JP6411049B2 - Jelly preparation - Google Patents

Description

  The present invention relates to a jelly agent containing thiamine or a derivative thereof. More specifically, the present invention relates to a jelly agent that has thiamine or a derivative thereof, has reduced bitterness, has good taste, and is easy to take. The present invention also relates to a jelly-like uncoated tablet using the jelly agent, and a jelly-like drop agent comprising a sugar coating or the like applied thereto.

  A jelly agent such as a jelly-like drop agent or an oral jelly agent is one of the dosage forms used in the pharmaceutical and food fields. It is a formulation molded into Since the jelly agent contains a jelly-like gelled product, there is an advantage that water is not necessary when taking and can be taken whenever necessary. Furthermore, since the jelly agent can be finely broken, it is easy to take without depending on the size of the preparation, and can be easily taken even by children and elderly people with low chewing ability. (Compliance) can also be improved (see, for example, Non-Patent Document 1).

  On the other hand, the vitamin B group is widely used as a water-soluble vitamin in drinks and the like. However, the vitamin B group generally has a bitter taste, and in particular, thiamine (vitamin B1), its derivatives, and salts thereof (hereinafter sometimes referred to as “thiamines”) have a very strong taste. It is known to have a peculiar property that it has a bitter taste and remains in the mouth for a long time after taking. Therefore, the preparation containing thiamines has a problem that its bitterness is remarkably expressed and pain is accompanied by taking.

  Conventionally, a method for masking the bitter taste of thiamines has been reported. For example, Patent Document 1 reports that the bitter taste of a thiamine derivative can be reduced by using a herbal extract having a bitter taste together with the thiamine derivative in a drinking liquid composition. However, with the method of Patent Document 1, it is still difficult to sufficiently suppress the specific bitterness of thiamines.

  In addition, jelly preparations are usually designed so that a large amount of nutrients can be ingested by taking a small amount, so that the nutritional components are contained at a higher concentration than the drinking liquid composition. Therefore, the jelly agent containing thiamines has a higher concentration of thiamines than in the case of a drinking liquid composition, and the taste deterioration due to thiamines becomes more serious. Therefore, the bitterness masking technology disclosed in Patent Document 1 that discloses a drinking liquid composition cannot be diverted to reduce the bitterness of thiamines contained in a jelly agent.

  Conventionally, it is known that when a component having a bitter taste is formulated, the bitter taste can be masked by applying a coating such as sugar coating to the formulation. However, since the jelly agent is finely chewed in the mouth and taken, even if a coating is applied to the jelly agent containing thiamines, it is difficult to suppress the bitter taste felt when chewed in the mouth.

  Against the background of such conventional technology, it is desired to develop a formulation technique that reduces the bitterness of jelly agents containing thiamines and makes them easy to take with good taste.

Monthly Pharmaceutical Affairs, Vol. 37, no. 11, p2381385 (1995)

JP-A-10-150959

  An object of the present invention is to provide a jelly agent that contains thiamines but has reduced bitterness, good taste, and easy to take.

  The present inventor has intensively studied to solve the above problems. As a result, in a jelly agent containing thiamines, a sweetener having a solubility in water at 25 ° C. of 50% or less is blended, and the water content is 35% by weight. It was found that the bitterness attributed to thiamines can be effectively suppressed by setting to the following, and the taste is good and easy to take. The present invention has been completed by further studies based on such knowledge.

That is, this invention provides the invention of the aspect hung up below.
Item 1. (A) at least one thiamine selected from the group consisting of thiamine, derivatives thereof, and salts thereof, and (B) a sweetener having a solubility in water at 25 ° C. of 50% or less and having a water content A jelly agent, which is 35% by weight or less.
Item 2. Item 2. The jelly agent according to Item 1, wherein the (A) thiamine is thiamine sulfate and / or thiamine hydrochloride.
Item 3. Item 3. The jelly agent according to Item 1 or 2, wherein the sweetener (B) is at least one selected from the group consisting of sucralose, thaumatin, aspartame, and acesulfame K.
Item 4. Item 4. The jelly agent according to any one of Items 1 to 3, which is a jelly-like uncoated tablet.
Item 5. Item 5. A jelly-like drop agent comprising the jelly agent according to Item 4.

