Composition

Abstract

To provide novel means that suppresses an unpleasant odor of a component possessing an unpleasant odor.SOLUTION: A composition comprising the following components (A) and (B): (A) a component having an unpleasant odor; (B) one or more selected from the group consisting of bilastine, a salt thereof and solvate forms thereof.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a composition and the like. [Background technology]

[0002] Various components that have unpleasant odors, such as vitamin B6, are known, and attempts have been made to suppress these unpleasant odors (Patent Documents 1 to 3).

[0003] On the other hand, bilastine (chemical name: 2-[4-(2-{4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]piperidin-1-yl}ethyl)phenyl]-2-methylpropanoic acid) has the following formula:

[0004] [ka]

[0005] and is used to treat itching associated with allergic rhinitis, urticaria, and skin diseases (eczema, dermatitis, cutaneous pruritus) (Non-Patent Document 1). [Prior art documents] [Patent documents]

[0006] [Patent Document 1] Japanese Patent Application Publication No. 2019-131517 [Patent Document 2] Japanese Patent Application Laid-Open No. 2003-231647 [Patent Document 3] Japanese Patent Application Publication No. 2022-144779 [Non-patent literature]

[0007] [Non-Patent Document 1] Package insert "Bilanoa Tablets 20mg" Taiho Pharmaceutical Co., Ltd., July 2021 Summary of the Invention [Problem to be solved by the invention]

[0008] An object of the present invention is to provide a new means for suppressing the unpleasant odor of a component having an unpleasant odor. [Means for solving the problem]

[0009] The present inventors have conducted extensive research to solve the above-mentioned problems and have surprisingly found that the unpleasant odor can be suppressed by adding one or more members selected from the group consisting of bilastine, its salts, and solvates thereof to a composition containing a component with an unpleasant odor, such as pyridoxine, and have thus completed the present invention.

[0010] That is, the present invention provides a composition comprising the following components (A) and (B): (A) ingredients having an unpleasant odor; (B) one or more selected from the group consisting of bilastine, a salt thereof, and a solvate thereof; The present invention provides a composition comprising: The present invention also provides a deodorant containing at least one member selected from the group consisting of bilastine, a salt thereof, and a solvate thereof. The present invention also provides a deodorizing method using one or more members selected from the group consisting of bilastine, salts thereof, and solvates thereof. [Effects of the Invention]

[0011] According to the present invention, the unpleasant odor of a component having an unpleasant odor can be suppressed, and therefore, a composition such as a pharmaceutical composition that contains a component having an unpleasant odor but has a less unpleasant odor can be provided. DETAILED DESCRIPTION OF THE INVENTION

