JPH114666A - Foaming agent composition for supplying magnesium - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a magnesium-supplying foaming agent composition light in weight, extremely good in taste, easy in intake and administration and excellent in stability, uniformity and practicality by including magnesium sulfate, a foaming agent component and a neutralizing agent component in a specific ratio. SOLUTION: This magnesium-supplying foaming agent composition comprises (A) 0.6-6 wt.% (as magnesium) of magnesium sulfate, (B) 10-35 wt.% of a foaming agent such as potassium bicarbonate, and (C) 15-60 wt.% of a neutralizing agent component comprising 20-30 wt.% of citric acid and L-tartaric acid and 5-25 wt.% of L-ascorbic acid. The composition preferably further contains 0.2-13 wt.% of potassium carbonate and 0.2-13 wt.% of potassium carbonate, and the composition is preferably prepared in the form of tablets, granules, powders or capsules.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a magnesium supplemented foaming composition, and more particularly to a magnesium supplemented foaming composition capable of supplying magnesium to a living body and having improved pharmaceutical properties.

[0002]

2. Description of the Related Art Magnesium (Mg) is distributed in bone in an amount of 50% or more in a living body, and is distributed in a parenchyma tissue, particularly in an intracellular fluid, and plays a physiological function indispensable for maintaining life. It is known that when this Mg is insufficient, the living body falls into various pathological states. For example, when Mg is deficient, the patient suffers from depression, causing anxiety, slowing of emotions, and further mental disorders such as excitement and mental confusion. The M
It is known that if the intake of g continues to be inadequate, the feeling of fatigue becomes remarkable, and the body and mind become unwell. In addition, there have been reports of cases in which it is difficult to speak or write.

[0003] Mg also has an antagonistic function with calcium (Ca).
In addition, the metabolism of a may be disturbed, and the Ca may be deposited on blood vessels and visceral tissues, causing arteriosclerosis, kidney stones, and the like.
It has also been reported that the Mg deficiency also interferes with the correct metabolism of large amounts of minerals including sodium (Na) and potassium (K), triggers the onset of cardiovascular diseases, and contributes to sudden death.

[0004] The above Mg is contained abundantly in beans such as brown rice, soybeans, red beans and the like, but as the spread of refined processed foods, instant foods, etc. is accelerated, especially in the postwar period, the shortage of intake of the Mg is serious. Has become a major problem. In particular, the target intake of Mg for adults is set at 300 mg per day, but the current daily intake per adult is about 20 mg.
It is said to be about 0 mg, and there is clearly a lack of intake.
It is known that with this insufficient intake, Mg is lost due to various mental stresses and drinking in modern society.

[0005] Further, as described above, due to the antagonistic function sharing between Mg and Ca, they have an appropriate intake balance, and it is generally said that Mg / Ca = 1/2. However, in recent years, the lack of Ca intake by the Japanese people has become serious, and great attention has been paid to the increase in the intake of Ca.
Developed to curry, sprinkle and other processed foods C
Although the addition of a has become widespread, such Ca supplements are not considered at all with regard to their Mg content.
/ 4 to 1/5, resulting in a marked decrease in the intake balance. This imbalance causes a cardiovascular disease, particularly an ischemic heart disease. Thus, the increase in Ca intake is important in itself, but at the same time, it must be balanced with the Mg intake.

As described above, modern people suffer from severe Mg deficiency due to lack of intake, loss due to stress, etc., and imbalance in Mg / Ca intake balance due to Ca supplementation, and suffer from the various diseases described above. You are in danger.

On the other hand, as a food additive containing Mg, magnesium oxide, magnesium chloride, magnesium carbonate, magnesium sulfate, and magnesium phosphate have been conventionally known. Of these, magnesium oxide is defined by the Food Sanitation Law. , Must not be used except for the purpose of food processing and for the purpose of adsorption, and magnesium carbonate must not be used as a swelling agent except in the case of food processing. There is a regulation that the residual amount in the food must be 0.5% by weight or less. Magnesium chloride and magnesium sulfate are known as main components of bitterness, and both have the disadvantage of exhibiting strong bitterness, and at present there is no use as a Mg supplement.

