RU2527042C1 - Biologically active food additive for osteoporosis prevention - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to biologically active food additives. The biologically active food additive for osteoporosis prevention contains calcium and magnesium salts, vitamin D3, as well as boron and zinc salts. The above calcium salt is normal calcium phosphate, and the above magnesium salt is magnesium phosphate. The biologically active food additive also contains selenium salt and vitamin B6. The ingredients in a single dose of the biologically active food additive are taken in the following proportions: calcium phosphate Ca₃(PO₄)2·2H₂O - 400 to 4000 mg; vitamin D3 - 300 to 1000 IU; magnesium phosphate -Mg₃(PO₄)2·2H₂O - 100 to 800 mg; soluble boron salt at B⁺³ basis - 0.003 to 0.005 mg; soluble zinc salt at Zn⁺² basis - 2 to 20 mg; selenium salt at Se⁺⁶ basis - 0.0005 to 0.003 mg; vitamin B6 - 0.001 to 0.005 mg.

EFFECT: invention enables providing higher calcium absorption by bone tissue and eliminating a negative effect of the biologically active food additive on the gastric and gastrointestinal walls.

3 dwg, 2 ex

Description

The invention relates to the pharmaceutical industry and medicine, namely to biologically active food supplements (BAA), and can be used to prevent diseases of osteoporosis.

A wide range of calcium-containing preparations for the prevention of diseases of osteoporosis is known: these are calcium preparations based on calcium carbonate, calcium citrate, calcium gluconate, calcium aspartate, calcium ascorbate, calcium amino chelate, calcium fumarate, calcium succinate, calcium acid phosphates, calcium citrate, etc. connections. In this case, most calcium-containing preparations contain vitamin D3, which controls the absorption of calcium by the body. Magnesium also plays an important role in the prevention of osteoporosis: by regulating the absorption of calcium, it provides magnesium-calcium balance and prevents calcification in soft tissues.

Known biologically active food supplement "Orthocalcium + Magnesium" containing as active substances calcium citrate, magnesium dicitrate trisubstituted anhydrous, ascorbic acid (vitamin C), zinc sulfate, manganese sulfate, pyridoxine hydrochloride (vitamin B6), phytomenadion (vitamin K1) and cholecalciferol (D3 (Orthomolecular Medicine Website. URL: KMD_0.html) [1]. It is known that calcium citrate is one of the most well-absorbed calcium compounds: when it enters the stomach, it is well absorbed in an ionized form in a very short time However, by providing calcium into the body in the form of ions, the known supplement thus irritates the walls of the stomach, causes the osmotic effect of calcium ions in the cell membrane and causes irritation of the upper gastrointestinal tract (GIT) .For this reason, clinicians are forced to stop taking these drugs in most cases.

A known pharmaceutical composition containing calcium, or a mixture of calcium and vitamin D, or a mixture of calcium and magnesium, characterized in that it contains calcium as an active substance in an amount of from 150 to 1500 mg, more preferably from 200 to 600 mg, or a mixture of calcium and vitamin D, where vitamin D is present in an amount of from 100 to 1000 ME, preferably from 400 to 900 ME, or a mixture of calcium and magnesium, which contains magnesium in an amount of from 20 to 500 mg, more preferably from 150 to 300 mg, where the active substances containing calcium and magnesium are finely ground, so h then at least 80% of the particles are less than 75 micrometers in size; and, in addition, containing adjuvants (Patent CZ 303069, publ. 03.21.2012) [2]. The known solution also does not solve the problem of the negative effect of calcium compounds on the walls of the stomach.

Known biologically active additive designed to protect against bone loss, including a calcium salt selected from calcium carbonate, calcium gluconate, calcium lactate, calcium hydrogen phosphate and calcium nitrate, vitamin D and at least one mineral substance selected from the group including salts of boron, copper, magnesium, manganese and zinc. The content of calcium salt is from 1000 to 2000 mg, vitamin D from 50 to 800 ME, boron salt from 50 to 3000 mg, copper salt from 0.1 to 0.3 mg, magnesium salt from 10 to 150 mg, manganese salt - from 3 to 10 mg, zinc salt - from 3 to 25 mg (Patent RU 2152216, publ. 10.03.2000) [3]. Like solutions [1,2], this supplement does not solve the problems of destruction of the walls of the stomach and irritation of the gastrointestinal tract by calcium ions. In addition, the intake of calcium in the body in an ionized form does not guarantee high adsorption of calcium by bone cells, which is explained by blood homeostasis: calcium that appears in the ionic form is immediately “thrown” into a depot such as blood vessels, cartilage, kidneys and bile, causing undesirable pathology. Thus, very quickly penetrating the walls of the stomach, calcium ions enter, including the joints, walls of arteries and other tissues of the body, calcining them.