[0012] <Component (A)> In the present invention, the component having an unpleasant odor that is used as component (A) is not particularly limited, and examples thereof include known components such as those described in Patent Documents 1-3.More specifically, aloe, Mallotus japonicus (red bud oak), Asarum serrata (asian medicine), Ephedra chinensis (yarrow), Inchinko (innocent vine), Fennel (aniseed), Turmeric, Scutellaria baicalensis (sweetcorn), Corydalis chinensis (corkscrew root), Astragalus chinensis (astragalus root), Scutellaria baicalensis (yarrow root), Phellodendron bark (Phellodendron bark), Coptis chinensis (cherry bark), Coptis chinensis (Coptis Rhizome), Onji (Atractylodes orientalis), Zedoary (Atractylodes rhizome), Cascara sagrada (cascarilla tree), Valerian (valerian), Pueraria lobata (pueraria root), Cuckoo chrysanthemum, Chamomile, Guarana, Calonin, Glycyrrhiza uralensis (licorice root), Platycodon grandiflorum (platycodon), Phellodendron (Phewberry), Phellodendron amurense (Apricot kernel), Lycium chinense (Lycium bark), Lycium koensis (Lycium berry), Sophora root (Bitter ginseng), Kernel root (Cinnamon bark), Cassia seed (Cassia nut), Cinnamon root (Cassium globulus), Gentian (Gentiana), Geranium herb (German ginseng), Red ginseng (Red ginseng), Magnolia root (Philippinarum), Magnolia chinensis (Citrus berry), Bezoar root (Bezoar), Goshitsu (Cuscolumbine), Schisandra chinensis (Schismiflora), Colombo (Cornus chinensis), Bupleurum root (Bupleurum chinensis), Saffron (Saffron), Zanthoxylum chinense (Japanese pepper), Gardenia berry (Cornus chinensis), Cornus chinensis (Wild bean root), Rehmannia root (Grape root) Yellow), Aster, Lithospermum Root, Perilla Seed, Jigokpi (Ground Bone Bark), Peony, Musk, Shajin (Shrimp), Shazenshi (Plant Seed), Shazensou (Plant Seed), Animal Gall (including Bear Gall), Zingiber Officinale (Ginger), Cimicifuga (Citric Acid), Jiryu (Earth Dragon), Shini (Magnolia), Seihi (Green Bark), Sekishokon (Celestial Root), Sekisan (Garlic), Senega, Cnidium Rhizome (Centaurea Root), Zenko (Centaurea Root), Senkotsu (Centaurea Root), Sentarium Grass, Swertia Root, Senbo (Centaurea Root), Senso (Toad Venom), Senna, Atractylodes Rhizome (Blue Root) Atractylodes macrocarpa (Atractylodes macrocarpa), Sophora chinensis (Mulberry bark), Perilla japonica (Perilla leaf), Garlic, Rhubarb, Bamboo joint ginseng, Chimo (Ancestral mother ginseng), Chiretta grass, Clove, Citrus fruit peel, Orange peel, Angelica acutiloba (Angelica quince), Peach kernel, Angelica dahurica (Angelica root), Ipecac (Ipecac), Eucommia ulmoides (Eucommia ulmoides), Nandina fruit (Nandina berry), Bitter tincture, Carrot, Fritillaria rubra (Fritillaria rosa), Ophiopogon chinensis (Ophiopogon), Glehnia littoralis (Beach windbreak), Pinellia japonica (Pinella verum), Scutellaria baicalensis (Safflower), Pinellia japonica (Pinellifera serrata), White peony, White angelica,Herbal medicines such as Atractylodes Root (White Atractylodes), Poria Cocos (Poria Cocos), Belladonna, Belladonna Root, Belladonna Leaf, Hops, Nux Vomica, Bowie (Springweed), Peony Bark (Mouth Peony), Ephedra (Mahuang), Mongolian Root (Small Tree), Saussurea Root (Small Tree), Job's Nectar, Artemisia, Artemisia Root, Gentian (Willow Tree), Luzonka (Lucifera), Forsythia Fruit (Forsythia), Velvet Antler (Velvety Veitchii), Royal Jelly, and their extracts (extracts, tinctures, dried extracts, etc.); Vitamin B1 (e.g., thiamine, thiamine chloride hydrochloride, thiamine nitrate, dicethiamine hydrochloride, cetothiamin), Thiamine hydrochloride, fursultiamine, fursultiamine hydrochloride, octotiamine, sicotiamine, thiamine disulfide, bis-ibutiamine, bis-bentiamine, prosultiamine, benfotiamine, etc.), niacinamide, biotin, pyridoxines (e.g., pyridoxine hydrochloride), calcium pantothenate, nicotinamide, vitamins such as vitamin B12 (e.g., cyanocobalamin, mecobalamin, etc.); acetaminophen, aspirin, phenacetin, mefenamic acid, antipyrine, phenacetin Nilbutazone, sulpyrine, diclofenac sodium, ibuprofen, ketoprofen, indomethacin, tranexamic acid, caffeine anhydrous, caffeine, glucosamine, chondroitin sulfate, chondroitin sulfate sodium, hyaluronic acid, cysteine, naproxen, epirizole, tiaramide hydrochloride, pentazocine, acetylcholine chloride, alimemazine tartrate, cyproheptadine hydrochloride, epinastine, diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, methylmethionine Examples of suitable antiperspirants include benzophenone sulfonium chloride, codeine phosphate, dihydrocodeine phosphate, dextromethorphan hydrobromide, pentoxyverine citrate, theophylline, aminophylline, ephedrine hydrochloride, epinephrine hydrochloride, salbutamol sulfate, trimetoquinol hydrochloride, procaterol hydrochloride, methylephedrine hydrochloride, phenylpropanolamine hydrochloride, guaifenesin, potassium chloride, oyster shell powder, seaweed powder, and pirenzepine hydrochloride. These may be used alone or in combination of two or more. Among these, pyridoxines are preferred.

[0013] In the present invention, the term "pyridoxine derivatives" refers to one or more compounds selected from the group consisting of pyridoxine and its derivatives (pyridoxamine, pyridoxal, pyridoxal phosphate, etc.) and their salts (salts with Group 2 elements such as calcium salts; inorganic acid salts such as hydrochlorides, etc.). In the present invention, these compounds may be used alone or in combination of two or more. In the present invention, from the viewpoint of manufacturability and the like, one or more selected from the group consisting of pyridoxine, pyridoxamine, pyridoxal, pyridoxal phosphate, and salts thereof are preferred, one or more selected from the group consisting of pyridoxine and salts thereof are more preferred, and pyridoxine hydrochloride is particularly preferred. Pyridoxine compounds are known compounds and may be produced by known methods, or commercially available products may be used. Specific examples of commercially available products include Viewplex VH (DSM Nutrition Japan Co., Ltd.), V.B6 Hydrochloride (DSM Nutrition Japan Co., Ltd.), pyridoxine hydrochloride (Nacalai Tesque Inc.), pyridoxine hydrochloride (Kyowa Pharma Chemical Co., Ltd.), pyridoxine hydrochloride (BASF Japan Ltd.), pyridoxal phosphate (Watanabe Chemical Co., Ltd.), pyridoxal phosphate ester (Sekisui Medical Co., Ltd.), pyridoxal phosphate ester hydrate (Kyowa Pharma Chemical Co., Ltd.), and pyridoxal calcium phosphate (Watanabe Chemical Co., Ltd.).

