JP2016069292A - Chewable tablets - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a chewable tablet which can suppress a powdery feel and rough feel at the time of chewing and can give a good melting feeling in the mouth, while it contains carnitine and/or a salt thereof, and dimethylpolysiloxane and/or a derivative thereof.SOLUTION: A powdery feel and rough feel at the time of chewing can be suppressed and can give a good melting feeling in the mouth by formulating a chewable tablet in combination with (A) carnitine and/or a salt thereof, (B) dimethylpolysiloxane and/or a derivative thereof, (C) silicon dioxide, and (D) sugar alcohol.SELECTED DRAWING: None

Description

  The present invention relates to chewable tablets. More specifically, the present invention includes carnitine and / or a salt thereof, and dimethylpolysiloxane and / or a derivative thereof, and suppresses the powdery and rough feeling at the time of mastication, and has a good mouth melt feeling. The resulting chewable tablet.

  Carnitine and its salts are known to be effective in the treatment of chronic gastritis and the like, which have a digestive function activation enhancing action and a decrease in digestive tract function, and are widely used as gastrointestinal drugs. Carnitine and its salts also have the function of transporting long-chain fatty acids to intracellular mitochondria in vivo, and play an important role in the metabolism of neutral fat, and can also be used as dietary supplements. Has been.

  On the other hand, dimethylpolysiloxane is a kind of silicone and is used in the fields of foods, cosmetics, pharmaceuticals and the like as additives such as lubricants, coating agents and ellimont agents. Furthermore, since dimethylpolysiloxane can reduce surface tension and exert an antifoaming effect, it is caused by gas in the gastrointestinal tract such as belching, stomach fullness, flatulence, etc. in the field of food and medicine for internal use. It is also used for preventing or treating abdominal symptoms.

  Thus, carnitine and its salts, and dimethylpolysiloxane have beneficial effects, so when they are formulated in combination, enhanced digestive function activation, promotion of neutral fat metabolism, gastric abdominal symptoms It is expected that effects such as prevention or treatment can be provided in combination.

  Conventionally, a pharmaceutical formulation in which carnitine or a salt thereof and dimethylpolysiloxane are used in combination has been proposed. Specifically, in Patent Document 1, by using carnitine or a salt thereof and dimethylpolysiloxane or a derivative thereof in combination, a hygroscopic reducing action on a solid preparation for internal use containing carnitine or a salt thereof is provided. It is disclosed that it can have an effect of improving the change in fluidity over time.

JP 2014-24793 A

  Since chewable tablets are taken after being chewed or dissolved in saliva, it is important to have a good mouth-melting feeling compared to other preparation forms. However, as a result of the inventor's study, as in Patent Document 1, when carnitine or a salt thereof and dimethylpolysiloxane or a derivative thereof are used in combination to form a chewable tablet, the powderiness and the rough feeling at the time of chewing are obtained. It became clear that there was a problem that it appeared prominently and the feeling of melting in the mouth was significantly worsened. Therefore, in order to put chewable tablets containing carnitine or a salt thereof and dimethylpolysiloxane or a derivative thereof into practical use, a formulation technology that can suppress powderiness and a rough feeling during chewing and obtain a good mouth-melting feeling is developed. It will be necessary.

  Therefore, the present invention has carnitine and / or a salt thereof and dimethylpolysiloxane and / or a derivative thereof, and suppresses the powderiness and the rough feeling at the time of mastication, so that a good mouth melting feeling can be obtained. It is an object to provide chewable tablets.

  The present inventor has intensively studied to solve the above problems, and (A) carnitine and / or a salt thereof and (B) dimethylpolysiloxane and / or a derivative thereof together with (C) silicon dioxide and (D) It has been found that by formulating a chewable tablet in combination with sugar alcohol, the powderiness and the rough feeling at the time of chewing can be suppressed, and a good mouth-melting feeling can be obtained. The present invention has been completed by further studies based on this finding.

