DESC:Technical field of the invention

The present invention relates to improved oral compositions of creatine and the method of preparing said compositions. The compositions of the invention provide enhanced absorption of creatine with reduced side effects. The composition contains creatine, piperine, acidity regulator and optionally multi nutrients, electrolytes, macronutrients and bioavailability enhancers.

Background of the Invention

Taking oral creatine supplements has been used to increase creatine and creatine phosphate stores in the human body to meet the increased energy requirements. Creatine consumption is more critical in case of the athletes because creatine aids in the production of extra energy due to increased demand of the muscles during exercise. When an athlete exercises, energy is required for the muscle to function properly. The increased energy comes from several different sources, but primarily from nutrients obtained from the food. These nutrients are broken down by natural processes occurring within the human body, and new compounds formed which are used to generate energy for use by the muscles.

A disadvantage with the preparations according to the prior art is that the creatine supplement available are not absorbed properly due to various reasons leading to decreased energy production and subsequent low performance during a strenuous session. The supplemental consumption of creatine does not help to provide the expected extra energy due to poor absorption.

In the light of the disadvantages mentioned in the prior art with respect to the poor absorption, the objective of the present invention is to develop creatine compositions which are stable and increase creatine efficacy by enhancing its absorption with piperine and other optional multi-nutrients and bioavailability enhancers.

Summary of the Invention

In one general aspect, the present invention provides an improved oral composition of creatine wherein the composition comprises:
(a) creatine monohydrate;
(b) piperine;
(c) acidity regulator and optionally,
(c) multi-nutrients, electrolytes, macronutrients and bioavailability enhancers.
In an embodiment of the above aspect, creatinine monohydrate is present in an amount of about 70% to about 99% by weight of the composition. Creatine monohydrate may be present in micronized form to enhance the solubility.

In an embodiment of the above aspect, piperine is present as black pepper extract or pure piperine. Alternatively, piperine can be present as powdered black pepper. Black pepper extract is present in an amount of about 0.01% to about 5% by weight of the composition, preferably from about 0.1 to about 2.0% by weight of the composition.

In another embodiment of the above aspect, the acidity regulator is present in an amount sufficient to provide a stable pH environment within the pH 1.5 to 4 or 8 to 14. The acidity regulator can be an alkaline substance selected from sodium carbonate, sodium bicarbonate, magnesium oxide, magnesium hydroxide, calcium carbonate and calcium hydroxide etc, while acidity regulator can be an acidic substance selected from citric acid, malic acid, acetic acid, glycine, phosphoric acid, lactic acid, ascorbic acid etc. The acidity regulator is preferably used which provides a pH of between 8 and 14.

In yet another embodiment of the above aspect, the composition may optionally contain multi-nutrients, electrolytes, macronutrients, amino acids and bioavailability enhancers such as enzymes and probiotics.

In still another embodiment of the above aspect, the composition is prepared by dry mixing the constituents and formulating the powder mixture into tablets, capsules, sachet or filling the powder mixture in a multidose container.

In still another embodiment of the above aspect, the composition is prepared by dry mixing and reconstituting in liquid medium to formulate the ready to drink shots, beverages or filling it in a multidose container.

Description of the Drawing

Figure 1 describes the study on degradation of a sample of creatine solution for neat creatine monohydrate and creatine monohydrate composition of Example 2.

Detailed Description of the Invention

Creatine is an energy generating amino acid-based metabolite produced in the liver, kidneys, and pancreas and commonly used by the muscles. Creatine in various forms has been used as a supplement to increase athletic performance. Studies have suggested that the degradation of creatine results from pH changes. At normal physiological pH, 10% of creatine has been suggested to convert to creatinine. It is believed that the main reason for complaints resulting from creatine consumption, namely, stomach cramps, edema, bloodedness and dehydration, is caused by the body's defense to this toxic metabolite compound creatinine.

It is believed that these complaints resulting from creatine consumption would be decreased when creatine is subjected to have a better stability when exposed to the acidic pH environment of the stomach, therefore leading to lesser creatinine conversion and more absorbable creatine.