[0008]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a new Mg replenishing composition which is effective for the deficiency of Mg and correction of imbalance with Ca intake, etc. The composition is in the form of a foamed product that is highly uniform, has excellent uniformity and stability in the form of the preparation, is easy to ingest and take (easy to drink, has excellent taste, etc.), and can supply a sufficient amount of Mg stably. To provide.

The inventors of the present invention have conducted intensive studies for the above purpose, and have found that magnesium sulfate is used as a Mg-containing compound at a predetermined ratio as an essential component, and a predetermined amount of a foaming agent component, a neutralizing agent component, and the like are added thereto. It has been found that a composition obtained by adding and blending into a foamed preparation meets the above-mentioned object, and the present invention has been completed.

[0010]

According to the present invention, magnesium sulfate is 0.6 to 6% by weight as Mg, and a blowing agent 10 is used.
There is provided an Mg-supplemented blowing agent composition, characterized in that it is an effervescent formulation containing -35% by weight and 15-60% by weight of neutralizing agent.

The pharmaceutical composition of the present invention has improved water dispersibility, solubility, ease of ingestion, etc. based on the form of a foaming agent. In particular, the Mg-supplemented foaming agent composition of the present invention has excellent storage stability in the form of tablets, granules, capsules, etc., has good solubility and dispersibility, and is neutralized simply by putting it in water at the time of use. Can easily and uniformly dissolve and disperse the magnesium sulfate contained in the formulation in water with the generation of carbon dioxide by this method, and this solution has a very easy to take (oral administration) and delicious characteristics, and By taking the drug, a sufficient amount of Mg can be supplied and absorbed to the living body. Therefore, according to its use, healing and improvement effects of Mg deficiency and the like can be expected, and modern humans who are liable to Mg deficiency can be ingested and replenished with sufficient Mg to avoid the risk of falling into the Mg deficiency. It has the effect of maintaining a healthy state.

[0012]

DETAILED DESCRIPTION OF THE INVENTION In the composition of the present invention, it is essential to use magnesium sulfate as Mg. The magnesium sulfate has good solubility in water, particularly when it is in the form of a foaming agent, and has low deliquescence and hygroscopicity,
It has the advantage of being stable in itself. In addition, this inherently has bitterness itself, but according to the composition of the present invention, the mineral balance is adjusted based on the combination of the foaming agent component, the neutralizing agent component, the stabilizer and the like, and thus Is softened,
The taste can be swelled and rounded.

[0013] However, magnesium chloride, which is conventionally known as an Mg source, has good solubility in water, but is deliquescent and difficult to handle, and has a very bitter taste. It is not suitable for taking. Magnesium carbonate and magnesium oxide have the advantage of being tasteless and odorless, but there are legal restrictions on the use of food, and it is difficult to use them in amounts that satisfy the purpose of Mg supplementation. It is insoluble, and there is a disadvantage that its solubility in water cannot be made sufficient even by reaction with an acid (neutralizing agent). Compounds as other Mg sources, for example, magnesium citrate, magnesium acetate, magnesium gluconate, magnesium aspartate, magnesium nitrate, magnesium silicate, magnesium silicate, etc., generally have poor solubility in water, There are drawbacks such as prolongation of dissolution time, generation of precipitates, generation of turbidity in the dissolution solution, and the Mg content is often relatively small, and it is difficult to add the required amount to a preparation of a predetermined size. Furthermore, there is a disadvantage that bitterness is remarkable and taste is bad.

The magnesium sulfate as an essential component in the present invention is not particularly limited, but can be advantageously used in the present invention in a commonly available form, generally in a powder form having a particle size of 350 μm or less. The compounding amount is Mg
It is good to be selected from the range of 0.6 to 6% (% by weight, hereinafter the same), preferably 1 to 4%.

The composition of the present invention has a form of a foaming agent. The foaming agent contains the above-mentioned specific Mg compound at a predetermined ratio, and also contains a predetermined amount of a foaming agent component and a neutralizing agent component. Is required. The foaming agent component used here is selected from potassium bicarbonate, potassium carbonate, sodium bicarbonate, sodium carbonate, magnesium carbonate, and calcium carbonate. These can be used alone or in combination of two or more. Can also.