  Although the jelly agent of the present invention contains thiamines, its specific bitterness can be sufficiently reduced, and even if it is finely crushed in the mouth, the bitterness specific to thiamines is hardly felt and has a good taste. Can show. As described above, the jelly agent of the present invention has a good taste and is easy to take, and can further improve the taking performance (compliance).

  The jelly agent of the present invention comprises (A) at least one thiamine selected from the group consisting of thiamine, a derivative thereof, and a salt thereof, and (B) a sweetener having a solubility in water at 25 ° C. of 50% or less. The water content is 35 wt% or less. Hereinafter, the jelly agent of the present invention will be described in detail.

(A) Thiamines The jelly agent of the present invention contains at least one selected from the group consisting of thiamine, derivatives thereof, and salts thereof as thiamines.

  Thiamine derivatives may be any physiologically acceptable and known as vitamin B1 derivatives, such as fursultiamine, octothiamine, bisbenchamine, benfotiamine, thiamine pyrophosphate, dicetiamine, chicotiamine Bisbutiamine, prosultiamine and the like. These thiamine derivatives may be used alone or in combination of two or more.

  The salt of thiamine and / or a derivative thereof is not particularly limited as long as it is physiologically acceptable, and examples thereof include hydrochloride, nitrate, sulfate ester salt and the like. Thiamine derivatives and / or salts thereof may be used singly or in combination of two or more.

  In the jelly agent of the present invention, as thiamines, thiamine, its derivatives, and salts thereof may be used alone or in combination of two or more. Among these thiamines, preferably thiamine, fursultiamine, benfotiamine, and salts thereof; more preferably thiamine nitrate, thiamine hydrochloride, fursultiamine hydrochloride, fursultiamine, benfotiamine; particularly preferred Includes thiamine nitrate and thiamine hydrochloride.

  In the jelly agent of the present invention, the content of thiamines is appropriately set according to the daily dose, etc., for example, 0.01 to 6% by weight, preferably 0.05 to 3% by weight. Can be mentioned. In the jelly agent of the present invention, even if it contains a high content of thiamines, the bitterness peculiar to thiamines can be reduced and the taste can be improved. More preferably, the content of the class is 0.1 to 2.0% by weight, particularly preferably 0.5 to 1.5% by weight.

(B) Sweetener whose solubility in water at 25 ° C. is 50% or less The jelly agent of the present invention contains a sweetener whose solubility in water at 25 ° C. is 50% or less. In the present invention, “solubility (25%) in water at 25 ° C.” is the maximum concentration (% by weight) at which a sweetener can be dissolved in water at 25 ° C. Hereinafter, in this specification, “solubility (%) in water at 25 ° C.” may be simply referred to as “solubility”.

  The sweetener having a solubility of 50% or less is not particularly limited as long as it is physiologically acceptable. For example, sucralose (solubility 28.3%), thaumatin (solubility 20%), aspartame (solubility 1%) Acesulfame K (solubility 27%), erythritol (solubility 35%) and the like. These sweeteners may be used alone or in combination of two or more.

  Among the sweeteners having a solubility of 50% or less, a sweetener having a solubility of 0.1 to 30% is preferably used from the viewpoint of more effectively reducing the bitter taste of thiamines.

  More specifically, as a sweetener having a solubility of 50% or less, sucralose, thaumatin, aspartame, and acesulfame K are preferable, and sucralose is more preferable from the viewpoint of more effectively reducing the bitter taste of thiamines. And thaumatin. In the jelly agent of the present invention, in particular, the bitter taste of thiamines can be more effectively reduced by using sucralose and thaumatin in combination. When sucralose and thaumatin are used in combination as a sweetener having a solubility of 50% or less, these ratios are not particularly limited, but for example, thaumatin is 5 to 500 parts by weight per 100 parts by weight of sucralose, preferably 20 to 500 weight part, More preferably, 50-300 weight part is mentioned.

  In the jelly agent of the present invention, the content of the sweetener having a solubility of 50% or less is, for example, 0.01 to 3% by weight, preferably 0.03 to 1% by weight, more preferably 0.05 to 0.5% by weight. %. By including a sweetener having a solubility of 50% or less at such a content, the bitter taste of thiamines can be more effectively reduced.