That is, this invention provides the invention of the aspect hung up below.
Item 1. A chewable tablet comprising (A) carnitine and / or a salt thereof, (B) dimethylpolysiloxane and / or a derivative thereof, (C) silicon dioxide, and (D) a sugar alcohol.
Item 2. Item 2. The chewable tablet according to Item 1, wherein the component (C) is at least one selected from the group consisting of light anhydrous silicic acid, heavy anhydrous silicic acid, hydrous silicon dioxide, and anhydrous silicic acid hydrate.
Item 3. Item 3. The chewable tablet according to Item 1 or 2, wherein the component (D) is at least one selected from the group consisting of sorbitol, erythritol, maltitol, mannitol, lactitol, xylitol, and galactitol.
Item 4. Item 4. The chewable tablet according to any one of Items 1 to 3, wherein 30 to 200 parts by weight of the component (B) is contained with respect to 100 parts by weight of the component (A).
Item 5. Item 5. The chewable tablet according to any one of Items 1 to 4, wherein 30 to 500 parts by weight of the component (C) are contained with respect to 100 parts by weight of the component (A).
Item 6. Item 6. The chewable tablet according to any one of Items 1 to 5, wherein the component (D) is contained in an amount of 650 parts by weight or more with respect to 100 parts by weight of the component (A).

  According to the chewable tablet of the present invention, although it contains carnitine and / or a salt thereof and dimethylpolysiloxane and / or a derivative thereof, the powdery and rough feeling at the time of chewing is suppressed, and a good mouth-melting feeling Therefore, taking becomes easy and compliance can be improved. Further, the chewable tablet of the present invention contains carnitine and / or a salt thereof and dimethylpolysiloxane and / or a derivative thereof, so that digestive function activation is enhanced, metabolism of neutral fat is promoted, and abdominal symptoms caused by gas occur. Effects such as prevention or treatment can be exhibited in combination.

  The chewable tablet of the present invention comprises carnitine and / or a salt thereof (also sometimes referred to as (A) component), dimethylpolysiloxane and / or a derivative thereof (also sometimes referred to as (B) component), silicon dioxide ( (C) component)), and sugar alcohol (sometimes referred to as (D) component). Hereinafter, the chewable tablet of the present invention will be described in detail.

(A) Carnitine and / or salt thereof The chewable tablet of the present invention contains carnitine and / or a salt thereof. Carnitine and its salts are known compounds that are known to enhance the digestive function activation, transport the long chain fatty acid to the mitochondria, and the like.

  The carnitine used in the present invention may be any of L-form, D-form, and DL-form.

  The carnitine salt is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include halide salts, metal salts, ammonium salts, organic acid salts, and inorganic acid salts. More specifically, as a salt of carnitine, chloride salt; metal salt such as sodium salt, potassium salt, calcium salt, magnesium salt, zinc salt; ammonium salt; acetate salt, propionate salt, lactate salt, tartrate salt, Examples include organic acid salts such as citrate, succinate, maleate, and fumarate; inorganic acid salts such as hydrochloride, sulfate, and phosphate. These carnitine salts may be used alone or in combination of two or more.

  In the chewable tablet of the present invention, as component (A), either carnitine or a salt thereof may be used alone, or a combination thereof may be used.

  Among these components (A), carnitine, carnitine chloride salt, preferably from the viewpoint of effectively suppressing the powdery and rough feeling during mastication and imparting a better mouth melt feeling, More preferred are DL-carnitine and DL-carnitine chloride salt, and particularly preferred is DL-carnitine chloride salt.

  Although there is no restriction | limiting in particular about content of (A) component in the chewable tablet of this invention, For example, 0.1-20 weight%, Preferably it is 1-15 weight%, More preferably, 3-12 weight% is mentioned.

(B) Dimethylpolysiloxane and / or its derivative The chewable tablet of the present invention contains dimethylpolysiloxane and / or its derivative. Dimethylpolysiloxane is a kind of silicone, and is a known compound that reduces surface tension and exhibits antifoaming action.