As the neutralizing agent component, an acidic compound capable of generating carbon dioxide by neutralizing the foaming agent component compound is used. The acidic compound typically includes, for example, organic acids such as L-tartaric acid, citric acid, fumaric acid, L-ascorbic acid, gluconic acid, acetic acid, lactic acid, and malic acid.

The mixing ratio of the above-mentioned foaming agent component and neutralizing agent component to the composition of the present invention is such that when the obtained foamed pharmaceutical composition of the present invention is dissolved in water, the solution is acidic, and particularly the pH is about 3.
The ratio is preferably such that the acidity is about 6 to 5.1, preferably about 4.0 to 4.7. More specifically, the above ratio is preferably selected from the range of 10 to 35% of the foaming agent component and 15 to 60% of the neutralizing agent component.

In particular, sodium carbonate as a foaming agent component is 0 to 23%, preferably 5 to 15%, sodium bicarbonate is 0 to 35%, preferably 10 to 250%, potassium carbonate is 0.2 to 13%, Preferably 2-10%, potassium bicarbonate 0-19%, preferably 5-15%, calcium carbonate 0.2-13%, preferably 2-10%,
Magnesium carbonate is preferably selected from a range of about 0.5% or less.

The present inventors have found that, together with calcium carbonate, potassium carbonate which can be used as the above-mentioned foaming agent component also functions as a magnesium sulfate stabilizer (bittering inhibitor). Therefore, in the Mg replenishing blowing agent composition of the present invention, it is important to add and mix such potassium carbonate and calcium carbonate, whereby the intended effect of the present invention is achieved. Particularly preferred compositions of the composition of the present invention to which these are added are as follows.

Magnesium sulfate (as Mg) 0.6-6% by weight Sodium hydrogen carbonate (as Na) 0-10% by weight Potassium carbonate (as K) 0.1-7.3% by weight Calcium carbonate (as Ca) 0 However, the total amount of the sodium hydrogen carbonate, potassium carbonate, and calcium carbonate as the foaming component is 10% by weight or more.

The neutralizing agent component is selected from the range of 15 to 60%, preferably 20 to 50%,
-20-30% of tartaric acid and / or citric acid, and L-
Most preferably, ascorbic acid is used in the range of 5 to 25%. By combining the foaming agent component and the neutralizing agent component, the excellent effects expected according to the present invention are achieved.

The composition of the present invention comprises the above-mentioned components as essential components, and various other commonly known additive components,
For example, sugars, sugar alcohols, sweeteners and the like, excipients,
A binder, a disintegrant, a lubricant, a thickener, a surfactant, an osmotic pressure regulator, an electrolyte, a fragrance, a dye, a pH regulator, and the like can be appropriately added and blended as necessary. Examples of the additives include starches such as wheat starch, potato starch, corn starch, dextrin, sugars such as sucrose, glucose, fructose, maltose, xylose, and lactose; sugar alcohols such as sorbitol, mannitol, maltitol, and xylitol. , Coupling sugars, transglycosides such as palatinose, excipients such as calcium phosphate and calcium sulfate, starch, saccharides, gelatin, gum arabic, dextrin, methylthicellulose, polyvinylpyrrolidone, polyvinyl alcohol, hydroxypropylcellulose, xanthan gum , Pectin, gum tragacanth, casein, alginic acid and other binders or thickeners, leucine, isoleucine, L-
Lubricants such as valine, sugar ester, hardened oil, stearic acid, magnesium stearate, talc, macrogol, Avicel, CMC, CMC-Na, CMC-Ca
Disintegrants, such as polysorbate, surfactants such as lecithin, dipeptides such as aspartame and alitame, and other sweeteners such as stevia and saccharin. In consideration of the above, an appropriate amount can be appropriately selected and used.

Further, an appropriate amount of vitamins can be added to the preparation of the present invention. The vitamins also include L-ascorbic acid (vitamin C) as the above-described neutralizing agent, which functions as an antioxidant.

Particularly preferred representative compositions of the Mg-supplemented blowing agent composition of the present invention include the following.