The task of the invention is to develop a biologically active food supplement, providing replenishment of calcium in the bones of the body and high adsorption of calcium in bone cells while eliminating the negative effects of the additive on the walls of the stomach and gastrointestinal tract.

To solve this problem, a biologically active food supplement for the prevention of diseases of osteoporosis is proposed, including calcium salt, vitamin D3, as well as magnesium, boron and zinc salts, characterized in that said calcium salt is normal calcium phosphate, magnesium salt is magnesium phosphate, in addition contains salt of selenium and vitamin B6, with the following content of components in a single dose of biologically active additives:

Calcium phosphate - Ca ₃ (PO ₄ ) × 2H ₂ O - from 400 to 4000 mg;

Vitamin D3 - from 300 to 1000 ME;

Magnesium phosphate-Mg ₃ (PO ₄ ) 2 × 2H ₂ O - from 100 mg to 800 mg;

Soluble boron salt in terms of B ⁺³ - from 0.003 to 0.005 mg;

Soluble zinc salt in terms of Zn ⁺² - from 2 to 20 mg;

Soluble salt of selenium in terms of Se ⁺⁶ - from 0.0005 to 0.003 mg;

Vitamin B6 - from 0.001 to 0.005 mg.

The inventive biologically active additive is a phosphate complex formed by calcium and magnesium phosphates, vitamins D3 and B6, as well as salts of boron, zinc and selenium, necessary for the active complexation of nonionic calcium. Entering the stomach, the calcium compound does not dissolve immediately and is not absorbed by the walls of the stomach, but for a long time exists in the form of an organic complex, moves into the digestive tract and is absorbed not in the stomach, but in the digestive tract, thus not causing irritation of the walls of the stomach. In addition, with the first intake of this complex, the activity and proliferation of osteoblasts begins to increase, which, in turn, release a greater amount of the protein precomplex into the blood, which are involved in the absorption of the calcium phosphate complex in the digestive tract. Thus, a positive feedback loop is formed and auto-amplification of the consumption of the phosphate complex from the gastrointestinal tract occurs. Against the background of an increase in the activity of osteoblasts and an increase in the concentration of nonionic calcium, the processes of restoration in the bones intensify. Moreover, the activation of osteoblasts and stem cells in the bone marrow enhances the reproductive functions of the whole organism.

The quantitative content of the dietary supplement components is determined by the daily norm, while the content and ratio of the components is such that a stable phosphate complex is formed that is well absorbed by the bone tissue. Moreover, the claimed solution allows the use of even double, triple single doses of dietary supplements, which is important in acute cases of osteoporosis. In this case, the excess of the drug goes through the stool, without causing inconvenience to patients.

Unlike the prototype [3], which contains minerals selected from the group including salts of boron, copper, magnesium, manganese and zinc, which are considered equivalent in it, in the claimed solution, the magnesium salt in the form of magnesium phosphate performs the function of supporting calcium along with calcium phosphate, and vitamins D3 and B6, boron, zinc and selenium salts are necessary to fully ensure the functioning of the feedback loop. In addition, from the prototype, the claimed solution is distinguished by the use of normal calcium phosphate as a calcium salt, whereas in the prototype secondary acid calcium phosphate is declared as a possible calcium salt. Since acid calcium phosphate behaves like other ionogenic calcium salts, immediately penetrating the walls of the stomach, causing their irritation, the use of normal calcium phosphate is essential for the active complexation and absorption of nonionic calcium.

Thus, normal calcium phosphate, magnesium phosphate, vitamin D3, soluble salts of boron, zinc, selenium and vitamin B6 in the declared amounts form a phosphate complex that exists in the gastrointestinal tract for a long time, and calcium is adsorbed in the gastrointestinal tract in a non-ionic form and therefore does not irritate the walls of the stomach while this complex enhances the activity and proliferation of osteoblasts, which, in turn, enhances the recovery processes in the bones.

A new technical result achieved by the claimed invention is to increase the adsorption of calcium by bone tissue and auto-amplification of this process while eliminating the negative effects of biologically active additives for the prevention of osteoporosis on the walls of the stomach and gastrointestinal tract. This drug did not detect side effects and does not irritate the digestive tract.

The invention is illustrated by the following.

