KR20150128157A - Taste-masked granules containing vitamin C - Google Patents

Abstract

The present invention provides vitamin C granules which can be taken in megadoses by masking tastes thereof, a medicine comprising the same for oral administration, and a method for producing the vitamin C granules and the medicine. More specifically, the present invention relates to vitamin C granules which comprise: (a) a core including vitamin C or a mixture of vitamin C and xylitol; and (b) a coating layer consisting of butter or butter powder, enzyme-treated stevia, and one or more components selected from a group selectively comprising a sweetener, a colorant, and spices. According to the present invention, the vitamin C granules have outstanding appealing ability by masking unique sour tastes of vitamin C and is also excellent in terms of enhancing convenience of drinking.

Description

Taste-masked granules containing vitamin C < RTI ID = 0.0 >

The present invention relates to a vitamin C granule containing a vitamin C granule, particularly a vitamin C containing a high content of vitamin C, and having a greatly improved new taste of vitamin C, an oral pharmaceutical preparation containing the same, and a process for producing the same.

Vitamin C is a six-carbon lactone. Plants and most animals can synthesize vitamin C in the body, but humans, primates, guinea pigs, large bats, several species of birds, and fish are synthesized It must be ingested in the form of food. Vitamin C includes both reduced ascorbic acid and oxidized form dehydroascorbic acid, both of which are interchangeable.

Vitamin C is used as a coenzyme in various enzymatic reactions in vivo and is involved in the synthesis of collagen, a main protein that constitutes connective tissues such as skin, skeleton, blood vessels and cartilage. When the amino acids proline and lysine are hydrolyzed to form hydroxyproline and hydroxylysine, vitamin C plays a role in the reduction of iron in the hydroxylase. The collagen will retain its tissue. In addition, vitamin C has an antioxidant function. Vitamin C has an antioxidant activity that removes free radicals such as reactive oxygen species (ROS) and reactive nitrogen species (RNS) . In particular, tissues susceptible to damage from free radicals such as eyes, neutrophils, and semen are known to have a relatively high content of vitamin C, and besides they are also involved in the saving action of vitamin E by preventing initiation of lipid peroxidation such as low density lipoprotein (LDL) . In addition, vitamin C radicals have a relatively long half-life as compared to other antioxidants and are thus recognized as stable antioxidants. In addition, vitamin C promotes absorption of vegetable iron that is not bound to hemoglobin by converting the iron to a reduced form in the small intestine.

Therefore, vitamin C, which plays an important role in vivo, must be consumed in a certain amount. The average amount of vitamin C required by men and women is 75 mg / day, and the recommended intake is 100 mg / day. Vitamin C source foods are easy to break down due to storage, cooking and processing methods due to the easily oxidized nature of fresh vegetables and fruits, and vitamin C, and vitamin C, which is not consumed as food, should be supplemented in the form of nutritional supplements .

However, Vitamin C has a unique sour taste, depending on the individual differences in the severity of the tongue can cause a degree of pain to the extent. Therefore, conventionally, in order to consume a large amount of vitamin C at a time, it has been common to prepare it in a liquid form or to tablet it. However, the liquid phase has a disadvantage that it is bulky and has a high possibility of corruption, has disadvantages such as inconvenience of storage and distribution, and has a disadvantage that it is difficult to take without water, because it is deteriorated in terms of digestion and absorption ability.

Accordingly, there is a need for a granular vitamin C which overcomes the disadvantages of such liquid formulations and tablet formulations and at the same time minimizes the taste of the product and minimizes the rejection of sourness.

Korean Patent Registration No. 10-1055229 (Registration date: 2011. 08. 02)

Accordingly, it is an object of the present invention to provide a vitamin C granule which is capable of taking a large amount of food at the same time with its taste masked, an oral pharmaceutical preparation containing the vitamin C granule, and a process for producing the same.

In one aspect, the present invention provides vitamin C granules having (a) a core comprising vitamin C and (b) a coating layer comprising butter.