  The derivative of dimethylpolysiloxane used in the present invention is not particularly limited as long as it is pharmaceutically acceptable. For example, some of the methyl groups bonded to dimethylpolysiloxane may contain other atoms and / or Or what is substituted by the substituent is mentioned. Specific examples of such other atoms and / or substituents include hydrogen atoms, carboxyl groups, amino groups, hydroxyl groups, and substituents such as epoxy groups, carboxyl groups, amino groups, and hydroxyl groups. Examples thereof include an alkyl group having 2 to 10 carbon atoms or a phenyl group.

  Although it does not restrict | limit especially about the viscosity in 25 degreeC of the dimethylpolysiloxane and / or its derivative used by this invention, For example, 100-1000 cSt, Preferably it is 200-600 cSt, More preferably, 250-450 cSt is mentioned. In the present specification, “viscosity of dimethylpolysiloxane and / or a derivative thereof at 25 ° C.” is a value measured at a measurement temperature of 25 ° C. in accordance with a method defined in JIS K 2283.

  In the chewable tablet of the present invention, as component (B), either dimethylpolysiloxane or a derivative thereof may be used alone, or a combination thereof may be used.

  Among these components (B), dimethylpolysiloxane is preferably used from the viewpoint of effectively suppressing powderiness and a rough feeling during chewing and imparting a better mouth-melting feeling.

  Although there is no restriction | limiting in particular about content of (B) component in the chewable tablet of this invention, For example, 0.1 to 15 weight%, Preferably it is 1 to 12 weight%, More preferably, it is 3 to 9 weight%.

  In the chewable tablet of the present invention, the ratio of the component (B) to the component (A) is not particularly limited. For example, the amount of the component (B) is 30 to 200 parts by weight per 100 parts by weight of the component (A). Can be mentioned. In particular, from the viewpoint of effectively suppressing the powderiness and the rough feeling during chewing and imparting a better mouth melt feeling, the component (B) is preferably 50 to 100 parts by weight per 100 parts by weight of the component (A). 200 weight part, More preferably, 100-150 weight part is mentioned.

(C) Silicon dioxide The chewable tablet of the present invention contains silicon dioxide. In chewable tablets using carnitine or a salt thereof and dimethylpolysiloxane or a derivative thereof by the interaction between silicon dioxide and a sugar alcohol described later, the powdery and rough feeling at the time of chewing is suppressed, and the mouth melting feeling is improved. Is possible.

  The type of silicon dioxide used in the chewable tablet of the present invention is not particularly limited, and examples thereof include light anhydrous silicic acid, heavy anhydrous silicic acid, hydrous silicon dioxide, and anhydrous silicic acid hydrate. These silicon dioxides may be used individually by 1 type, and may be used in combination of 2 or more type.

  Among these components (C), light anhydrous silicic acid, heavy anhydrous silicic acid are preferred from the viewpoint of effectively suppressing powderiness and rough feeling during chewing and imparting a better mouth melt feeling. An acid, more preferably light anhydrous silicic acid is mentioned.

  Although there is no restriction | limiting in particular about content of (C) component in the chewable tablet of this invention, For example, 1 to 10 weight% is mentioned. The content of the component (C) in the chewable tablet of the present invention is preferably 2 to 8 from the viewpoint of effectively suppressing the powderiness and the rough feeling during chewing and imparting a better mouth-melting feeling. % By weight, more preferably 3 to 6% by weight.

  In the chewable tablet of the present invention, the ratio of the component (C) to the component (A) is not particularly limited. For example, the amount of the component (C) is 30 to 500 parts by weight per 100 parts by weight of the component (A). Can be mentioned. In particular, from the viewpoint of effectively suppressing the powderiness and the rough feeling during chewing and imparting a better mouth melt feeling, the component (C) is preferably 30 to 100 parts by weight per 100 parts by weight of the component (A). 250 weight part, More preferably, 30-140 weight part is mentioned.