The compositions of the present invention provide dual advantage via increasing the stability of creatine in vivo thus leading to reduced conversion to creatinine and enhanced absorption. The critical aspects to the enhanced efficacy of the compositions of the invention are that the creatine is protected from the acidic pH of the stomach by the acidity regulator and simultaneously, its absorption is enhanced by piperine present in the composition. Creatinine monohydrate is present in an amount of about 70% to about 99% by weight of the composition. Creatine monohydrate may be present in micronized form to enhance the solubility.

Piperine is obtained from Black pepper (Piper nigrum Linn). It is the dried fruit of Piper nigrum belonging to the family pipercea of the order Angiospermae. It has been used in human diet since ancient times and is one of the most widely used spices throughout the world. Black pepper or piperine treatment has been reported to enhance the bioavailability of a number of therapeutic drugs as well as phytochemicals via the modulation of metabolic enzymes and/or intestinal absorption. Piperine is considered to enhance the bioavailability of drugs and nutrients either by inhibiting the drug metabolizing enzyme, cytochrome P450 or by controlling the permeability of intestinal mucosa. In this process the pore size between the mucosal epithelial cells are increased, which in turn increases the permeability of intestinal mucosa resulting in higher rate of absorption. Thus the mechanism of action of piperine is said to be by promoting rapid absorption from gastrointestinal tract or by protecting the drugs and nutrients from being metabolized in its first passage through the liver after being absorbed from gastro-intestinal tract or by a combination of both. Black pepper extract is present in an amount that is sufficient to provide enough piperine to enhance the absorption of creatine monohydrate. Black pepper extract is present in an amount of about 0.01% to about 5% by weight of the composition, preferably from about 0.1 to about 2.0% by weight of the composition.

The compositions of the invention for oral consumption may be is prepared by a process of mixing the ingredients (a) creatine (monohydrate), (b) piperine as extract or powdered fruit), (c) acidity regulator; and optionally, (d) multi-nutrients, electrolytes, macronutrients and other bioavailability enhancers. The mixture is then formulation into tablets, capsules, sachet, powder packed into container, and ready to drink containers.

A degradation study was conducted to compare the stability of neat creatine monohydrate and composition of the invention in normal water. Creatinine monohydrate solution was prepared in water and kept aside at room temperature (37 °C). Similarly, a solution of composition of Example 2 was prepared in water and kept at room temperature. There was very less degradation of creatine in the solution of Example 2 composition in about 15 minutes compared to neat creatine solution in water. Thus, it can be said that the composition of the invention provide greater stability and thus would make creatine more bioavailable for absorption. [See Figure 1].

The present invention will be further described by having reference to the following examples, by way of illustration only.

Examples

Example 1
INGREDIENTS Quantity (grams)
Creatine Monohydrate 2.835
Black Pepper Extract 0.005
Glycine 0.1
Phosphoric acid 0.06
Total 3.000

Example 2
INGREDIENTS Quantity (grams)
Creatine Monohydrate 3.000
Black Pepper Extract 0.005
Magnesium salt 0.030
Total 3.035

Example 3
INGREDIENTS Quantity (grams)
Creatine Monohydrate 3.000
Magnesium salt 0.060
Black Pepper Extract 0.005
Protease 0.080
Amylase 0.050
Total 3.195

Example 4
INGREDIENTS Quantity (grams)
Creatine Monohydrate 2.795
Magnesium salt 0.08
Black Pepper Extract 0.005
Protease 0.07
Amylase 0.05
Total 3.000

Example 5
INGREDIENTS Quantity (grams)
Creatine Monohydrate 2.750
Potassium salt 0.100
Black Pepper Extract 0.005
Protease 0.050
Amylase 0.050
Probiotics (Bifidobacterium lactis, Bifidobacterium bifidum, Bifidobacterium longum, Bifidobacterium breve, Lacticaseibacillus casei, Lactobacillus acidophilus, Lacticaseibacillus paracasei, Ligilactobacillus salivarius, Lactiplantibacillus plantarum, Lactobacillus delbrueckii sub-sp. bulgaricus) 0.045
Total 3.000

