JPH0624963A - Masked granulate - Google Patents

Abstract

PURPOSE:To obtain granulates capable of masking smell and taste of a material to be granulated because of property causing no dissolution in a mouth or stomach, capable of readily taking in, reduced in irritation or side effects on the stomach and high in deodorizing effects even when a raw material causing oral is added. CONSTITUTION:A material containing an odor component of garlic, etc., or a taste ingredient of a medicine, etc., is used as the material to be granulated and the material is double-coated with (A) a layer containing oils and fats and vehicles and (B) a layer containing a protein such as zein soluble in hydrous alcohol.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a peculiar odor of an odor component or a taste component contained in a medicinal substance, garlic or the like,
The present invention relates to granules with taste masking that are easy to take. More specifically, the granules can be used not only in the field of pharmaceuticals but also in the field of foods such as foods for specified health uses, and have no effect on the flavor of foods. Regarding granules.

[0002]

2. Description of the Related Art In general, pharmaceuticals such as Chinese herbs and intestinal stabilizers have a odor and taste peculiar to their active ingredients, and thus are difficult to take. Therefore, as a method for masking the odor and taste, a medicinal substance is encapsulated in a gelatin capsule.

However, the gelatin capsule itself has a peculiar odor, and it is not possible to completely wipe off the difficulty of drinking when taking the capsule. In addition, once the gelatin capsule is opened and exposed to the outside air to absorb moisture, the effectiveness of the drug in the capsule is reduced. On the other hand, if the capsules are exposed to the open air and dried, the capsules will crack and the appearance will deteriorate.
Air penetrates inside the capsule, again reducing the effectiveness of the drug. In addition, some pharmaceuticals have recently been used as food materials for specified health use, but in the field of foods, the use of capsules as a shape is not allowed to avoid confusion with pharmaceuticals. Therefore, gelatin capsules cannot be used.

As another masking method, a method of masking the bitterness of erythromycin with sodium sulfate (Japanese Patent Laid-Open No. 25425/1990) or 5
Examples include a method of masking by adding'-inosinic acid, 5'-guanylic acid and a sweetener (Japanese Patent Laid-Open No. 61-148129).

However, although the former is effective in reducing bitterness, it cannot be expected to have an effect on other tastes and odors, and cannot be used for food. The latter method is intended to reduce the difficulty of taking the drug by the synergistic effect of sweetness and umami derived from amino acids and sweeteners. Does not shut off. Therefore, depending on the type of the odorous component or the taste component, some may not be masked, and in the case of food, there is a problem that sweetness and umami affect the flavor of the food itself.

[0006]

SUMMARY OF THE INVENTION The present invention has been made in view of such circumstances, and an object thereof is to give an unpleasant odor without reducing the effectiveness of an odor component or a taste component. An object is to provide a granulated product containing an odor component or a taste component, which masks the taste and has an excellent versatility without affecting the flavor even when applied to foods and the like.

[0007]

Means for Solving the Problems The above object is characterized in that an agglomerate containing an odor component or a taste component is coated with two layers shown in (A) and (B) below. Is achieved by a masked granulation of (A) Oil-and-fat and excipient-containing layer (B) Hydrous alcohol-soluble protein-containing layer.

That is, the present inventors have proposed a masking method capable of masking the odor and taste of pharmaceuticals, foods, etc. without using a form such as the conventional gelatin capsules, and having excellent long-term storage stability. Study was carried out. as a result,
The odorous component or the taste component is (A) a layer containing fats and oils and a excipient (a long-term storage stabilizing layer) and (B) a hydrous alcohol-soluble protein-containing layer (dissolution preventing layer by saliva or gastric juice) When a granulated product having two layers is used, no unpleasant odor or taste can be felt during administration, and there is no contact with air during long-term storage, and a granulated product with excellent storage stability can be obtained. I found it. Furthermore, the granules thus obtained are themselves tasteless and odorless, and even if they are applied to the food field such as foods for specified health use, they can be used without affecting the flavor of foods. Completed the invention.