More preferably, the present invention relates to a composition comprising (a1) vitamin C, or (a2) a core comprising a mixture of vitamin C and xylitol, and (b1) butter or butter powder, (b2) enzyme-treated stevia, and (b3) A vitamin C granule comprising a coating layer composed of at least one selected from the group consisting of a colorant and a fragrance.

The inventors of the present invention have found that when a core containing vitamin C is coated with butter, vitamin C of a granular formulation can be produced which is highly effective in shielding the taste characteristic of vitamin C, thus completing the present invention. The present inventors have tested various taste-masking coating materials to improve / mask the taste of vitamin C, but it has been difficult to achieve the desired purpose without using a very large amount of coating material. That is, when a large amount of the coating material is used, the taste of vitamin C can be shielded. However, in this case, the dosage is very large, the preparation time is long, and the manufacturing cost is increased. On the other hand, when butter was used as a coating material, it was able to effectively improve the fresh taste of vitamin C while using a small amount of vitamin C content.

In addition, the present invention is based on a very remarkable synergistic effect that when the enzyme-treated stevia is used together with the coating material in addition to the butter mentioned above, the content of the coating material can be greatly reduced and the fresh taste of vitamin C can be improved very effectively.

Furthermore, still more preferably, the core further comprises xylitol together with vitamin C, and in addition to butter, an enzyme-treated stevia and optionally other additives such as flavoring agents, sweeteners, coloring agents and the like are added to the composition for coating the core, It was confirmed that the butter was significantly improved in the sensory quality of the vitamin C granules by treating it in the form of butter powder (i.e., butter mixed powder).

In the present invention, the butter plays a major role in exerting an effect of shielding the characteristic taste of vitamin C, and is a main component of the core coating composition. The butter may contain 2.5 to 10% by weight, preferably 3 to 10% by weight, more preferably 3 to 7% by weight, and most preferably 3 to 6% by weight based on the total weight of the vitamin C granule. When the butter is contained in an amount of less than 2.5% by weight based on the total weight of the vitamin C granules, it is not possible to fully shield the vitamin C-specific sour taste. The butter may be contained in an amount of 40 wt% or more, preferably 50 wt% or more, and most preferably 50 to 70 wt%, based on the total dry weight of the core coating composition. Including a core coated with butter is less than 40% by weight, based on the weight of the total dry composition can not sufficiently shield a distinctive sour vitamin C.

In the present invention, the butter may be selected from, for example, spread dairy products, vegetable purees or nuts (such as peanut butter and almond butter), fruit butter (e.g. apple butter, mango butter, etc.) Any butter that is commonly used in the art, such as a fat product in a state (e.g., shea butter, carita butter, leek butter, cocoa butter, etc.) or a mixture thereof can be used without limitation. In the present invention, the fat component of the butter may be selected from non-tempering fats comprising a butter equivalent or a butter modifier, and a butter substitute or a butter substitute.

The butter according to the present invention can be preferably used in the form of a butter powder, which means butter which is slightly fats removed and pulverized into powder, preferably butter, lactose, sodium caseinate, glycerin fatty acid ester, lecithin And a tablet salt. The content of butter contained in the butter powder may be at least 50 wt%, more preferably at least 60 wt%, and still more preferably at least 65 wt%, based on the total weight of the butter powder. The butter powder may contain at least 3.5 wt.%, Preferably 3.5 to 10 wt.%, More preferably 4 to 8 wt.%, And most preferably 4 to 6 wt.% Of the total weight of the vitamin C granules. If the butter powder is contained in an amount of less than 3.5% by weight based on the total dry weight of the vitamin C granules, it is not possible to fully shield the vitamin C-specific sour taste. The butter powder may be contained in an amount of 55 wt% or more, preferably 60 wt% or more, more preferably 60 to 90 wt%, and most preferably 60 to 70 wt%, based on the total dry weight of the core coating composition. If the butter powder is contained in an amount of less than 55% by weight based on the total dry weight of the core coating composition, the acidic taste of vitamin C can not be sufficiently shielded.

