LT5888B - Food supplement increasing protection of the epithelium of lower urinary tract against repeatedly occurring infections - Google Patents

Abstract

The present invention claims food supplement increasing protection of the epithelium of lower urinary tract against repeatedly occurring infections by being composed of mixture of not more than 99,999975 % by weight of lyophilized fruits of American cranberry (Vaccinium macrocarpon) and/or its juice, and/or lyophilized juice, and/or their extracts and of from 0,0000025 to 0,0694 % by weight vitamin D in the form of ergocalciferol D2 or cholecalciferol D3 or mixture thereof D2/D3.

Description

Technical field

This technical solution provides a nutritional supplement with lower urinary tract protection against recurrent bacterial infections. the supplement comprises a combination of lyophilized fruit and / or juice of Vaccinium macrocarpon and vitamin D2 / D3 (ergocalciferol / cholecalciferol). Its action results in increased resistance of the urinary tract surface, that is, the epithelium, to the attachment of uropathogenic bacteria.

State of the art

For centuries, North American continents have used Vaccinium macrocarpon fruit and / or juice to treat lower urinary tract infections in both sexes. The pharmacological action of cranberry fruit-based substances is due to the inhibition of uropathogenic bacterial adhesion to the urinary epithelium. Due to its anti-adhesive action, this plant has become a popular active food or nutritional supplement in Europe as well. The substances contained in berry cranberry also have antioxidant and anti-inflammatory properties, inhibit the formation of pathogenic bacterial biofilm on the gastric and urinary tract mucosal epithelium (Howell AB (2007). 737; Howell AB et al (2010) Dosage effect on uropathogenic Escherichia coli anti-adhesion activity in urine following consumption of cranberry powder standardized for proanthocyanidin content: a multicentric randomized double-blind study BMC Infectious Diseases 10, 94; Shmuely H, Yahav J, Samra Z et al (2007) Effect of cranberry juice on eradication of Helicobacter pylori in patients treated with antibiotics and a proton pump inhibitor Mol Nutr Food Res 51,746-751; Yamanaka A, Kimizuka R, Kato T, Okuda K. (2004) Inhibitory effects of cranberry juice on attachment of weather streptococci and biofilm formation Weather Microbiol I mmunol 19, 150-154; Jepson RG, Craig JC (2008) Cranberries for preventing urinary tract infections. Cochrane Database Systemic Revievs, issue 4, CD001321).

Vitamin D is the most important signaling molecule (hormone) in the body's regulation of calcium metabolism (homestase), affecting bone density and remodeling. The physiological level of 25-hydroxyvitamin D in childhood is essential for bone growth, for bone quality in adults, and for slowing down osteoporosis and reducing the risk of fractures in old age. Low levels of 25-hydroxyvitamin D in the blood are associated with an increased risk of developing colon cancer, autoimmune diseases, type 1 diabetes, and a number of cardiovascular events. In a clinical experiment, vitamin D supplementation has been shown to improve the protection of the lower urinary tract and the bladder epithelium by inducing the expression of the gene responsible for cathelicidin synthesis. This peptide protects urinary system organs from colonization by urapathogenic bacteria (Cavalier E et al. (2009) Vitamin D: Current Status and Perspectives. Clin Chem Lab Med 47 (2), 120127; Rosen CJ (2011) Vitamin D insufficiency. N Engi J Med 364,248-254; Souberbielle JC et al (2010) Vitamin D and Musculoskeletal Health, Cardiovascular Disease, Autoimmunity and Cancer: Recommendations for Clinical Practice, Autoimmunity Revievs 9, 709-715; Hertting O (2010) Vitamin D Induction of the Human antimicrobial peptide cathelicidin in the urinary bladder. PLOS one 5 (12), e15580).

The objective of the proposed solution is to enrich the market for food supplements with the active ingredient containing a combination of freeze-dried cranberry (Vaccinium macrocarpon) juice or its juice or its extract and vitamin D ₂ / D ₃ (ergocalciferol / colecalciferol). The purpose of this combination is to exploit the synergism between the antiadhesive action of the cranberry and the regulatory function of vitamin D in the synthesis of the antimicrobial peptide catelicidin in the urinary epithelium and thereby protect the urinary tract from colonization by uropathogenic bacteria. Both components have no side effects. Commercially available products containing a combination of higher cranberry fruit juice and vitamins A, B, C, D, and E. These products are available in the form of juice, fruit jelly or chewing gum as described in RU 2242145, CN 101590093, EA 200801042 or US 7056541. However, the active substances of Vaccinium macrocarpon and vitamin D in these products correspond to the category of the product as a food supplement and not as a food supplement. The declared content of vitamin D in the proposed dietary supplement, in addition to the indicated activity, contributes to the deficiency of this vitamin in the central European population. Acute hypercalcaemia, which may occur at doses greater than 10,000 IU of vitamin D, that is, more than 150 ng of 25-hydroxyvitamin D per ml of blood, cannot be induced by the proposed dietary supplement.