Water content The jelly agent of the present invention has a water content of 35% by weight or less. In such a jelly agent having a low water content, the bitterness peculiar to thiamines can be reduced by blending the aforementioned sweetener with low solubility. Although not intended to be limited in interpretation, the jelly agent of the present invention is thought to reduce the bitter taste of thiamines by utilizing the property that sweeteners with low solubility tend to diffuse into an environment where the concentration is low. It is done. That is, in a jelly preparation having a low water content, a thiamine having a high solubility and a sweetener having a low solubility are included, so that when a jelly preparation in the mouth comes into contact with saliva at the time of taking, the sweetener having a low solubility is more It is considered that the taste of the sweetener having a lower solubility is more easily felt than the bitter taste of thiamines, because it is easier to diffuse into saliva than the fruit and the diffusion rate is increased. Of course, the present invention is not construed as being limited based on the mechanism.

  The water content of the jelly agent of the present invention may be 35% by weight or less, but from the viewpoint of more effectively reducing the bitter taste of thiamines, preferably 5 to 30% by weight, more preferably 10 to 10%. 25% by weight.

Gelling agent The jelly agent of the present invention is formed into a gel using a gelling agent. The gelling agent used in the jelly agent of the present invention is not particularly limited as long as it is physiologically acceptable. For example, agar, pectin, gelatin, carrageenan, xanthan gum, locust bean gum, alginic acid and its Salt, gellan gum, native gellan gum, curdlan, tamarind gum, glucomannan and the like can be mentioned. These gelling agents may be used individually by 1 type, and may be used in combination of 2 or more type. Among these viewpoints, agar and / or pectin are preferable, and a combination of agar and pectin is more preferable.

  The content of the gelling agent in the jelly agent of the present invention may be appropriately set according to the type of gelling agent used and the like, for example, 0.1 to 5.0% by weight, preferably 1.0. -4.0 weight%, More preferably, 2.0-3.0 weight% is mentioned.

Other sweeteners The jelly agent of the present invention may contain a sweetener having a solubility of more than 50%, if necessary, in addition to the above components. A sweetener having a solubility of more than 50% is useful as a base of a jelly agent and can further reinforce the good taste of the jelly agent.

  The sweetener having a solubility exceeding 50% is not particularly limited as long as it is physiologically acceptable. For example, sucrose, fructose, lactose, water candy, fructose-glucose liquid sugar, xylitol, sorbitol, maltitol , Reduced palatinose, oligosaccharide (for example, malto-oligosaccharide, isomalto-oligosaccharide, galactooligosaccharide, inulo-oligosaccharide, fructooligosaccharide, xylo-oligosaccharide), polydextrose, dextrin, indigestible dextrin, reduced indigestible dextrin and the like. These sweeteners may be used alone or in combination of two or more. Among these sweeteners, sucrose and water candy are preferably used from the viewpoint of improving the jelly strength and producing a good chewy jelly agent, and further providing a better taste. Can be mentioned.

  In the jelly agent of the present invention, the content of the sweetener having a solubility of more than 50% may be appropriately set according to the type of sweetener used, etc. For example, the total amount of the sweetener having a solubility of more than 50% 10 to 90% by weight, preferably 20 to 90% by weight, and more preferably 30 to 87.9% by weight. In addition, when water candy is used as a sweetener having a solubility of more than 50%, the content of water candy in terms of dry solid content is set to satisfy the above range.