In the present invention, an enzyme-treated stevia may be further included in the core coating composition in addition to the butter. The present inventors have found that synergistic effect of coating the vitamin C-containing core with an enzyme-treated stevia in addition to the butter to the core coating composition significantly improves the sensory quality of the vitamin C granules as well as the specific taste of the vitamin C Respectively.

The enzyme-treated stevia is obtained by purifying α-glucosyl stevioside and α-glucosyl beadsioside A produced by acting α-Glucosyltransferase (α-glucosyltransferase) or the like on Stevia extract. Or may be manufactured and used by methods known to those skilled in the art.

The total weight ratio of butter and enzyme-treated stevia included in the present invention is preferably 20 wt% or less, more preferably 15 wt% or less, still more preferably 10 wt% or less, and most preferably 5 to 10 wt% to be. When the total weight ratio of butter and enzyme-treated stevia contained in the present invention exceeds 20% by weight based on vitamin C, there is a problem that the total volume of granules becomes too large and the coating layer becomes too thick. The enzyme-treated stevia and butter contained in the coating layer of the vitamin C granule according to the present invention may be included in any mixing ratio capable of exhibiting the synergistic effect of the present invention. Preferably, the enzyme-treated stevia butter is 1: 0.8-3, 1: 0.8 - 2, and most preferably 1: 1 - 1.5. Enzyme-treated stevia: When the weight ratio of butter is less than 1: 0.8, it is difficult to expect a sufficient taste shielding effect, and when it exceeds 1: 3, coating is difficult.

The composition for core coating may optionally further contain a small amount of a component which is generally used in the art and which does not affect the object of the present invention, for example, a sweetener, a coloring agent, a perfume or the like. More specifically, the core coating composition of the present invention may contain, for example, a sweetener, and the sweetener may include tau martin, saccharin, sucralose, aspartame, crystalline fructose, steviol glycosides or a mixture of two or more thereof But is not limited thereto.

Further, the present invention is based on the fact that the coating layer of the vitamin C granules of the present invention does not contain a conventional hydrophilic polymer for coating is more effective for the taste shielding purpose of the present invention. Therefore, the hydrophilic polymer (for example, a coating polymer such as hydroxypropylmethylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, vinylpyrrolidone-vinyl acetate copolymer, polyethylene glycol, etc.) Is contained in an amount of 4% by weight or less, preferably 3% by weight or less, more preferably 2% by weight or less, even more preferably 1% by weight or less based on the dry weight of the vitamin C granule precursor, It does not use the coating polymer conventionally used for the above-mentioned taste masking.

In the present invention, the core coating composition coated on the core is referred to as a coating layer. The weight ratio of the coating layer to the core of the vitamin C granules according to the present invention is preferably 5 to 20% by weight, more preferably 7 to 20% 15% by weight, still more preferably 9 to 13% by weight, most preferably 10 to 12% by weight. When the weight ratio of the vitamin C granules to the core-coating layer is less than 5% by weight, the taste shielding effect is not sufficiently achieved. When the weight ratio exceeds 20% by weight, the total volume of the granules becomes too large and the coating layer becomes too thick, .

Various methods commonly used in the art can be used for coating the core coating composition according to the present invention on the core, for example, a top spray, a bottom spray, a tangential method with centrifugal force added, (Bottom spray). A bottom spray fluid bed granulator may preferably be used for the bottom spray. Specific methods such as spray rate, temperature and spray pressure using a bottom spray fluid bed granulator are disclosed in Korean Patent Application No. Nos. 10-2010-0063533. ≪ / RTI >

The core of the vitamin C granules according to the present invention includes vitamin C. The vitamin C may be contained in a liquid or solid phase, and preferably, it may be contained as a solid phase, more preferably as a powder.