The essence of the technical solution

The stated aim has been achieved by a technical solution which is a dietary supplement for bacterial infections of the lower urinary tract. The mode of action is that the active ingredient is a mixture of up to 99.999975% by weight of freeze-dried cranberry (Vaccinium macrocarpori) fruits and / or their juices and / or their dried juices and / or their extracts, and 0.00000025 to 0.0694% by weight of vitamin D in the form of ergocalciferol D2 or cholecalciferol D3 or a mixture thereof D2 / D3.

The active ingredient is advantageously mixed with up to 1000 times the amount of physiologically harmless base, if necessary supplemented with excipients, where the harmless base consists of at least one material selected from the group consisting of emollient or solvent or carrier and mixtures thereof, and optionally, the added excipients include at least one material selected from the group consisting of colloidal reagents or antioxidants, or colorants, or stabilizers, or emulsifiers, or film-forming materials, or mixtures thereof.

Ideally, the emollient is selected from glycerol or polyols as water or ethanol as solvent and carriers are selected from gelatin or modified starch or cellulose and its derivatives or starch and its derivatives or calcium and sodium carbonates or calcium phosphate or carrageenan , or vegetable oils, or glycerol, or triglycerides, or phosphates, or invert syrup groups, or mixtures thereof. In another embodiment, the colloidal reagent is selected from the group consisting of silica or magnesium stearate, or a mixture thereof, the antioxidant is selected from the group consisting of tocopherol or rosemary acid or sodium ascorbate or ascorbyl palmitate and the dyes are selected from iron oxide or titanium oxide groups of vegetable concentrates, or combinations thereof. In yet another embodiment, the stabilizer is comprised of beeswax or polysorbates or esters of polyglycerol and fatty acids, wherein the emulsifiers are selected from lecithins or sorbitan mono stearate or sorbitan mono stearate or sorbitan monolaurate or sorbitan monopalmitate or hydrolyzate of the sorbitan monopalmitate group and hydroxypropylcellulose, or polyethylene glycols, or polyvinyl alcohol, or shellac.

The dietary supplement contains polyphenols such as anthocyanins, flavonoids, phenolic acid and also minerals and vitamins in the cranberry, which have a positive effect on the lower urinary tract, which, when combined with ergocalciferol D2 or cholecalciferol D3, reduces the risk of urinary tract infection.

Examples of technical solution implementation

The specific implementation of the available technical solutions can be seen from the following examples of food supplement uses:

Example 1:

The dietary supplement, which enhances protection of the lower urinary tract epithelium against recurrent infections, is presented as a solid 530 mg capsule with liquid content. It consists of:

- active substances:

freeze-dried pome fruit cranberry powder ............. 180 mg ergocalciferol D2 ............................ ........................... 0.005 mg

- harmless base: carrier consisting of:

gelatin .......................................... 105 mg vegetable oil ... ................................. 225,615 mg Softener - Polyol ............. ............................................. 12.35 mg diluent - water 5.03 mg

- Emergent material :

antioxidant - sodium ascorbate ..................................... 2 mg

Example 2:

A nutritional supplement that enhances protection of the lower urinary tract epithelium against recurrent infections is provided as a soft powder capsule with a weight of 735 mg. It consists of:

- active substances:

spray dried dried cranberry juice ..... 200 mg cholecalciferol D3 .................................... ................... 0.005 mg

- harmless base: carrier - mixture of:

gelatin ............................ 142.545 mg of soy oil .................. ............ 290 mg Softener - Glycerol .................................. ................... 67.58 mg solvent - water ......................... ............................... 8.22 mg

- Emergent material:

antioxidant - tocopherol acetate ..................................... 2 mg dye - iron oxide ... ......................................... 1.65 mg stabilizer - beeswax. .......................................... 10 mg Emulsifier - Lecithin ... .................................................. 13 mg

Example 3:

The nutritional supplement, which enhances the protection of the lower urinary tract epithelium against recurrent infections, is presented as a solid powder capsule of 670 mg. It consists of:

- active substances:

lyophilized bitter cranberry powder .......................... mixture of ergocalciferol D2 and cholecalciferol D3 500 mg ......... 0.0075 mg