Example 1

To obtain the claimed biologically active additives from the conditions for 2000 mg of Ca ₃ (PO ₄ ) and 400 mg of Mg ₃ (PO ₄ ), an equimolar amount of CaCL ₂ + MgCL ₂ and Na ₃ PO ₄ solutions is prepared and mixed in a disintegrator. The resulting mixture is placed in a reactor, stirred and brought into an exact equimolar ratio to organoleptic neutrality (tastelessness). This is achieved by adding a small amount of CaCL ₂ salt _, or MgCL _2, or Na ₃ PO ₄ to the mixture. The mixture is kept under stirring at a temperature of 50 to 90 ° C. and a nanogel with a size of 10 nm to 10 μm is grown. The resulting nanogel is filtered and washed with soluble salts, then mixed with vitamin D3 - 500ME, boron salt, for example, potassium borate in terms of B ⁺³ - 0.004 mg, zinc salt, for example, zinc citrate in terms of Zn ^{+ 2} - 12 mg ; salt of selenium, for example, potassium selenate in terms of Se ⁺⁶ - 0.0005 mg; Vitamin B6 - 0.002 mg. The taste of dietary supplements is formed using natural flavors, the stability of microbiology is achieved by the addition of antibacterial drugs that are allowed for preservation. The manufacture of dietary supplements in the form of a nanogel relieves problems with swallowing the drug, the taste is made with the help of natural flavors, the stability of microbiology is achieved by adding permitted antibacterial drugs for preserving the products.

Example 2

To obtain the claimed biologically active additives from the conditions for 1500 mg of Ca ₃ (PO ₄ ) and 300 mg of Mg ₃ (PO ₄ ), an equimolar amount of CaCL ₂ + MgCL ₂ + Na ₃ PO ₄ solutions is prepared and mixed in a disintegrator. The resulting mixture is placed in a reactor, stirred and brought into an exact equimolar ratio to organoleptic neutrality (tastelessness). This is achieved by adding a small amount of CaCL ₂ or MgCL ₂ or Na ₃ PO ₄ salt to the mixture. The mixture is kept under stirring at a temperature of from 50 to 90 ° C and grown nano gel with a size of from 10 nm to 10 μm. The resulting nanogel is filtered and washed with soluble salts, then mixed with vitamin D3 - 600 ME, boron salt, for example sodium tetraborate in terms of B ⁺³ - 0.003 mg, zinc salt, for example zinc citrate in terms of Zn ⁺² - 6 mg ; salt of selenium, for example magnesium selenate in terms of Se ⁺⁶ - 0.001 mg; Vitamin B6 - 0.003 mg. The taste of dietary supplements is formed using natural flavors, the stability of microbiology is achieved by the addition of antibacterial drugs that are allowed for preservation. The gel is dried in a lyophilizer, crushed in a mill and tableted.

The claimed biologically active additive for the prevention of diseases of osteoporosis was tested in clinics in Germany, Bulgaria, France and Russia, while there were no cases of side effects, including those associated with indigestion. So, there was a successful remission and overgrowing of a crack of a shin bone caused by genetic problems of an adult male of 30 years. The tibia bone for 7 months was in a cast, while bone remission with standard preparations was not achieved. Plaster was removed due to the appearance of edema and the phenomena of atrophy. Figure 1 presents an x-ray of the leg bone with a crack, not fused after 7 months of being in a cast. Figure 2, 3 presents x-rays of this bone after two months of use of the claimed dietary supplement. They show that the crack is filled with bone tissue of good density.

Thus, the claimed biologically active food supplement for the prevention of diseases of osteoporosis provides replenishment of the calcium content in the bones of the body and high adsorption of calcium in the cells of the bone tissue while eliminating the negative effects of the additive on the walls of the stomach.

Claims (1)

Biologically active food supplement for the prevention of osteoporosis, including calcium and magnesium salts, vitamin D3, as well as boron and zinc salts, characterized in that said calcium salt is normal calcium phosphate, magnesium salt - magnesium phosphate, additionally contains selenium salt and vitamin B6 with the following components in a single dose of a dietary supplement:
Calcium phosphate - Ca ₃ (PO ₄ ) 2 × 2H ₂ O - from 400 to 4000 mg;
Vitamin D3 - from 300 to 1000 ME;
Magnesium phosphate - Mg ₃ (PO ₄ ) 2 × 2H ₂ O - from 100 to 800 mg;
Soluble boron salt in terms of B ⁺³ - from 0.003 to 0.005 mg;
Soluble zinc salt in terms of Zn ⁺² - from 2 to 20 mg;
Soluble salt of selenium in terms of Se ⁺⁶ - from 0.0005 to 0.003 mg;
Vitamin B6 - from 0.001 to 0.005 mg.

Images