Preferably, the core of the vitamin C granule according to the present invention may further contain xylitol in addition to vitamin C. According to a specific embodiment of the present invention, the inclusion of a mixture of vitamin C and xylitol in the core of the vitamin C granules significantly improved the sensory quality. Xylitol may comprise up to 10% by weight, more preferably up to 8% by weight, even more preferably from 3 to 7% by weight, most preferably from 4 to 6% by weight, based on the weight of the vitamin C granulate.

Alternatively, the core may further comprise various components within a small amount that do not adversely affect the activity and flavor improving effects of vitamin C.

The vitamin C granules according to the present invention can be used for various purposes, for example, as a cosmetic composition, a food composition or a pharmaceutical composition. In particular, the vitamin C granules according to the present invention may be advantageously used as a food composition or a pharmaceutical composition for oral administration in that a large amount of vitamin C granules can be shielded from the sour taste peculiar to vitamin C.

In another aspect, the present invention provides an oral pharmaceutical preparation comprising the vitamin C granules as an active ingredient.

The pharmaceutically acceptable carrier may include a pharmaceutically acceptable carrier. The pharmaceutically acceptable carrier means a carrier or a diluent which does not disturb the biological activity and does not inhibit the biological activity and properties of the administered ingredients. If necessary, conventional additives such as antioxidants, buffers, bacteriostats, fragrances, sweeteners, and natural carbohydrates may be further included. The sweetener is not particularly limited, but tau Martin, saccharin, sucralose, aspartame, crystalline fructose, steviol glycoside or a mixture of two or more thereof may be used. The natural carbohydrate is not particularly limited, but includes, for example, monosaccharides such as glucose and fructose, disaccharides such as maltose, polysaccharides such as dextrin and cyclodextrin and sugar alcohols such as xylitol and sorbitol , Erythritol, etc.) and the like can be used.

The pharmaceutical preparations can be administered in single or multiple doses in a pharmaceutically effective amount. In addition, the pharmaceutical preparation may be administered in combination with other pharmaceutical preparations, and may be administered separately or sequentially or simultaneously with conventional pharmaceutical preparations.

The pharmaceutical preparations are administered in a pharmaceutically effective amount. The pharmaceutically effective amount means an amount sufficient to treat or prevent a disease, disorder, and / or symptom at a reasonable benefit / risk ratio applicable to medical treatment or prevention, and an effective dosage level is determined by the activity of the drug, , The body weight, the health, the sex, the sensitivity of the patient to the drug, the time of administration, the route of administration, and the rate of excretion of the pharmaceutical agent of the present invention used, the time of treatment and the factors including the pharmaceutical formulations used or co- May be determined according to factors well known in the medical arts.

The present invention also provides a food composition comprising the above vitamin C granules as an active ingredient.

The above-mentioned vitamin C granules can be used as food additives, food additives and food additives. When the vitamin C is included in the food, the addition amount is not particularly limited, but it may be 1 to 10% by weight, preferably 3 to 5% by weight based on the weight of the final food. However, in the case of long-term intake intended for health and hygiene purposes or for the purpose of controlling health, the amount of vitamin C contained in the food may be less than the above range, and as long as there is no problem in terms of safety, Or more.

Foods that may include the vitamin C granules include tablets, granules, rings, capsules, gums, tea, and vitamin complexes.

There are no particular limitations on the ingredients that are included in the food other than the above-mentioned vitamin C granules as an active ingredient, and may include various ingredients that can be included in ordinary foods. For example, various nutrients, electrolytes, flavors, An auxiliary component such as an acid or a salt thereof, alginic acid or a salt thereof, an organic acid, a protective colloid thickener, a pH adjuster, a stabilizer, a preservative, glycerin, an alcohol or a perfume. In addition, a sweetener or a natural carbohydrate may be added. The sweetener is not particularly limited, but tau Martin, saccharin, sucralose, aspartame, crystalline fructose, steviol glycosides, or a mixture of two or more thereof may be used. The natural carbohydrate is not particularly limited, but includes, for example, monosaccharides such as glucose and fructose, disaccharides such as maltose, polysaccharides such as dextrin and cyclodextrin and sugar alcohols such as xylitol and sorbitol , Erythritol, etc.) and the like can be used.