Other additive components Furthermore, the jelly agent of the present invention can contain various additive components as needed in addition to the components described above. Such an additive component is not particularly limited as long as it can be used in medicines and foods. For example, vitamin B2, vitamin B6, vitamin B12, vitamin C, vitamin A, vitamin D, vitamin E, vitamin K, Vitamins such as niacin, pantothenic acid, folic acid, biotin, and lycopene; stomachic agents such as betaine hydrochloride, carnitine chloride, and betanecol chloride; Herbal extracts such as clove, aloe, hop, kakkonto, katsushiyu, saikokueda, maoyu, shosaikoto, koseiryu, etc .; aspirin, acetaminophen, etenzamid, ibuprofen, salicylamide, etc. Antipyretic analgesics; expectorants such as noscapine hydrochloride and noscapine; acrino , Berberine chloride, creosote, tannic acid, scopolamine hydrobromide, methyl atropine bromide, papaverine hydrochloride, ethyl aminobenzoate, and the like; dextromethorphan hydrobromide, tipepidine hydrobenzoate, dihydrocodeine phosphate, etc. Vasodilators; antihistamines such as isothibenzyl hydrochloride, diphenylpyraline hydrochloride, diphenhydramine hydrochloride, chlorpheniramine maleate, alimemazine tartrate; antitussives such as dextromethorphan hydrobromide, tipepidine hibenzate, dihydrocodeine phosphate; calcium, sulfur Minerals such as magnesium, zinc, selenium, iron; proteins such as soy protein, egg white powder, whey protein; glycine, alanine, arginine, aspartic acid, cystine, phenylalanine, taurine, Amino acids such as liptophan; fatty acids such as EPA, DHA, linoleic acid, γ-linolenic acid, α-linolenic acid; starch such as corn starch, potato starch, wheat starch, rice starch, tapioca starch; caramel pigment, gardenia pigment, Anthocyanin, Anato, Paprika, Safflower, Scarlet, Flavonoid, Cochineal, Amaranth, Erythrosine, Allara Red AC, New Coxin, Phloxine, Rose Bengal, Acid Red, Tartrazine, Sunset Yellow FCF, Fast Green Pigments such as FCF, brilliant blue FCF, indigo carmine; flavors such as flavors and essences of various fruits; citric acid and salts thereof, malic acid and salts thereof, tartaric acid and salts thereof, acetic acid and salts thereof, lactic acid and salts thereof, salt , Glutamic acid and its salts, mirin, vinegar, natural fruit juice, seasonings such as cuts and powdered products such as vegetables, fruits and marine products; mushrooms such as agaricus, shiitake extract, litchi and yamabushitake or extract thereof; preservative; pH adjustment Agents: dietary fiber, royal jelly, propolis, honey, chondroitin sulfate, glucosamine, ceramide, hyaluronic acid and other functional materials. These additive components may be used alone or in combination of two or more. Moreover, about content of these additive components, it sets suitably according to the kind of additive component to be used, the use of a jelly agent, etc.

Production Method The jelly agent of the present invention can be produced according to a general method for producing a jelly agent. Specifically, a raw material solution is prepared by adding a predetermined amount of each component to a predetermined amount of heated water to solubilize the gelling agent. Next, after pouring this raw material liquid into a predetermined container or mold, it is allowed to stand, cooled to room temperature, gelled, and dried to a predetermined moisture content as necessary to obtain the jelly agent of the present invention. Manufactured.

Uses / Forms The jelly agent of the present invention is provided as a jelly-like drop agent, an oral jelly agent or the like, and a jelly-like drop agent is preferred. In this specification, “jelly-form drop agent” means a jelly-form uncoated tablet formed by drying a composition gelled by a gelling agent, or a coating obtained by coating the jelly-form uncoated tablet It is a lock. The “oral jelly agent” is a preparation formed by gelling a composition gelled with a gelling agent into a non-flowable gel.

  When the jelly preparation of the present invention is made into a jelly-like uncoated tablet, its shape is not particularly limited and may be any tablet shape that is usually employed in pharmaceuticals and foods. Examples include shapes.

  When the jelly agent of the present invention is provided as a jelly-like drop agent, the jelly-like uncoated tablet may be left as it is, but in consideration of ease of administration, the jelly-like uncoated tablet is coated. The coated tablet is preferable.

  When making a jelly-like drop into a coated tablet, the coating may be either a sugar-coating coating using sucrose or a film coating with a water-soluble polymer. From the viewpoint of further improving easiness, sugar coating is preferable. When the jelly-like drop agent is a coated tablet, the weight ratio between the jelly-like uncoated tablet and the coating part is not particularly limited. For example, the coating part is 10 to 200 parts by weight per 100 parts by weight of the jelly-like uncoated tablet. Any degree is acceptable.

  About the method of coating a jelly-like uncoated tablet, it can carry out in accordance with the method of the film coating generally used and the sugar-coating coating. For example, in the case of sugar coating, a binding solution (an aqueous solution containing a thickening polysaccharide) is added to the surface of the jelly-shaped uncoated tablet as necessary while rotating the sugar-coated bread containing the jelly-shaped uncoated tablet. After uniform coating, the sugar-coating material for forming the sugar-coating coating is placed in a rotating sugar-cooking pan, whereby the sugar-coating can be applied to the jelly-like uncoated tablets.