Next, the present invention will be described in detail. The agglomerate used in the present invention contains at least one of an odor component and a taste component, and various pharmaceuticals such as synthetic medicines, Chinese herbal medicines, or active ingredients for pharmaceuticals, garlic, onion, leek, etc. , Which are useful for living organisms, but are worried about their odor and taste, and these are appropriately used.

For example, as a medicinal substance, one having an extremely unpleasant bitterness such as a water-soluble drug thiamine chloride and an oil-soluble drug berberine chloride hydrochloride, and an unpleasant odor such as a liver water-soluble substance and creosote. The thing etc. are mentioned. Further, since the granulated product of the present invention is not dissolved by gastric juice, if the granulated product is aspirin or the like which may damage the stomach or cause damage if dissolved in gastric juice, an effect other than masking is also obtained. To be These may be used alone or in combination of several kinds. Moreover, the form is not particularly limited, and various forms such as powder, paste, extract, and crystal can be appropriately used.

Of the two layers that coat the granules, the (A) layer (hereinafter referred to as "A layer") for stabilizing the granules for a long period of time contains oil and fat and an excipient. Is used. In the present invention, the term “coating” also includes the case where the granules are mixed in the coating layer. First, as fats and oils, vegetable fats and oils such as palm oil, palm oil, soybean oil, rapeseed oil, and cacao butter and solid fats such as hardened oils obtained by curing them, rice wax, candelilla wax, edible wax such as honey wax, etc. Etc. The melting point of these oils and fats is preferably 30 to 45 ° C. from the viewpoint of uniform dispersibility and spreadability in a temperature range that does not impair the effectiveness of the granulated material.

[0012] Similarly, as the excipient used in the layer A, proteins and glucose, lactose, sucrose, starch and eggs made from potato, corn, rice, wheat and the like as raw materials, glucose, lactose, sucrose, Examples include sugars such as maltose, which may be used alone or in combination of several kinds.

Next, of the two layers that coat the granules, the (B) layer (hereinafter referred to as "B layer") that prevents the granules from dissolving in saliva or gastric juice is A hydrous alcohol-soluble protein is used. Examples of the hydrous alcohol-soluble protein include zein contained in corn, and vegetable or animal proteins derived from wheat, soybean, rice, collagen, gelatin and the like. These may be used alone or in combination of two or more. Further, for example, after treating zein with an alkali, a fraction such as a zein peptide having a molecular weight of 5,000 to 40,000 obtained by extracting with acetone is used, or the untreated zein and the zein peptide are used in combination. May be. Of these, zein is preferable because it becomes more insoluble. Further, about 10% by weight (hereinafter referred to as "%") of a water-soluble protein may be mixed with the hydrous alcohol-soluble protein and used.

In addition, in order to enhance the uniform dissolution and dispersibility of the hydrous alcohol-soluble protein in the B layer, if necessary,
It is better to use a plasticizer. Examples of the plasticizer include emulsifiers such as glycerin fatty acid ester, sucrose fatty acid ester, polyglycerin fatty acid ester, and sorbitan fatty acid ester, and glycerin and sugar alcohol. Among these, glycerin fatty acid ester is particularly preferable in terms of uniform dissolution and dispersibility of the hydrous alcohol-soluble protein and uniform coverage when the granule containing the odor component or the taste component is coated. The amount of the plasticizer added varies depending on the amount of the hydrous alcohol-soluble protein, but is preferably about 0.8% of the total weight of the layer B solution.

As for the coating of the above-mentioned layer A and layer B on the granulated material, either layer A or layer B may be coated first. When the layer A is first coated and then the layer B is coated, the dissolution resistance is more excellent, and the work efficiency in producing the granulated product is good. On the contrary, when the B layer is first coated and then the A layer is coated, a granulated product having a smaller particle size can be obtained.