Example 6
INGREDIENTS Quantity (grams)
Creatine Monohydrate 2.760
Magnesium salt 0.060
Black Pepper Extract 0.005
Protease 0.080
Amylase 0.050
Probiotics (Bifidobacterium lactis, Bifidobacterium bifidum, Bifidobacterium longum, Bifidobacterium breve, Lacticaseibacillus casei, Lactobacillus acidophilus, Lacticaseibacillus paracasei, Ligilactobacillus salivarius, Lactiplantibacillus plantarum, Lactobacillus delbrueckii sub-sp. bulgaricus) 0.045
Total 3.000

Example 7
INGREDIENTS Quantity (grams)
Creatine Monohydrate 2.760
Phosphoric acid 0.060
Black Pepper Extract 0.005
Protease 0.080
Amylase 0.050
Probiotics (Bifidobacterium lactis, Bifidobacterium bifidum, Bifidobacterium longum, Bifidobacterium breve, Lacticaseibacillus casei, Lactobacillus acidophilus, Lacticaseibacillus paracasei, Ligilactobacillus salivarius, Lactiplantibacillus plantarum, Lactobacillus delbrueckii sub-sp. bulgaricus) 0.045
Total 3.000

Example 8
INGREDIENTS Quantity (grams)
Creatine Monohydrate 2.750
Sodium salt 0.080
Black Pepper Extract 0.005
Protease 0.070
Amylase 0.050
Probiotics (Bifidobacterium lactis, Bifidobacterium bifidum, Bifidobacterium longum, Bifidobacterium breve, Lacticaseibacillus casei, Lactobacillus acidophilus, Lacticaseibacillus paracasei, Ligilactobacillus salivarius, Lactiplantibacillus plantarum, Lactobacillus delbrueckii sub-sp. bulgaricus) 0.045
Total 3.000

Example 9
INGREDIENTS Quantity (grams)
Creatine Monohydrate 3.000
Black Pepper Extract 0.005
Magnesium salt 0.030
Sodium salt 0.117
Potassium salt 0.172
Chloride Salt 0.176
Total 3.500

Example 10
INGREDIENTS Quantity (grams)
Creatine Monohydrate 3.000
Black Pepper Extract 0.005
Phosphoric acid 0.030
Sodium salt 0.117
Potassium salt 0.172
Chloride Salt 0.176
Carbohydrate (sucrose , lactose etc) 0.500
Total 4.000 ,CLAIMS:1. An improved oral composition of creatine wherein the composition comprises:
(a) creatine monohydrate;
(b) piperine;
(c) acidity regulator and optionally,
(d) multi-nutrients, electrolytes, macronutrients and bioavailability enhancers.
2. The oral composition of creatine as claimed in claim 1, wherein creatinine monohydrate is present in an amount of about 70% to about 99% by weight of the composition.
3. The oral composition of creatine as claimed in claim 1, wherein piperine is present as black pepper extract or pure piperine.
4. The oral composition of creatine as claimed in claim 3, wherein black pepper extract is present in an amount of about 0.01% to about 5% by weight of the composition, preferably from about 0.1 to about 2.0% by weight of the composition.
5. The oral composition of creatine as claimed in claim 1, wherein the acidity regulator is present in an amount sufficient to provide a stable pH environment within the pH 1.5 to 4 or 8 to 14.
6. The oral composition of creatine as claimed in claim 6, wherein the acidity regulator is an alkaline substance selected from sodium carbonate, sodium bicarbonate, magnesium oxide, magnesium hydroxide, calcium carbonate and calcium hydroxide.
7. The oral composition of creatine as claimed in claim 6, wherein the acidity regulator is an acidic substance selected from citric acid, malic acid, acetic acid, glycine, phosphoric acid, lactic acid, and ascorbic acid.
8. The oral composition of creatine as claimed in claim 1, wherein the acidity regulator is preferably used which provides a pH of between 8 and 14.
9. The oral composition of creatine as claimed in claim 1, wherein the composition optionally contains multi-nutrients, electrolytes, macronutrients, amino acids and bioavailability enhancers such as enzymes and probiotics.
10. The oral composition of creatine as claimed in claim 9, wherein the composition is prepared by dry mixing the constituents and formulating the powder mixture into tablets, capsules, sachet or filling the powder mixture in a multidose container.