- harmless basis:

carrier - gelatin ................................................ 148.7925 mg Softener - Glycerol ........................................... .............. 7.60 mg solvent - water .............................. .............................. 3.60 mg

- Emergent material :

antioxidant - sodium ascorbate ....................................... 2 mg colloidal reagent - silica .................................. 8 mg

Example 4:

A nutritional supplement that enhances protection of the lower urinary tract epithelium in the form of a 550 mg tablet or coated tablet against recurrent infections. It consists of:

- active substances:

dry cranberry extract ......................... 90 mg ergocalciferol D2 ................. ........................... 0.005 mg

- harmless base: carrier - mixture of:

microcrystalline cellulose .................... 230.045 mg calcium hydrogen phosphate .................... 192.50 mg carboxymethylcellulose .......................... 13.75 mg cotton oil ................. ................. 1.50 mg

- excipients: colloidal reagent - mixture of:

magnesium stearate ..................... 3.30 mg of silica ..................... ....... 4.80 mg film-forming material - mixture of:

hydroxypropylmethylcellulose .......... 4.20 mg hydroxypropylcellulose .................... 3.40 mg dye mixture:

titanium oxide ............................. 2.50 mg natural vegetable concentrates ............. ......... 4 mg

Example 5:

A nutritional supplement that increases the protection of the lower urinary tract epithelium against recurrent infections is provided in the form of a syrup of 5,000 mg. It consists of:

- active substances:

dried cranberry fruit juice ........... 500.0 mg ergocalciferol D2 ............................. ................. 0.005 mg

- harmless basis:

carrier - invert syrup ............................... 4.492,995 mg solvent - ethanol ......... ............................................ 5 mg

- Emergent material :

antioxidant - sodium ascorbate ................................... 2 mg

Industrial use

A food supplement with a protective action on the epithelium of the urinary tract can be used prophylactically against recurrent acute inflammation of the lower urinary tract caused by uropathogenic bacteria. The dietary supplement also positively influences the gastrointestinal microflora and supplements vitamin D deficiency in the modern population.

Claims (13)

DEFINITION OF INVENTION 1. A food supplement for the treatment of bacterial infections of the lower urinary tract, characterized in that the active ingredient is a mixture of up to 99.999975% by weight of the dried and / or dried fruit and / or juice of Vaccinium macrocarpon. juice and / or their extracts and 0.0000025 to 0.0694% by weight of vitamin D in the form of ergocalciferol D2 or cholecalciferol D3 or a mixture thereof D2 / D3. 2. A nutritional supplement according to claim 1, wherein the active ingredient is mixed with up to 1000 times the amount of physiologically harmless base, optionally supplemented with excipients. 3. A nutritional supplement according to claim 2, wherein the non-toxic base comprises at least one substance selected from the group consisting of a softener or a solvent or a carrier, or a variety of mixtures thereof. Food supplement according to claim 2, characterized in that, if necessary, the added excipients consist of at least one substance selected from the group consisting of colloidal reagents or antioxidants or dyes or stabilizers or emulsifiers or film-forming substances and / or from various variations of their blends. Food supplement according to claim 3, characterized in that the emollient is selected from the group consisting of glycerol or polyol. 6. The nutritional supplement according to claim 3, wherein the solvent is water or ethanol. 7. The nutritional supplement according to claim 3, wherein the carrier is selected from gelatin or modified starch or cellulose and its derivatives or starch and its derivatives or calcium and sodium carbonate or calcium phosphate or carrageenan or vegetable oils, or glycerol, or triglycerides, or phosphates, or invert syrup groups, or mixtures thereof. 8. The dietary supplement of claim 4, wherein the colloidal reagent is selected from the group consisting of silica or magnesium stearate or mixtures thereof. 9. The dietary supplement of claim 4, wherein the antioxidant is selected from the group consisting of tocopherols or rosemary acid or sodium ascorbate or ascorbyl palmitate. 10. The dietary supplement of claim 4, wherein the coloring agents are selected from the group consisting of iron oxide or titanium oxide, or natural vegetable concentrates, or combinations thereof. 11. The dietary supplement of claim 4, wherein the stabilizer is beeswax or polysorbates or polyglycerol and fatty acid esters. 12. The dietary supplement of claim 4, wherein the emulsifiers are selected from the group consisting of lecithins or sorbitan mono stearate, or sorbitan monooleate, or sorbitan mono stearate, or sorbitan monolaurate, or sorbitan monopalmitate. 13. The dietary supplement of claim 4, wherein the film-forming materials are selected from hydroxypropylmethylcellulose or hydroxypropylcellulose, or polyethylene glycol, or polyvinyl alcohol, or shellac.