(D) Sugar alcohol The chewable tablet of the present invention contains a sugar alcohol. In the chewable tablet of the present invention, the sugar alcohol is a chewable tablet using carnitine or a salt thereof and dimethylpolysiloxane or a derivative thereof together with the silicon dioxide, and suppresses the powderiness and the rough feeling at the time of chewing, and has a mouth-melting feeling. Play a good role.

  The type of sugar alcohol used in the chewable tablet of the present invention is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include sorbitol, erythritol, maltitol, mannitol, lactitol, xylitol, galactitol and the like. Can be mentioned.

  In the chewable tablet of the present invention, as the component (D), one type of sugar alcohol may be used alone, or two or more types may be used in combination.

  Among these components (D), from the viewpoint of effectively suppressing the powderiness and the rough feeling during mastication and giving a better mouth melt feeling, preferably at least sorbitol, erythritol, and maltitol 1 type; More preferably, erythritol and / or erythritol, or a combination of sorbitol, erythritol, and maltitol is included.

  When sorbitol, erythritol, and maltitol are used in combination as the component (D), these ratios are not particularly limited. For example, erythritol is 5 to 50 parts by weight per 100 parts by weight of sorbitol, preferably 10 parts. -40 parts by weight, more preferably 20-30 parts by weight; the ratio of maltitol is 5-50 parts by weight, preferably 5-30 parts by weight, more preferably 10-20 parts by weight.

  Although there is no restriction | limiting in particular about content of (D) component in the chewable tablet of this invention, For example, 50 to 95 weight% is mentioned. The content of the component (D) in the chewable tablet of the present invention is preferably 60 to 92 from the viewpoint of effectively suppressing the powderiness and the rough feeling at the time of chewing and imparting a better mouth melting feeling. % By weight, more preferably 70 to 90% by weight.

  In the chewable tablet of the present invention, the ratio of the component (D) to the component (A) is not particularly limited. For example, the component (D) is 650 parts by weight or more per 100 parts by weight of the component (A). A ratio is mentioned. In particular, from the viewpoint of effectively suppressing powderiness and a rough feeling during chewing and imparting a better mouth-melting feeling, component (D) is preferably 650 to 100 parts by weight of component (A). 3000 parts by weight, more preferably 1000 to 2000 parts by weight.

Other Components The chewable tablet of the present invention may contain other nutritional components and pharmacological components as necessary in addition to the components (A) to (D). Such nutritional components and pharmacological components are not particularly limited as long as they can be used in foods and pharmaceuticals. For example, vitamin B1, vitamin B2, vitamin B6, vitamin B12, vitamin C, vitamin A, vitamin D, Vitamins such as vitamin E, vitamin K, niacin, pantothenic acid, folic acid, biotin, lycopene; gastric agents such as betaine hydrochloride and betanecol chloride; carrots, yokuinin, processed daikon, mao, nantamami, cinnamon, gentian, crust, assembly, Herbal extracts or herbal medicines such as goshu, sojutsu, clove, aloe, hop, kakkonto, keiedayu, saikokuedayu, maoyu, koshisaifuto, shoseiryuto; aspirin, acetaminophen, etenzamid, ibuprofen, salicyl Antipyretic analgesics such as amides; expectorants such as noscapine hydrochloride and noscapine; Depressants such as clinol, berberine chloride, creosote, tannic acid, scopolamine hydrobromide, methyl atropine bromide, papaverine hydrochloride, ethyl aminobenzoate; dextromethorphan hydrobromide, tipepidine hibenzate, 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 , Magnesium, zinc, selenium, iron and other minerals; soy protein, egg white powder, whey protein and other proteins; glycine, alanine, arginine, aspartic acid, cystine, phenylalanine, Amino acids such as phosphorus and tryptophan; sucrose, fructose, lactose, water candy, fructose glucose liquid sugar, clarose, thaumatin, aspartame, acesulfame K, oligosaccharide (eg, malto-oligosaccharide, isomalt-oligosaccharide, galactooligosaccharide, inulo-oligosaccharide, fructo-oligo) Sugar, xylooligosaccharide), polydextrose, dextrin, indigestible dextrin, reduced indigestible dextrin and other sweeteners; fatty acids such as linoleic acid, γ-linolenic acid, α-linolenic acid; agaricus, shiitake extract, litchi, Examples include mushrooms such as yamabushitake or extracts thereof; 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 etc. of additive component to be used.