Magnesium sulfate 0.6 to 6% by weight Blowing agent component 10 to 35% by weight Citric acid 20 to 30% by weight L-ascorbic acid 5 to 25% by weight Sugar such as sugar or sugar alcohol 8 to 40% by weight Aspartame 0.5-1% by weight of flavoring agent, coloring agent, etc. Suitable amount The composition of the present invention can be produced according to a usual pharmaceutical production technique. For example, the preparation of the present invention in the form of an effervescent tablet can be produced by weighing and mixing a predetermined amount of each component, and directly following a powder compression method, a dry or wet granulation compression method, or the like.

The composition of the present invention thus obtained is generally administered orally depending on its form of preparation. In particular, an effervescent tablet can be made into a beverage form suitable for oral administration simply by putting it into water. The administration (dose) amount is appropriately determined according to the age, sex, body weight, purpose of ingestion and the like of the living body to which this is to be applied, and is not particularly limited.
Tablets 1-2 of the tablet of the present invention prepared to about 1.5 to 6.0 g
The tablet may be dissolved in 100 to 300 ml of water at a time and taken.

The composition of the present invention is not particularly limited to the above-mentioned tablets, and may be in the form of, for example, granules, powders, capsules, etc. as long as it has the above-mentioned composition range.
These are all suitable forms that can be dissolved and dispersed in water and taken.

According to the present invention, there is provided a new Mg-supplemented blowing agent composition, which has the advantage that it is stable, has excellent storage stability, is easily dissolved, and is easy to take. In addition, the composition of the present invention is capable of safely supplying and absorbing sufficient Mg to a living body by taking the composition, has an effect of treating or improving Mg deficiency and the like, and has a feature of being low in calories. Moreover, the foaming agent composition of the present invention generally has a good taste, and has a characteristic of having a refreshing and mild taste by masking the bitterness of Mg and the like.

[0029]

The present invention will be described in more detail with reference to the following examples. In the examples, “parts” and “%” indicate “parts by weight” and “% by weight” unless otherwise specified.

[0030]

Example 1 The following components were mixed, and the mixture was tableted by a direct powder compression method to produce a foamed preparation of the present invention (K ^{+ 3} mEq, Mg ²⁺
8 mEq and Na ⁺ 12 mEq, 100 mg per tablet, Mg
(Content 2%).

Granulated sugar 28% L-ascorbic acid 10% Citric anhydride 23% Magnesium sulfate (trihydrate) 14% Magnesium carbonate 0.4% Sodium bicarbonate 18% Potassium carbonate (anhydrous) 4% Sweetener trace amount Flavor trace amount 100% in total (4.8 g in total)

[0032]

Test Example 1 Stability Test The stability of the pharmaceutical composition of the present invention obtained in Example 1 was adjusted in the same manner without adding potassium carbonate (hereinafter referred to as a comparative pharmaceutical composition). A comparative test was performed as follows.

That is, each tablet was separately packaged in an aluminum blister package (silica gel sheet included), stored in a thermostatic chamber (50 ° C., 2 weeks or 37 ° C., 3 months), and tested for the effect of stability on the following evaluation items. did.

(1) Swelling of Packaging Material The swelling of packaging material was visually determined as the amount of gas generated in the packaging material.

(2) Discoloration of tablet The change with time of the color of the tablet surface was visually determined using the tablet before storage start (stored at 4 ° C after tableting) as a standard.

(3) Dissolution time The tablets were put into about 140 ml of cold water at 8 to 9 ° C., and the time required for complete dissolution was measured.

(4) Change in taste Two tablets were compared by a sensory test with the tablet before the change with the lapse of time (preserved in a cold place at 4 ° C. after tableting), and the results were expressed by the following five-point evaluation.

1 point; no change 2 points; slight change but no problem 3 points; change 4 points; clear change 5 points; significant change The results are shown in Table 1 below. ), Table 2 (discoloration of tablets),
The results are shown in Table 3 (dissolution time) and Table 4 (change in taste).