  The sugar coating raw material used for the sugar coating is not particularly limited, and those used in general sugar coating for pharmaceuticals and foods can be used. For example, sucrose, fructose, lactose, water candy, sugar alcohol (Eg, erythritol, xylitol, sorbitol, maltitol, reduced palatinose), oligosaccharide (eg, maltooligosaccharide, isomaltooligosaccharide, galactooligosaccharide, inulooligosaccharide, fructooligosaccharide, xylooligosaccharide), polydextrose, dextrin, indigestible dextrin And saccharides such as reduced indigestible dextrin. These saccharides may be used alone or in combination of two or more. Furthermore, the sugar coating material may contain various additives exemplified above as necessary.

  The jelly agent of the present invention is provided as a pharmaceutical or food in the form of a jelly-like drop agent, an oral jelly agent or the like. When provided as a medicine, it may be used as an internal medicine for the purpose of nutritional supplementation or alleviation of specific symptoms. When provided as food, functional food, food for the sick, etc. It may be used as food.

  EXAMPLES Hereinafter, although an Example demonstrates this invention concretely, this invention is not limited only to the range of a following example.

1. Production of jelly-like uncoated tablets Jelly-shaped uncoated tablets having the compositions shown in Tables 1 to 6 were produced. Specifically, a predetermined amount of agar, purified sucrose, and water candy were added and dissolved while heating water to 90 ° C. Next, an aqueous solution in which pectin, thiamine nitrate or thiamine hydrochloride, and a sweetener were dissolved by heating was added in a state heated to 80 ° C. to prepare a raw material solution. In addition, the said raw material liquid contains about 0.1 to 2 times the amount of water by weight ratio with respect to the total solid content of a containing component. The obtained raw material liquid was dispensed into a disk-shaped starch mold, allowed to stand and cooled to room temperature, and dried to gel until the water content reached a predetermined value shown in Tables 1-6. In addition, the fluctuation | variation of the weight by the change of the moisture content was adjusted with the addition amount of the water candy to add. Thereafter, the starch mold was removed to produce a jelly-like uncoated tablet (weight per one 0.56 g).

2. Taste evaluation of jelly-like uncoated tablets In order to reproduce the chewing conditions in the mouth, 9 pieces obtained by dividing each jelly-shaped uncoated tablet into 4 pieces were poured into 50 ml of water at 40 ° C., left for 1 minute, and then divided. The jelly-like uncoated tablet was taken out to prepare an exudate. The taste of the obtained exudate was evaluated by 10 evaluation monitors. Specifically, 1 ml of exudate was placed on the tongue to determine the bitterness. Judgment of bitterness was evaluated by conducting a questionnaire by Visual Analogue Scale with bitterness being “1” and not bittering being “10”. The questionnaire results were averaged, and the evaluation results were summarized by rounding off the first decimal place.

3. Evaluation results The results obtained are shown in Tables 1-6. As shown in Table 1, a jelly-like uncoated tablet having a water content of 40 or 50% by weight has a strong bitterness even if a sweetener (sucralose, thaumatin, aspartame, acesulfame K) having a solubility of 50% or less is contained. I felt it. Moreover, even when the water content is 35% by weight or less, sweetness is hardly felt when it contains only sucrose and water candy as a sweetener, or when it further contains saccharin (solubility 66%), and is derived from thiamines. However, it was difficult to take. On the other hand, when a sweetener (sucralose, thaumatin, aspartame, acesulfame K) having a water content of 35% by weight or less and a solubility of 50% or less is contained, the bitter taste is remarkably reduced. The taste was easy to take. In particular, when the water content was 10 to 25% by weight, the bitterness reducing effect was very high, and the taste was extremely easy to take.

Claims (3)

(A) at least one thiamine selected from the group consisting of thiamine, derivatives thereof, and salts thereof, and (B) at least one sweetener selected from the group consisting of thaumatin, aspartame, and acesulfame K And a water content of 35% by weight or less.   (A) It contains at least one thiamine selected from the group consisting of thiamine, derivatives thereof, and salts thereof, and (B) sucralose, and has a water content of 10 to 35% by weight. Jelly agent. The jelly agent according to claim 1 or 2 , wherein the (A) thiamines are thiamine sulfate and / or thiamine hydrochloride.