  Furthermore, the chewable tablet of the present invention may contain a base, an additive, and the like as necessary. Such bases and additives are not particularly limited as long as they can be used in foods and pharmaceuticals. For example, water, fats and oils, waxes, hydrocarbons, fatty acids, higher alcohols, esters , Water-soluble polymers, surfactants, metal soaps, lower alcohols, polyhydric alcohols, pH adjusters, buffers, antioxidants, preservatives, fragrances, powders, thickeners, dyes, chelating agents, etc. Can be mentioned. These additive components may be used alone or in combination of two or more. Moreover, about content of these bases and additives, it sets suitably according to the kind etc. of the additive component to be used.

Formulation Form / Use The chewable tablet of the present invention may be coated with a sugar coating base, a water-soluble film coating base or the like, if necessary.

  The weight per tablet of the chewable tablet of the present invention may be appropriately set within a range that can be easily chewed according to the dose per time, the contents of the components (A) and (B), etc. 0.1-2g is mentioned.

  The chewable tablet of the present invention can exert combined effects such as enhanced digestive function activation, promotion of neutral fat metabolism, prevention or treatment of gastric abdominal symptoms by the components (A) and (B). Therefore, it is taken for the purpose of prevention or treatment of abdominal symptoms (burp, stomach fullness, flatulence, etc.) caused by gastrointestinal regulation, diet, gas in the gastrointestinal tract.

  The dose of the chewable tablet of the present invention is not particularly limited, and examples of the dose per day include an amount that is about 120 to 600 mg in terms of component (A).

Production Method The chewable tablet of the present invention can be obtained in accordance with a known chewable tablet production method. Specifically, the components (A) to (D) and pharmacological components, nutritional components, bases, additives, and the like that are added as necessary are mixed at a predetermined ratio, and the mixture is formed into a tablet. Manufactured by.

  From the standpoint of improving moldability and formulation stability, the mixture used for tableting molding is a state in which the component (B) is previously mixed with the component (C) and impregnated in the component (C) After the preparation, it is preferable to produce the mixture by mixing with the component (A), the component (D), and a pharmacological component, a nutritional component, a base, an additive and the like which are added as necessary.

Tableting can be performed by using a single tablet machine, a rotary tablet machine, a high-speed rotary tablet machine or the like. Further, the tableting pressure at the time of tableting is not particularly limited as long as a chewable tablet can be molded, but it is usually set to about 200 to 2000 kg / cm ² .

  EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples. In the following test examples and production examples, carnitine chloride is trade name “DL-Carnitine HCL” (manufactured by Chengda Pharmaceuticals Co., LTD.), And dimethylpolysiloxane is trade name “Dow Corning Q7-9120” (25 ° C. Viscosity: 350 cst; manufactured by Toray Dow Corning Co., Ltd.), and light anhydrous silicic acid, trade name “AdSolider 101” (manufactured by Fuji Silysia Chemical Co., Ltd.) was used.

Test Examples Chewable tablets having the compositions shown in Tables 1 and 2 were prepared and evaluated for their meltability in the mouth. Specifically, the test was conducted by the following method.

  First, a predetermined amount of dimethylpolysiloxane shown in Tables 1 and 2 is mixed with and impregnated with a predetermined amount of light anhydrous silicic acid, magnesium aluminate metasilicate or calcium silicate shown in Tables 1 and 2, followed by a predetermined amount. The other ingredients were mixed to obtain a mixture for tableting molding. The obtained mixture for tablet molding was subjected to tableting using a tableting device (“20 kN table press TB-20H-V09”, manufactured by NPa System Co., Ltd.) so that the tablet hardness was 70 N. 1 g (φ15 mm) chewable tablets per tablet were produced.