[0039]

[Table 1]

[0040]

[Table 2]

[0041]

[Table 3]

[0042]

[Table 4]

[0043]

Example 2 The following components were mixed, and the mixture was tableted by a direct powder compression method to prepare a foamed preparation of the present invention (K ^{+ 3} mEq, Mg 2 ⁺
8 mEq and Na ⁺ 9 mEq, 100 mg per tablet, Mg
(Content 2%).

Granulated sugar 27% L-ascorbic acid 10% Citric anhydride 23% Magnesium sulfate (trihydrate) 14% Sodium hydrogen carbonate 15% Potassium carbonate (anhydrous) 4% Calcium carbonate 2.5% Sweetener trace amount Flavor trace amount Coloring agent trace total 100% (total 5g)

[0045]

Test Example 2 Stability Test The stability of the pharmaceutical composition of the present invention obtained in Example 2 was adjusted in the same manner without adding calcium carbonate (hereinafter referred to as a comparative pharmaceutical composition). A comparative test was performed as follows.

That is, each tablet was individually packaged in an aluminum blister package (silica gel sheet inclusion), stored in a thermostatic chamber (50 ° C., 2 weeks), and the effect of stability was described in the above Test Example 1 (1). Each of the test items of swelling of the packaging material, (2) discoloration of the tablet, (3) dissolution time and (4) change in taste was similarly tested.

(2) Regarding the discoloration of the tablet, a color difference meter (Color Ace MODEL TC-1, manufactured by Tokyo Denshoku Co., Ltd.)
Was used to evaluate the change over time in the color of the tablet surface in NBS units (ΔE = color difference) and Lab, using the tablet before the start of transformation (stored at 4 ° C. after tableting) as a standard. The guideline of the relationship with the difference in visual perception is, for example, as follows.

NBS unit Difference in sensation 0-0.5 Slightly 0.5-1.5 Slightly 1.5-3.0 Sensitive 3.0-6.0 Prominent 6.0- 12.0 Greatly 12.0 or more Significantly, the results are shown in Table 5 (bulging of packaging material), Table 6 (discoloration of tablets),
The results are shown in Table 7 (dissolution time) and Table 8 (change in taste).

[0049]

[Table 5]

[0050]

[Table 6]

[0051]

[Table 7]

[0052]

[Table 8]

[0053]

Examples 3 to 5 In the same manner as in Example 1, an Mg-supplemented blowing agent composition of the present invention was prepared from the components shown in Table 9 below.

[0054]

[Table 9]

The preparations of the present invention obtained in each of the examples are effective as K and Mg supplement foods or pharmaceuticals have a delicious taste (cool feeling, etc.) and can easily supplement the above K and Mg. Particularly, the preparation of the present invention in the form of an effervescent preparation obtained in Examples 1 to 5 is provided in a dry state,
The stability of the contents is excellent, and the taste and nutritional effects are also excellent. Furthermore, these preparations dissolve and disperse promptly when they are put into water, and have excellent solubility in which the solution becomes totally transparent.There is no discomfort due to coloration or the like due to the liquidity after dissolution, and And the like, the color of the liquid at the time of drinking can be arbitrarily adjusted, and its appearance is also preferable. In addition, the preparation of the present invention is lightweight, highly stable, convenient for transportation and the like, and is preferable for market distribution. In addition, the preparation of the present invention has a very good taste,
Bitterness and the like were masked and had a refreshing and mild taste.

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 9/14 A61K 33/06 ADD 9/16 A23L 2/00 F 9/46 2/40 9/50 A61K 9/14 L33 / 06 ADD

Claims (4)

[Claims] 1. A magnesium supplement which is a foaming preparation containing 0.6 to 6% by weight of magnesium sulfate as magnesium, 10 to 35% by weight of a foaming agent component and 15 to 60% by weight of a neutralizing agent component. Blowing agent composition. 2. A neutralizing agent comprising citric acid and L-tartaric acid 2
The effervescent preparation according to claim 1, which is 0 to 30% by weight and 5 to 25% of L-ascorbic acid. 3. Potassium carbonate 0.2 to 13 as a stabilizer
The effervescent preparation according to claim 1 or 2, further comprising 0.2% to 13% by weight of calcium carbonate. 4. The effervescent preparation according to claim 1, which is in the form of a tablet, granule, powder or capsule.