness.

Example 3

The patient, female, 23 years old. Complaints of severe redness and itching on the skin of the face, side of the neck, back, abdomen, upper and lower extremities and in the inguinal region. Itching is accompanied by generalized dry skin, peeling. The formation of papules with serous fluid is observed throughout the body. There is also severe cracking of the skin and large plaques of hyperkeratosis throughout the body, especially pronounced at the sites of scratching of the skin. This condition is accompanied by a periodic rise in temperature to 37.2-37.5 ° C. Also complaints of severe irritability and persistent insomnia. The diagnosis is atopic diffuse neurodermatitis.

Treatment - a dropper of the following composition was prescribed for 3 days:

Sodium flavin adenine dinucleotide 30 mg Nicotinamide adenine dinucleotide phosphate 100 mg Dexpanthenol 250 mg Pyridoxal Phosphate Hydrate 30 mg Biotin 2 mg α-lipoic (thioctic) acid 50 mg Tranexamic acid 250 mg Glutathione 2400 mg Monoammonium glycyrrhizinate (in terms of glycyrrhizic acid) 106 (80) mg Magnesium Sulfate Hydrate 1.23 g L-methionine 292 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 240.6 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-cysteine hydrochloride 120 mg L-glycine 698 mg Ubidecarenone 50 mg Vitamin C 2000 mg Distilled water up to 500 ml

3 days after the use of infusions: the general condition is satisfactory. Attacks of skin itching are not noted. The skin of the face, body and limbs turned pale and acquired a pinkish tint. Hyperkeratosis plaques have acquired clear boundaries and tend to decrease in size. The formation of new papules is not noted. Temperature rise is not observed. Irritability and sleep disturbances are not observed.

Example 4

The patient, husband., 32 years old. Complaints of an increase in body temperature to 37.5 ° C, a manifestation of general weakness and pain in the muscles and joints of the upper and lower extremities. On the skin, rashes of a characteristic type are noted, having the form of flat volume papules of red-pink or pinkish-brownish color. A small part of the papules is in the form of vesicles with serous light contents. Rashes in the region of the lower leg, knees, hands and feet, as well as on the surface of the elbows are accompanied by severe itching, a feeling of discomfort and burning. Also, the patient complains of increased irritability and insomnia. Diagnosis - Nebulous erythema multiforme.

Treatment - a dropper of the following composition was prescribed for 3 days:

Riboflavin Sodium Phosphate 10 mg A nicotinic acid 25 mg Dexpanthenol 100 mg Pyridoxine hydrochloride 30 mg Biotin 1 mg α-lipoic (thioctic) acid 25 mg Tranexamic acid 100 mg Glutathione 600 mg Monoammonium glycyrrhizinate (in terms of glycyrrhizic acid) 53 (40) mg Magnesium Sulfate Hydrate 1.23 g L-methionine 292 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 240.6 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-cysteine hydrochloride 120 mg L-glycine 698 mg Ubidecarenone 50 mg Vitamin C 750 mg Sodium chloride 0.9% up to 500 ml

3 days after the infusion: the general condition is satisfactory. Attacks of skin itching and burning are not noted. Pain in the muscles and joints of the upper and lower extremities is also not observed. The temperature component is normal. The skin of the upper, lower extremities of normal color. Papules and their formation is not observed. Irritability and sleep disturbances are not observed. There is a slight fatigue during physical exertion.

Thus, the present invention provides a highly effective and fast-acting pharmaceutical composition for parenteral drip, which can be used for various dermatological diseases of non-infectious origin.

Claims (2)

A pharmaceutical composition for parenteral drip, intended for the treatment of dermatological diseases of non-infectious genesis, characterized in that it contains a complex of active substances, in the following ratio of components: Riboflavin sodium phosphate or Sodium flavin adenine dinucleotide 10-30 mg Nicotinic acid or Nicotinamide adenine dinucleotide phosphate 20-100 mg Dexpanthenol  100-250 mg Pyridoxine Hydrochloride or Pyridoxal Phosphate Hydrate 30 mg Biotin 1-2 mg α-lipoic (thioctic) acid 25-50 mg Tranexamic acid 100-250 mg Glutathione 600-2400 mg Monoammonium glycyrrhizinate (in terms of glycyrrhizic acid)  53-106 (40-80) mg Magnesium Sulfate Hydrate 1.23 g L-methionine 292 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 240.6 mg L-threonine 128 mg L-valine 192 mg L-histidine hydrochloride hydrate 100 mg L-cysteine hydrochloride 120 mg L-glycine 698 mg Ubidecarenone 50 mg Vitamin C 750-2000 mg Sodium chloride 0.9%, or Dextrose 5%, or Distilled water up to 500 ml