In another aspect, the present invention provides a method for producing a vitamin C granule which is shielded from the characteristic flavor of vitamin C and has excellent sensory quality, or a method for shielding the characteristic taste of vitamin C and improving the sensory quality.

More specifically, the method comprises dissolving butter in water to prepare a coating solution; And vitamin C to the coating solution.

This method will be described step by step as follows.

(S1) a step of dissolving butter in water to prepare a coating liquid

The water is suitable for sterilization and / or living body, and the water includes purified water, saline, sterilized water, Ringer's solution or buffered saline.

In addition to butter, components which may be contained in the coating composition described above (especially including enzyme-treated stevia, preferably) may be further mixed with water to prepare a coating solution, which is preferably a butter powder.

(S2) spraying the coating solution onto a vitamin C, or a mixture of vitamin C and xylitol

Vitamin C, or vitamin C and the xylitol mixture is sprayed onto the surface of the mixture (S1) to form a coating layer. Occasionally, a coating layer is formed on a core containing vitamin C, and a coating layer is formed on a core containing both vitamin C and xylitol.

The vitamin C is not particularly limited, but preferably vitamin C powder can be used, and xylitol is also not particularly limited thereto, but xylitol powder can be preferably used. According to a specific embodiment of the present invention, the vitamin C powder and the xylitol powder are crushed and mixed in the fluidized bed, and then the coating liquid is sprayed.

In addition to the above steps, additional coating, filling and / or packaging steps may be added.

According to the present invention, there is provided a vitamin C granule which is shielded from taste and which can be massively ingested at once, an oral pharmaceutical preparation containing the same, and a method of producing the same, whereby the vitamin C granule according to the present invention has excellent sensory properties, And it has an excellent effect.

Hereinafter, embodiments of the present invention will be described in detail to facilitate understanding of the present invention. However, the embodiments according to the present invention can be modified into various other forms, and the scope of the present invention should not be construed as being limited to the following embodiments. Embodiments of the invention are provided to more fully describe the present invention to those skilled in the art.

< Example  1> Production of vitamin C granules

Vitamin C granules were prepared in the following formulation ratios as shown in Table 1 below.

Ingredients Compounding ratio (unit:% by weight) Vitamin C (ascorbic acid) powder 85.51 Xylitol powder 6.24 Butter powder
(Processed butter 65.0%, lactose 28.7%, casein sodium 4.5%, glycerin fatty acid ester 0.6%, lecithin 0.6%, refined salt 0.6%) 5.00 Enzyme treatment Stevia 3.00 Lemon incense 0.25 Sum 100.0

(1) Raw material crushing

 In order to increase the surface area of vitamin C powder and xylitol powder, two crystalline materials were pulverized and sorted into 100 mesh sieve or less.

(2) Preparation of coating liquid

The butter mixture powder and enzyme - treated stevia were dissolved in purified water (15% of the total working amount) to prepare a coating solution.

(3) mixing

 The undifferentiated vitamin C powder and xylitol powder were put into a fluidized bed coater and lightly suspended and mixed for about 3 to 5 minutes.

(4) Spraying of coating liquid

The coating solution was sprayed onto the powder which had been mixed. At this time, the spraying pressure was 1.5 to 3.0 bar, the spraying speed was 40 to 80 rpm, and the internal material temperature was 40 to 49 ° C.

(5) Drying

After the spraying of the coating liquid was completed, hot air drying and cold air drying were performed for about 5 to 10 minutes. Hot air drying was carried out at 40 ~ 45 ℃ for about 3-5 minutes, and cold air drying was conducted at 25 ℃ for 3 ~ 5 minutes.