  Each of the obtained chewable tablets was taken by three evaluation monitors, and the feeling of melting in the mouth was evaluated. In the evaluation of the mouth melting feeling, “10” indicates that there is no powderiness or graininess when chewing, and the mouthfeeling feeling is good, while “1” indicates that there is powderiness or graininess when chewing, and mouthfeeling feeling is “1”. This was done by conducting a questionnaire using the Visual Analogue Scale. The questionnaire results were averaged, and the evaluation results were summarized by rounding off the first decimal place.

  The obtained results are shown in Tables 1 and 2. As shown in Table 2, in chewable tablets containing carnitine and dimethylpolysiloxane, when both silicon dioxide and sugar alcohol are not included, powderiness and a rough feeling are noticeable when chewing, and the mouth melts. The feeling was worse (Comparative Example 5). In addition, in chewable tablets containing carnitine and dimethylpolysiloxane, even when only one of silicon dioxide or sugar alcohol was included, a powdery feeling and a rough feeling were felt during chewing, and a good mouth-melting feeling was not obtained (Comparative Example) 1 and 4). In addition, chewable tablets containing carnitine and dimethylpolysiloxane can feel powdery or gritty when chewed even when they contain silicates (magnesium aluminate or calcium silicate) and sugar alcohols. A good mouth melting feeling was not obtained (Comparative Examples 2 and 3).

  On the other hand, in chewable tablets containing carnitine and dimethylpolysiloxane, when both silicon dioxide and sugar alcohol are included, the powderiness and rough feeling can be sufficiently suppressed during chewing, and a good mouth melt feeling can be obtained. Obtained (Examples 1 to 6). In particular, when sorbitol alone, erythritol alone, or a combination of sorbitol, erythritol, and maltitol was used as the sugar alcohol, a much better mouth-melting sensation was observed (Examples 1 to 4 and 6).

Production Examples Chewable tablets having the composition shown in Table 3 were produced. Specifically, first, a predetermined amount of dimethylpolysiloxane shown in Table 3 is mixed with and impregnated with a predetermined amount of light anhydrous silicic acid shown in Table 3, and then a predetermined amount of other components are mixed and beaten. A mixture for tableting was obtained. The obtained mixture for tablet molding was subjected to tableting using a tableting device (“20 kN table press TB-20H-V09”, manufactured by NPa System Co., Ltd.) so that the tablet hardness was 70 N. 1 g (φ15 mm) chewable tablets per tablet were produced. All of the obtained chewable tablets were sufficiently suppressed in powderiness and rough feeling during chewing, and a good mouth-melting feeling was recognized.

Claims (6)

  A chewable tablet comprising (A) carnitine and / or a salt thereof, (B) dimethylpolysiloxane and / or a derivative thereof, (C) silicon dioxide, and (D) a sugar alcohol.   The chewable tablet according to claim 1, wherein the component (C) is at least one selected from the group consisting of light anhydrous silicic acid, heavy anhydrous silicic acid, hydrous silicon dioxide, and anhydrous silicic acid hydrate. .   The chewable tablet according to claim 1 or 2, wherein the component (D) is at least one selected from the group consisting of sorbitol, erythritol, maltitol, mannitol, lactitol, xylitol, and galactitol.   The chewable tablet according to any one of claims 1 to 3, wherein 30 to 200 parts by weight of the component (B) is contained with respect to 100 parts by weight of the component (A).   The chewable tablet according to any one of claims 1 to 4, wherein the component (C) is contained in an amount of 30 to 500 parts by weight with respect to 100 parts by weight of the component (A).   The chewable tablet according to any one of claims 1 to 5, wherein the component (D) is contained in an amount of 650 parts by weight or more with respect to 100 parts by weight of the component (A).