The masked granulated product of the present invention can be produced, for example, as follows. That is,
In the case of coating the layer A first, first, the material to be granulated and the excipient are mixed, and fats and oils melted in a liquid state in advance are added thereto, and the mixture is stirred while keeping the temperature. The heat retention temperature is preferably 45 ° C. or lower, more preferably 35 to 45, from the viewpoint of uniform dispersibility of oil and fat and prevention of thermal denaturation depending on the type of granules.
It is better to set the temperature below ℃.

The amount of the oil / fat used is preferably 10 to 30% of the total weight of the layer A. If the fat and oil is less than 10%, the surface of the granulated product cannot be sufficiently covered with the fat and oil, and the long-term storage stability and dissolution resistance tend to deteriorate.
On the other hand, if it exceeds 30%, a slip phenomenon occurs during granulation, and granulation tends to be difficult. The amount of the excipient used may be set appropriately, but from the viewpoints of uniform dispersibility of fats and oils, suitability for coating fats and oils on granules, and suitability for granulation, 30 to 8 in the total weight of layer A
It is preferably 0%.

Next, the above mixture is supplied to a granulating device while being stirred, and granulated to obtain an A layer-coated granulated product. Examples of the granulating device include a granulator with a screen, an extruder, and the like, and a device equipped with a cooling means is preferable because the granulated product can be solidified quickly. At this time, it is desirable that the granules coated with the layer A be left to stand for a few hours at a temperature of 20 ° C. or less and aged before the subsequent coating with the layer B. If this stationary aging is insufficient, the A layer granules are likely to be bound together or softened during the subsequent B layer coating granulation, and the granulation suitability tends to deteriorate.

The layer A-coated granulated product thus obtained is coated with layer B by spraying, dipping or the like. That is,
First, a hydrous alcohol-soluble protein is dispersed and dissolved in hydrous alcohol. The hydrous alcohol used here preferably has an alcohol concentration of about 85 to 95%. That is,
Outside this range, the uniform dispersion and solubility of the hydrous alcohol-soluble protein in the hydrous alcohol tend to deteriorate. At this time, the ratio of the hydrous alcohol-soluble protein to the hydrous alcohol is preferably 6 to 14 hydrous alcohol to 1 hydrous alcohol-soluble protein in terms of uniform solubility and dispersibility. At this time, a plasticizer is added as needed.

Next, the step of applying the solution dispersed and dissolved in the hydrous alcohol to the surface of the granule coated with the layer A and drying it is repeated to form the layer B. Examples of the application method include spraying and dipping. For example, when spraying,
A rolling machine such as a revolving pan, a fluidized dryer, a centrifugal fluidized granulation dryer, or the like may be used.

The hydroalcoholic soluble protein in the total weight of the granules thus obtained is preferably 5 to 5
It is desirable that the content is 0%, more preferably 15 to 35%. If the hydroalcoholic protein content is less than 5%,
When it exceeds 50%, the texture in the mouth tends to deteriorate.

The granules containing the granules thus obtained may be taken as they are, or the granules may be tableted or formulated. Alternatively, foods such as health foods may be prepared by adding flavor components such as flavors and dairy products.

[0023]

As described above, the granulated product of the present invention comprises an A layer (long-term storage stability stabilizing layer) containing fats and oils and a shaping agent,
Since the granules are covered with the two layers B (dissolution-resistant layer) containing the hydrous alcohol-soluble protein, the granules are not dissolved by saliva and have an unpleasant odor or taste peculiar to the granules. You can take and eat without feeling.

Further, since it is not dissolved by gastric juice, aspirin or other substances having side effects on the stomach can be orally ingested as a granulated product. Further, even when stored in a usual packaging state, the effect of the active ingredient does not decrease, and the long-term stability is excellent. Moreover, since it is almost tasteless and odorless, it is a granulated product excellent in versatility without impairing the flavor of the food itself even when used in food such as health food.

The present invention will be specifically described below with reference to examples.

