COMPOSITION CONTAINING PHYTIC ACID, MAGNESIUM AND POLYPHENOLS FOR THE TREATMENT OR PREVENTION OF RENAL LITHIASIS

Abstract

The present invention is related to a composition comprising phytic acid or a phytate salt, magnesium in the form of salt, hydroxide or oxide and optionally at least one polyphenol. These components may be in isolated form or be part of an enriched plant extract. The invention is also related to the use of this composition for the treatment of renal lithiasis, preferably calcium or calcium oxalate lithiasis, either in the form of a medicament, a nutraceutical or functional food or food supplement.

Claims

1. Composition comprising phytic acid or any of its salts and magnesium in the form of salt, hydroxide or oxide.

2. Composition according to claim 1 comprising at least one polyphenol.

3. Composition according to claim 2 wherein the polyphenol is selected from epicatechin, catechin, gallocatechin, epigallocatechin, quercetin, resveratrol, gallic acid and tannic acid.

4. Composition according to claim 2 wherein the polyphenol is in the form of enriched plant extract from grape seed.

5. Composition according to claim 1 wherein the phytate salt is selected from sodium, potassium, calcium, magnesium, zinc or calcium-magnesium.

6. Composition according to claim 1 wherein the phytate is in the form of an enriched plant extract from rice, locust bean, wheat, oat, soy or almond.

7. Composition according to claim 1 wherein the magnesium is in a form that is selected from magnesium oxide, magnesium hydroxide, magnesium citrate, magnesium stearate, magnesium carbonate, magnesium chloride and magnesium sulfate.

8. Composition according to claim 1 comprising between 40-50% by weight of phytic acid or its salts.

9. Composition according to claim 1 comprising between 25-40% by weight of magnesium in the form of salt, hydroxide or oxide.

10. Composition according to claim 2 comprising between 10-30% by weight of polyphenols.

11. Composition according to also comprising lactose, sucrose, talc, magnesium stearate, cellulose, calcium salts, gelatin or fatty acids.

12. Composition according to claim 1 which is presented in the form of a pharmaceutical composition, functional food, a nutraceutical product or a food supplement.

13. Composition according to claim 1 for the manufacture of a medicament.

14. Use of the composition according to claim 1 for the manufacture of a medicament for the treatment of renal lithiasis.

15. Use according to claim 14 wherein renal lithiasis is calcium renal lithiasis.

16. Use of the composition according to claim 1 for the preparation of a medicament intended to reduce the risks and improve the health status of patients with diseases related with the crystallization of calcium oxalate.

17. Use according to claim 14, wherein the composition is in a suitable dosage for administration of between 500 mg/day and 1,000 mg/day.

Description

BRIEF DESCRIPTION OF THE FIGURES

[0037] FIG. 1. It shows the graphical representation of the induction times of the crystallization (in minutes) for a 200 mg/L calcium and 50 mg/L oxalate solution, in synthetic urine, at different magnesium and phytate concentrations.

EXAMPLES

Example 1. Measurement of the Crystallization of Calcium Oxalate in the Presence of Magnesium and Phytate

[0038] From a 200 mg/L calcium and 50 mg/L oxalate solution, in synthetic urine, the induction times for the crystallization of calcium oxalate have been calculated in the presence of different phytate and/or magnesium concentrations. Table 1 shows said induction times, which as it can be clearly seen in FIG. 1, increase with the increase in the concentration of magnesium and phytate. Thus, when there is neither magnesium nor phytate, the calcium oxalate takes 1 minute to crystallize. This time increases up to 10 minutes when 100 mg/L magnesium is added and, in turn, it increases up to 44 minutes if, in addition to the 10 mg/L magnesium, 1 mg/L phytate is added.

TABLE-US-00001 TABLE 1 induction times of crystallization (in minutes) for a 200 mg/L calcium and 50 mg/L oxalate solution, in synthetic urine, at different concentrations of magnesium and phytate. mg/L 0 mg/L Mg 25 mg/L Mg 75 mg/L Mg 100 mg/L Mg phytate t (min) t (min) t (min) t (min) 0 1 1.5 6 10 0.5 3 6 12 20 0.75 4 7 18 27 1 6.5 9.5 35 44

Example 2. Effect of the Composition of the Invention on Wistar Rats Subjected to a Lithogenic Diet

[0039] A group of Wistar rats was pre-treated with polyphenols extracted from white grape seeds (added to the drinking water in concentrations of 200 mg/L) and phytate (1% of the solid diet fed to the animals, in the form of phytin, which is the calcium magnesium salt). Subsequently, papillary renal lithiasis was induced by administration of ethylene glycol and the preventive treatment was continued. The antilithiatic activity of the polyphenol+phytate mixture was evaluated through the calcium content of the kidneys of the animals (extracted at the end of the experiment) and the corresponding histological studies of the renal tissue, by comparison with the corresponding control groups. It was observed that the applied prophylactic treatment reduced renal calcification by 50%.

Example 3. Effect of the Composition of the Invention on Patients with Problems of Renal Lithiasis

[0040] In this example three pharmaceutical compositions of the present invention are illustrated.

Composition 1.

[0041]

TABLE-US-00002 Compound Amount Calcium-magnesium phytate 300 mg Magnesium citrate 250 mg Epicatechin 100 mg

Composition 2.

[0042]

TABLE-US-00003 Compound Amount Calcium-magnesium phytate 300 mg Magnesium citrate 250 mg Catechin 150 mg

Composition 3.

[0043]

TABLE-US-00004 Compound Amount Brown rice extract equivalent to 250 mg an amount of phytate of Magnesium oxide 150 mg Black grape seed extract equivalent to 150 mg an amount of polyphenols of

Composition 4.

[0044]

TABLE-US-00005 Compound Amount Locust bean germ extract and dry wheat extract 150 mg equivalent to an amount of phytate of Magnesium oxide 100 mg White grape seed extract equivalent to an 90 mg amount of polyphenols of

[0045] 200 mg of calcium-magnesium phytate (phytin) together with 200 mg of magnesium citrate and 100 mg of quercetin were orally administered to a patient, twice a day, at breakfast and after dinner. After the treatment, it was observed that the inhibitory capacity of the urine of the patient against the crystallization of calcium oxalate increased 40% with respect to the urine of the own patient before ingesting phytate. The antioxidant capacity of the urine (potentiometrically evaluated using a platinum electrode) increased 15%. These variations may imply from a significant reduction of the recurrence to a total elimination of the calculogenesis process because they eliminate and/or normalize key factors in the calculogenesis process, such as the inhibitory capacity of the urine, oxaluria and the protection against oxidative stress.