(6) mixing

 The cooled powder was mixed with lemon fragrance and mixed in the fluidized bed for about 3 minutes.

(7) Selection and packaging

18 mesh sieves and packed with vitamin C granules in a stick.

< Example  2> Analysis of taste shielding effect of vitamin C granules

As a result of administering to 10 adult males and 10 adult females in order to confirm the degree of taste masking of vitamin C prepared according to Example 1, there was no problem in that the specific vitamin C sour taste was effectively shielded and consumed.

< Example  2-5> Comparison of taste shielding effect of vitamin C granules

The taste shielding effect of the vitamin C granules was compared and analyzed by varying the ingredients contained in Example 1 and the vitamin C granules. The compounding ratio of the components contained in the vitamin C granules was as shown in Table 2. Vitamin C granules were prepared in the same manner as described in Example 1.

Raw materials Example 2 Example 3 Example 4 Example 5 Vitamin C powder 85.51 85.51 85.51 85.51 Xylitol powder 6.24 6.24 - - Butter powder - 8.00 5.00 14.24 Enzyme treatment Stevia 8.00 - 9.24 - Lemon incense 0.25 0.25 0.25 0.25 Sum 100 100 100 100

In order to compare the taste shielding effect of the vitamin C granules according to the prepared Example 2-5 and Example 1, 20 persons who were experienced in evaluating the taste shielding effect were selected and repeated training And evaluated the degree of aftertaste shielding. 40 points scoring method was used for the evaluation.

The results are as shown in Table 3 below. From these results, it was confirmed that the syneresis effect of the butter powder, the enzyme-treated stevia and the xylitol powder can shield the sour taste of vitamin C with excellent effect.

Example 1 Example 2 Example 3 Example 4 Example 5 Taste shielding
effect 38 10 17 26 14

Claims (15)

(a) a core comprising vitamin C; And
(b) Vitamin C granules having a coating layer containing butter. The vitamin C granule according to claim 1, wherein the butter is a butter powder consisting of butter, lactose, sodium caseinate, glycerin fatty acid ester, lecithin and tablet salt. [Claim 2] The vitamin C granule according to claim 1, wherein the vitamin C granule comprises 4% by weight or less of hydrophilic polymer based on the total dry weight of the vitamin C granule. The vitamin C granule according to claim 1, wherein the weight ratio of the butter to the total weight of the vitamin C granules is 2.5 - 10 wt%. The vitamin C granule according to claim 1, wherein the coating layer further comprises an enzyme-treated stevia. 6. The vitamin C granule according to claim 5, wherein the coating layer comprises enzyme-treated Stevia butter at a weight ratio of 1: 0.8-3. 6. The vitamin C granule according to claim 5, wherein the total weight ratio of vitamin C to butter and enzyme-treated stevia is 20% by weight or less. The vitamin C granule according to claim 1, wherein the weight ratio of the core to the coating layer is 5 to 20% by weight. The vitamin C granule according to claim 1, wherein the coating layer is a bottom spray coating layer. An oral pharmaceutical preparation comprising the vitamin C granule of claim 1 or 5 as an active ingredient. 11. The oral pharmaceutical preparation according to claim 10, wherein the oral pharmaceutical preparation further comprises xylitol. (a1) vitamin C, or (a2) a core comprising a mixture of vitamin C and xylitol; And
(b1) a butter or butter powder, (b2) an enzyme-treated stevia, and (b3) optionally a coating layer consisting of at least one selected from the group consisting of sweeteners, colorants and perfumes. Dissolving the butter in water to prepare a coating solution;
And spraying the coating liquid onto a vitamin C or vitamin C and xylitol mixture. 14. The method according to claim 13, wherein the manufacturing method uses a bottom spray fluid bed granulator. 14. The method according to claim 13, wherein an enzyme-treated stevia is further added to the coating solution.