RU2545920C1 - Nadh composition having antioxidant properties - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention provides a composition having antioxidant properties in the form of a tablet, comprising an active agent based on nicotinamide adenine dinucleotide in reduced form (NADH) and inert filling agents, characterised by that the active ingredient is a complex which is a mixture of 10 wt % NADH with 63 wt % vegetable fats, 17 wt % beeswax and 10 wt % chlorophyll, and the inert filling agents are in the form of microcrystalline cellulose, Macrogol 6000, intense sweetener and a food flavourant.

EFFECT: invention provides a new tablet form of NADH.

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Description

The invention relates to the field of chemical-pharmaceutical and food industries, as well as to the field of cosmetology.

These living conditions of people (stress, lack of sleep, environmental pollution, poor diet, bad habits and lifestyle, such as smoking, alcohol, etc.) lead to the fact that the body alone cannot replenish enough energy. Therefore, various energy pharmaceutical formulations and dietary supplements are becoming increasingly common.

An important role in the body, namely in its energy metabolism, is played by nicotinamide adenine dinucleotide (NAD, NAD). NAD is a coenzyme present in all living cells, which is part of the enzymes of the dehydrogenase group that catalyze redox reactions and acts as a carrier of electrons and hydrogen that it receives from oxidized substances. The reduced form of coenzyme (NADH or Coenzyme 1) is a metabolically active form of vitamin B3.

NADH deficiency is manifested in physical or mental fatigue. On the other hand, the more NADH is available to the cell, the more energy it can produce. With increasing age, the body's production of NADH increases markedly.

NADH was opened in 1905. It was only in the 80s that it was possible to create a form suitable for oral administration. This is due, inter alia, to the fact that NADH is extremely unstable in nature due to its chemical composition. Under the influence of oxygen and light, this vitamin can very quickly lose its effectiveness.

Known therapeutic composition according to patent US 5332727, publ. 07/26. 1994. The composition is in the form of tablets coated with an acid-resistant coating, which contain from 3 to 10% by weight of NADH or NADPH, or its physiologically acceptable salt, from 1 to 10% by weight of a stabilizer selected from the group consisting of NaHCO ₃ , ascorbic acid, sodium ascorbate, tocopherol, tocopherol acetate and polyvinylpyrrolidone, and a filler selected from the group consisting of mannitol, microcrystalline cellulose, carboxymethyl cellulose and dibasic calcium phosphate. Storage stability is achieved thanks to the shell.

From patent US 6500451 (B2), publ. 2002-12-31, energy supplement tablets are known that contain NADH, octocosonol, vitamin E, plant magnesium stearate, microcrystalline cellulose, hydrated silicon dioxide and dibasic calcium phosphate. Tablets also require a protective coating.

As the closest analogue (prototype) can be indicated a composition having antioxidant properties, prolonged release from a variety of particles with enteric coating, containing NADH, PVP, ethanol, vitamin E, microcrystalline cellulose, starch (EP 1346723 (A1), publ. 2003- 09-24).

The present invention is to develop a new tablet form of NADH, which manifests its properties when administered intragastrically in the form of a complex that protects the active active substance from the destructive effects of oral enzymes, stomach acids and other factors that deactivate NADH.

The problem is solved by the composition of the tablets, stable but not coated, which includes the active principle in the complex, which is a mixture of 10 wt.% The reduced form of nicotinamide adenine dinucleotide (NADH) with 63 wt.% Vegetable fats, 17 wt.% Beeswax and 10 wt. .% chlorophyll, and as inert fillers - microcrystalline cellulose, Macrogol 6000, an intense sweetener, food flavoring, with the following components, wt.%:

active principle in the form of a complex 10-35 microcrystalline cellulose 50-90 Macrogol 6000 0.05-4.5 sweetener 0.01-2.5 flavoring 0.01-5

As an intense sweetener, aspartame, stevioside, saccharin, acesulfame K and the like can be used.

As a food flavoring you can use any morning or identical natural flavors such as “Sweet Apple”, “Raspberry”, “Apricot”, “Vanilla Cream”, etc. The most preferred flavor is the Sweet Apple flavor.

The NADH tablet contains one active ingredient: the biologically active nicotinamide adenine dinucleotide (NADH), which is presented as part of a complex that is a mixture in a naturally stabilized acid-resistant form - PANMOL®-NADHmicro, containing in wt.%:

10% NADH;

63% vegetable fats;

17% beeswax;

10% chlorophyll.

