COMPOSITIONS CONTAINING CURCUMIN HAVING IMPROVED BIOAVAILABILITY

Abstract

The invention relates to the pharmaceutical or non-pharmaceutical use of an effective amount of spirulina and/or of an extract/extracts of spirulina for improving the bioavailability of orally administered curcumin in humans or animals. The invention also includes pharmaceutical or non-pharmaceutical preparations including spirulina and/or extracts of spirulina containing curcumin having improved bioavailability.

Claims

1.-21. (canceled)

22. A method for improving the bioavailability of orally administered curcumin in an animal or human, the method comprising: orally administering curcumin; and orally administering an effective quantity of at least one of spirulina and one or more spirulina extracts.

23. The method according to claim 22, wherein the animal comprises a horse, pig, dog, or cat.

24. The method according to claim 22, wherein the curcumin is administered as at least one of an antioxidant, antiseptic, antibacterial, and anti-inflammatory agent.

25. The method according to claim 22, wherein the curcumin is administered for the treatment or the prevention of cancer, cardiovascular diseases, diabetes, arthritis, neurological diseases, or Crohn's disease.

26. The method according to claim 22, wherein a weight ratio of the at least one of spirulina and one or more spirulina extracts:curcumin is between 20:1 and 1:3.

27. The method according to claim 22, wherein a weight ratio of the at least one of spirulina and one or more spirulina extracts:curcumin is between 10:2 and 1:2.

28. The method according to claim 22, wherein a weight ratio of the at least one of spirulina and one or more spirulina extracts:curcumin is between 8:3 and 3:4.

29. The method according to claim 22, wherein a quantity of spirulina ranges between 0.1 and 20 mg/kg body weight of the animal or human.

30. The method according to claim 22, wherein a quantity of spirulina ranges between 0.5 and 15 mg/kg body weight of the animal or human.

31. The method according to claim 22, wherein a quantity of spirulina ranges between 1 and 10 mg/kg body weight of the animal or human.

32. The method according to claim 22, wherein the curcumin is administered as a food supplement in the field of animal or human nutrition.

33. An oral preparation with improved bioavailability of curcumin, the preparation comprising: curcumin; an effective quantity of at least one of spirulina and one or more spirulina extracts; and optionally at least one of other active ingredients, excipients, and supports.

34. The preparation according to claim 33, wherein a weight ratio of at least one of spirulina and one or more spirulina extracts:curcumin is between 20:1 and 1:3.

35. The preparation according to claim 33, wherein a weight ratio of at least one of spirulina and one or more spirulina extracts:curcumin is between 10:2 and 1:2.

36. The preparation according to claim 33, wherein a weight ratio of at least one of spirulina and one or more spirulina extracts:curcumin is between 8:3 and 3:4.

37. The preparation according to claim 33, wherein a quantity of curcumin ranges between 0.1 and 20 mg/kg body weight of the animal or human.

38. The preparation according to claim 33, wherein a quantity of curcumin ranges between 0.5 and 15 mg/kg body weight of the animal or human.

39. The preparation according to claim 33, wherein a quantity of curcumin ranges between 1 and 10 mg/kg body weight of the animal or human.

40. The preparation according to claim 33, consisting of a combination of curcumin with at least one of spirulina and one or more spirulina extracts.

41. The preparation according to claim 33, wherein the preparation is a ready for use preparation, a concentrated preparation to be mixed with common foods, in powder form, or in the form of tablets or capsules.

42. Manufacturing process for a preparation according to claim 33, the process comprising mixing an effective quantity of at least one of spirulina and one or more spirulina extracts with curcumin, and optionally with other active ingredients, excipients, and supports.

Description

BRIEF DESCRIPTION OF THE DRAWINGS

[0028] Other distinguishing features and characteristics of the invention will emerge from the detailed description of several advantageous illustrative embodiments presented below, by referring to the appended figures. They show:

[0029] FIG. 1: is a graph representing the bioavailability (or the kinetics) of the curcumin preparation S1 according to the invention, administered orally to a horse;

[0030] FIG. 2: is a graph representing the comparative bioavailability (or the kinetics) of a curcumin preparation, administered intravenously to a pig.

EXAMPLES

[0031] Materials and Method

[0032] A first composition comprising curcumin and spirulina was prepared by combining in the following order, with constant stirring and homogenisation, purified water, potassium sorbate, citric acid, sucrose, curcumin 95% (curcuminoid content: 95.7%, determined by HPLC), spirulina extract and Xanthan gum. The spirulina extract was obtained by dissolving 1 g of standard raw material in 20 ml water under reflux for 60 minutes. The aqueous extract was filtered then made into a dry concentrate in a desiccator under vacuum. The dry residue was then dissolved in 5 ml methanol so as to obtain the spirulina extract. This preparation is designated hereinafter as curcumin S1.

[0033] A first experiment to determine the bioavailability (pharmacokinetic study) of curcumin in the horse was carried out by determining the quantity of curcumin in the blood (plasma concentration).

[0034] The 3 selected horses were between 7 and 10 years old, each estimated to weigh 500 kg. The curcumin S1 was administered orally (2.6 grams of curcumin S1 for 500 kg of live weight, i.e. 5.6 mg/kg) in a single dose.

[0035] Plasma samples were taken prior to the administration (time TO) of the curcumin S1 preparation and 3 hours, 6 hours, 9 hours, 12 hours, 24 hours, 36 hours and 50 hours after administration of the preparation.

[0036] The samples were frozen at −18° C. until the analytical determination.

[0037] The technique used for the determination of the curcumin concentration in the plasma was HPLC (high performance liquid chromatography).

[0038] Results

[0039] The results of the mean curcumin concentrations in the plasma as a function of time are presented in Table 1.

TABLE-US-00001 TABLE 1 Curcumin concentration in the plasma after oral administration of a preparation curcumin S1 in the horse Time (hours) Nanograms/millilitre 0 0 3 230 6 260 9 280 12 410 24 350 36 150 50 0

DISCUSSION

[0040] As can be seen, the curcumin concentrations in the plasma obtained with the preparation curcumin S1 are relatively high in relation to the orally administered single dose (2.6 grams of curcumin S1 for 500 kg of live weight, i.e. 5.6 mg/kg) with a plasma concentration peak at 12 hours and remaining almost constant for 12 hours (T12=410 ng/ml and T24=350 ng/ml).

[0041] Indeed, the comparison with a study in the pig after intravenous administration of 0.60 grams of curcumin for 23 kg of live weight, wherein the plasma concentration peaks at 24 hours and remains at a constant level during 10 hours (Table 2, FIG. 2), shows that the curcumin S1 level, thanks to the presence of spirulina or spirulina extracts, exhibits a very good bioavailability after oral administration with reduced effects of excretion and consequently a more rapid plasma concentration peak (12 hours) that remains for at least 12 hours.

TABLE-US-00002 TABLE 2 Curcumin concentration in the plasma after intravenous administration in the pig (for comparison) Time (hours) Nanograms/millilitre 0 0 3 537 6 557 9 713 24 724 48 537 72 385

CONCLUSIONS

[0042] The obtained results allow the following conclusions:

[0043] 1) Curcumin S1 (preparation according to the invention) exhibits a very good bioavailability of the curcumin with a plasmatic half-life of at least 24 hours, after a single oral administration.

[0044] 2) The pharmacokinetics of the orally administered curcumin S1 are similar to the kinetics of a curcumin used intravenously (in the pig).