NUTRACEUTICAL OR PHARMACEUTICAL COMPOSITION COMPRISING IRON PYROPHOSPHATE FOR TREATING AND/OR PREVENTING IRON DEFICIENCY CONDITIONS OR DISEASES

Abstract

Provided herein is a composition of substances preferably obtained from natural sources, which is effective in preventing and/or treating iron deficiency conditions or diseases. The composition includes iron pyrophosphate, phosphatidylserine, phosphatidylcholine and starch, preferably acetylated pregelatinised starch. The formulation gives the composition gastro-resistance properties and high bioavailability of the active ingredient iron pyrophosphate. The composition is prepared in the form of a solid, semi-solid or liquid pharmaceutical dosage, preferably for oral administration.

Claims

1-8. (canceled)

9. A method for improving absorption of iron in intestinal environment in a subject in need thereof, the method comprising administering to the subject a nutraceutical or pharmaceutical composition comprising a combination of iron pyrophosphate, phosphatidylcholine, phosphatidylserine and starch.

10. The method of claim 9, wherein the nutraceutical or pharmaceutical composition comprises iron pyrophosphate in an amount ranging between 0.1 and 90% of the total weight of said combination.

11. The method of claim 9, wherein the nutraceutical or pharmaceutical composition comprises starch in an amount ranging between 0.1 and 90% of the total weight of said combination.

12. The method of claim 11, wherein the starch is acetylated pregelatinized starch.

13. The method of claim 9, wherein the nutraceutical or pharmaceutical composition comprises phosphatidylcholine in an amount ranging between 0.01 and 50% of the total weight of said combination.

14. The method of claim 9, wherein the nutraceutical or pharmaceutical composition comprises phosphatidylserine in an amount ranging between 0.01 and 50% of the total weight of said combination.

15. The method of claim 9, wherein the subject suffers from an iron deficiency condition or disease.

16. The method of claim 15, wherein the iron deficiency condition or disease is selected from the group consisting of anaemia, iron deficiency, pregnancy and breastfeeding, loss of appetite, asthenia, menstruation, bleeding, menopause, inflammatory bowel disease, coeliac disease, obesity, gastric ulcers, colon cancer, uterine cancer, intestinal polyps, and haemorrhoids.

17. The method of claim 9, wherein the nutraceutical or pharmaceutical composition is formulated into a liquid, semi-solid or solid oral dosage form.

18. The method of claim 17, wherein the oral dosage form is a powder, a mouth-soluble powder, a granulate, a hard capsule, a soft-gel capsule, a tablet, a sachet, a solution, a suspension or an emulsion.

Description

EXAMPLES

Example 1

[0064]

TABLE-US-00001 Active ingredient Quantity % Iron pyrophosphate 54 Acetylated MODIFIED STARCH 44.2 AMPRAC01 44.2 30% Phosphatidylcholine 1.2 60% Phosphatidylserine 0.6

Example 2

[0065]

TABLE-US-00002 Active ingredient Quantity % Iron pyrophosphate 54 PREGELATINISED CORN STARCH VN 44.2 44.2 30% Phosphatidylcholine 1.2 60% Phosphatidylserine 0.6

Example 3

[0066]

TABLE-US-00003 Active ingredient Quantity % Iron pyrophosphate 40 PREGELATINISED CORN STARCH VN 44.2 55 30% Phosphatidylcholine 3.6 60% Phosphatidylserine 1.4

Example 4

[0067]

TABLE-US-00004 Active ingredient Quantity % Iron pyrophosphate 60 Acetylated MODIFIED STARCH 35 AMPRAC01 44.2 30% Phosphatidylcholine 2.5 60% Phosphatidylserine 2.5

Example 5

[0068] The fluidized bed granulation technology was used for the preparation of the product “Granular iron pyrophosphate” An example of a preparation applied to the compositions of Examples 1 and 2 is given below. The manufacturing process consists of the following steps:

[0069] a) Mixing:

[0070] The raw materials previously loaded into the basket granulator are subjected to a first fluidized bed mixing step, with the working air having a temperature of 80-90° C., until a mixture having an average temperature of 44° C. is obtained. During this step, a bulk is created which is homogeneous as regards composition and temperature, an indispensable prerequisite for the optimal course of the subsequent granulation step.

[0071] b) Granulation

[0072] The granulation step comprises the insertion of an aqueous solution of a suitably chosen binding or granulation agent, by means of direct nebulization on the premixed and fluidized-bed bulk. In this step, the working air is again used at 90° C., appropriately selecting the speed of introduction of the binding solution in order to obtain a granulate which is structured according to the expectations (particle size, bulk density, flowability) and homogeneous.

[0073] c) Drying

[0074] During the drying step, the water content of the preformed granulate is basically brought back to the conditions of the starting mixture of raw materials. The temperature of the working air of the granulate at the end of the step is appropriately assessed in the pilot testing phase towards this objective.

[0075] d) Calibration

[0076] The semi-finished product obtained from the above step is transferred from the fluidized bed granulator to an oscillating granulator where it is calibrated through a sieve to reduce the particle size of the granules and agglomerates having a coarser structure.

Example 6

[0077] Iron Release into a Sham Gastric Environment

[0078] 1 g of sample was weighed and introduced into the container of the dissolving apparatus containing 900 mL of 0.1 M HCl. The dissolution was performed for 2 h at 37° C. and 75 rpm. After dissolution, 1 mL of sample was diluted to 50 mL with 0.1 M HCl. The preparation was performed in six replicates for each sample.

[0079] The results thus obtained are shown in FIG. 1, where the iron values are expressed as grams per 100 grams of formulation (g/100 g).

[0080] FIG. 1 shows that iron pyrophosphate as such (blue, upper line), not delivered with a functional excipient, after 120 minutes in the sham gastric environment, releases an amount of iron of 7.5 g±0.5 g per 100 g of formulation.

[0081] Iron pyrophosphate delivered with the combination of phosphatidylcholine, phosphatidylserine and acetylated pregelatinized starch (orange, lower line), after 120 minutes in the sham gastric environment, releases an amount of iron of 3.4 g±0.2 g per 100 g of formulation.

[0082] Therefore, the results thus obtained show that the composition according to the present invention, comprising iron pyrophosphate, phosphatidylcholine, phosphatidylserine and acetylated pregelatinized starch, is able to protect iron from the gastric environment in a much better way than what happens with iron pyrophosphate devoid of delivery systems. By minimizing the side effects due to premature release of iron into the stomach, the composition according to the present invention ensures that the almost total amount of iron will be available for absorption in the intestinal environment, thus promoting bioavailability, compliance and efficacy in all those conditions or diseases characterized by iron deficiency, such as anaemia, iron deficiency, pregnancy and breastfeeding, loss of appetite, asthenia, menstruation, bleeding and menopause, inflammatory bowel disease, coeliac disease, obesity, gastric ulcers, colon or uterine cancer, intestinal polyps, and haemorrhoids.