Vegetable fats can be selected from edible oils, such as cedar, flaxseed, soybean, etc., and can also be glycerides of plant acids, for example palmitic, oleic or linoleic.

The complex may be microcapsules with an average size of 100-200 microns. Microcapsules may optionally be enteric coated.

The possibility of carrying out the invention can be illustrated by the following example.

Example 1

MANUFACTURE PROCESS

All ingredients are weighed:

PANMOL®-NADHmicro 72,000 kg Microcrystalline cellulose 276,480 kg Macrogol 6000 2,880 kg Aspartame 1,440 kg Fragrance "Sweet Apple" 7,200 kg

Next, each ingredient is sieved using a strainer (0.5 ± 0.05 mm) and mixed in a Servolift MC mixer (maximum capacity of the mixing drum is 500 kg - diffusion mixer)

The order of adding to the mixing drum:

1. Microcrystalline cellulose 200,000 kg 2. PANMOL®-NADHmicro 72,000 kg 3. Flavor "Sweet Apple" 7,200 kg 4. Aspartame 1,440 kg 5. Macrogol 6000 2,880 kg 6. Microcrystalline cellulose 76,480 kg

Mixing process parameters:

mixing speed eleven rpm mixing time 50 minutes

The resulting mixture was then compressed using a KILIAN S250 SMART tablet rotary tablet press. The weight of 20 tablets is 5.0 g ± 5%. The average weight of the tablets is 250 mg ± 5%. The height of the tablets is 3.4 ± 0.5 mm. Hardness is not less than 50 N and not more than 120 N.

Each tablet contains:

PANMOL®-NADHmicro (Nicotinamide Adenine Dinucleotide (NADH) Equivalent) 50.0 mg twenty% Inert fillers: Microcrystalline cellulose 192.0 mg 76.8% Macrogol 6000 2.0 mg 0.8% Aspartame 1.0 mg 0.4% Fragrance "Sweet Apple" 5.0 mg 2.0% Total amount 250.0 mg one hundred%

NADH tablets are round, unpainted, white or close to white or cream in color with rare black-green spots with a diameter of preferably 9 mm. The tablet form is with a flat top surface with beveled edges and an average weight of 250 mg.

Disintegration time no more than 15 minutes.

During the tabletting process, the appearance, average weight and hardness of 20 tablets are monitored every 20 minutes. Information corresponding to the technological process (time and date of production and all technological operations, the number of batches of starting materials and the weight of the starting materials, the number of tablet mixes and the mass of tablets, the appearance of the tablets, the average weight and height of the tablets) are recorded in the batch protocol in accordance with the current technological instructions .

Tablets are packaged in labeled primary packaging - blisters (10 tablets per blister).

Shelf life of at least 2.5 years.

The obtained tablet form of NADH shows its properties when administered intragastrically in the form of a complex that protects the active active substance from the destructive action of oral enzymes, gastric acid, and other factors that deactivate NADH.

Taking a new tablet form of NADH helps:

- increase the level of wakefulness;

- improving the ability to concentrate and hold attention;

- Prevention of fatigue and maladaptation when changing time zones;

- increase in daily working capacity and vitality;

- the prevention of impaired memory, attention, and other aspects of the cognitive functioning of various origins, including maladaptation associated with stress;

- normalization of mood swings of various origins;

- improvement in asthenia of any genesis;

- as part of complex therapy, improvement of conditions in chronic fatigue syndrome, Parkinson's disease, Alzheimer's disease, fibroimalgia, signs of aging, metabolic syndrome, including hypercholesterolemia and hypertension, depression of various origins, various conditions associated with a decrease in immunity.

Claims (1)

A composition having antioxidant properties in the form of a tablet containing an active principle based on nicotinamide adenine dinucleotide in reduced form (NADH) and inert fillers, characterized in that it contains an active principle in the complex, which is a mixture of 10 wt.% NADH with 63 wt.% vegetable fats, 17 wt.% beeswax and 10 wt.% chlorophyll, and as inert fillers, microcrystalline cellulose, Macrogol 6000, an intense sweetener, food flavoring, with the following components mass%:
active principle in the form of a complex 10-35 microcrystalline cellulose 50-90 Macrogol 6000 0.05-4.5 sweetener 0.01-2.5 flavoring 0.01-5