[Example 1] Thiamine hydrochloride powder 9 parts by weight (hereinafter referred to as "part") as a granulation object, 800 parts skimmed milk powder as a shaping agent and 50 parts glucose were mixed, and this mixture was mixed at 40 ° C. After adding 150 parts of palm oil and fat dissolved in the above and stirring, an A-layer-coated granulated product having a length of 1.2 to 2 mm was prepared with an extrusion granulator provided with a screen having a pore diameter of 0.8 mm, and this was 20 ° C. It was left to stand for 24 hours for aging.

Next, 300 parts of zein was added to 1952 parts of an ethanol aqueous solution (1,500 parts of ethanol, 452 parts of water) little by little and dissolved by stirring, and then 16 parts of glycerin fatty acid ester was added to obtain a coating solution. Then, using a centrifugal granulation dryer, the rotation speed of the rotor is 120 r
1500 parts of the coating solution was sprayed onto the layer A coated granulated product under the conditions of pm, product temperature 20 ° C., and blower 150 L / min, and dried to obtain a granulated product.

Comparative Example 1 A granulated product was obtained in the same manner as in Example 1 except that water was used instead of oil and fat.

Comparative Example 2 A granulated product was obtained in the same manner as in Example 1 except that 200 parts of palm oil and fat were applied without using the coating solution.

Each of the granules obtained in Example 1 and Comparative Examples 1 and 2 was contained in the mouth in an amount of 0.4 g, held for 30 seconds without chewing, and then swallowed. At this time, sensory evaluation was performed by 12 expert panelists on the masking effect on the odor or taste of the granulated material. The results are shown in Table 1.

[0031]

[Table 1] Evaluation criteria: The odor and taste of the granulated product are not felt ○ ………… Not felt △ ………… Slightly felt × ………… Strongly felt XX ………… Very strongly felt

From the above results, the granulated product of the present invention was a granulated product having an excellent masking effect.

[Examples 2 and 3] Granules were obtained in the same manner as in Example 1 except that the content of fats and oils (% by weight in the total weight of the layer A coated granules) was changed as shown in Table 2. It was The amount of skim milk powder was adjusted as the amount of fat and oil increased. The masking effect of the obtained granules was examined in the same manner as in Example 1. The above results are shown in Table 2.

[0034]

[Table 2]

From the results shown in Table 2, the masking effect was high even with the addition of 30% of oil and fat, the slipping phenomenon did not occur during granulation, and the granulation suitability was good.

Examples 5 to 9 Granules were prepared in the same manner as in Example 1 except that the content of zein in Example 1 was changed as shown in Table 3, and the masking effect was evaluated. The above results are also shown in Table 3.

[0037]

[Table 3]

From the results shown in Table 3, the zein content is 15%.
Above all, the granulated product exhibited good dissolution resistance, which was good.

[Examples 10 to 12] Granules were prepared in the same manner as in Example 1 except that the zein of Example 1 was replaced with each hydrous alcohol-soluble protein fractionated to be soluble in hydrous alcohol as shown in Table 4. It was prepared and the masking effect was evaluated. The results are shown in Table 4.

[0040]

[Table 4]

From the results shown in Table 4, the granulated product of the present invention using the hydrous alcohol-soluble protein was a granulated product having an excellent masking effect.

[Examples 13 to 16] Granules were prepared in the same manner as in Example 1 except that the thiamine hydrochloride of Example 1 was replaced with the granules shown in Table 5, and the masking effect was evaluated.
The results are also shown in Table 5.

[0043]

[Table 5]

From the results shown in Table 5, the masking effect was good even if the types of granules were different.

[Examples 17 and 18] Granules were prepared in the same manner as in Example 1 except that the thiamine hydrochloride of Example 1 was replaced with the granules shown in Table 6, and the masking effect was evaluated.
The results are also shown in Table 6.

[0046]

[Table 6]

From the results shown in Table 6, the masking effect was good even if the types of granules were different.

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Claims (1)

[Claims] 1. A masked granulated product, characterized in that the granulated product containing an odor component or a taste component is coated with two layers shown in the following (A) and (B). (A) Oil-and-fat and excipient-containing layer (B) Hydrous alcohol-soluble protein-containing layer.