[0014] In the present invention, the content of component (A) in the composition is not particularly limited and may be determined by appropriate consideration. However, from the viewpoint of the therapeutic or alleviating effect on allergies and the like, the content of component (A) is preferably 0.01 to 80 mass %, more preferably 0.1 to 70 mass %, and particularly preferably 0.5 to 60 mass %, of the total mass of the composition.

[0015] The daily dose of component (A) in the composition is not particularly limited and may be determined appropriately depending on the gender, age, symptoms, etc. of the recipient. For example, the composition preferably contains 0.1 to 3,000 mg of component (A) in free form / original herbal drug equivalent, more preferably 0.5 to 1,000 mg, particularly preferably 1 to 300 mg, and even more preferably 5 to 100 mg.

[0016] <Ingredient (B)> As used herein, "one or more selected from the group consisting of bilastine, its salts, and solvates thereof" includes not only bilastine itself, but also pharmaceutically acceptable salts of bilastine, and solvates of bilastine itself or its pharmaceutically acceptable salts with water, alcohol, etc. The salt is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include inorganic acid salts such as hydrochloride, sulfate, nitrate, hydrofluoride, and hydrobromide; organic acid salts such as acetate, tartrate, lactate, citrate, fumarate, maleate, succinate, methanesulfonate, ethanesulfonate, benzenesulfonate, toluenesulfonate, naphthalenesulfonate, and camphorsulfonate; metal salts such as sodium salt, potassium salt, lithium salt, calcium salt, and magnesium salt; amine salts such as ammonia, trimethylamine, triethylamine, pyridine, collidine, and lutidine; and organic base salts such as lysine and arginine. These may be used alone or in appropriate combination of two or more.

[0017] As component (B), bilastine is preferred. Component (B) is a known component and can be produced by known methods, or a commercially available product such as "Bilastine" (Sumitomo Chemical Co., Ltd.) can be used.

[0018] The content of component (B) in the composition is not particularly limited and may be determined after appropriate consideration. However, from the viewpoint of the effect of suppressing the unpleasant odor of component (A), the content of component (B) in total, calculated as the free form, relative to the total mass of the composition is preferably 0.1 to 75 mass%, more preferably 0.5 to 65 mass%, and particularly preferably 1 to 55 mass%.

[0019] The daily amount of component (B) in the composition is not particularly limited and may be determined appropriately depending on the gender, age, symptoms, etc. of the user. From the viewpoint of the effect of suppressing the unpleasant odor of component (A), the composition preferably contains 0.1 to 300 mg of component (B) per day in terms of the free form, more preferably 0.5 to 200 mg, and particularly preferably 1 to 150 mg.

[0020] Furthermore, in the present invention, the mass ratio of component (A) to component (B) contained in the composition is not particularly limited and may be determined through appropriate consideration. However, from the viewpoint of the unpleasant odor suppressing effect of component (A), the composition preferably contains 0.0001 to 150 parts by mass of component (B) in total, calculated as its free form, per 1 part by mass of component (A) in total, more preferably 0.001 to 70 parts by mass, and particularly preferably 0.01 to 30 parts by mass.

[0021] The composition may contain, as a medicinal ingredient, one or more ingredients other than those mentioned above, such as antipyretics, analgesics, antihistamines, antitussives, noscapines, bronchodilators, expectorants, hypnotics and sedatives, vitamins, aminocarboxylic acids, sterols, calcium salts, magnesium salts, iron salts, glucuronic acids, sugar alcohols, glycosides, thioctic acids, anti-inflammatory agents, gastric mucosa protective agents, antacids, anticholinergic agents, xanthine-based ingredients, etc.

[0022] Examples of antipyretic analgesics include ethenzamide, sazapyrine, salicylamide, lactylphenetidine, loxoprofen, sodium salicylate, etc. Examples of antihistamines include azelastine hydrochloride, isothipendyl hydrochloride, iproheptine hydrochloride, ebastine, emedastine fumarate, oxatomide, olopatadine hydrochloride, carbinoxamine diphenyldisulfonate, carbinoxamine maleate, clemastine fumarate, ketotifen fumarate, difeterol hydrochloride, difeterol phosphate, diphenylpyraline hydrochloride, diphenylpyraline teoclate, cetirizine hydrochloride, triprolidine hydrochloride, tripelennamine hydrochloride, thonzylamine hydrochloride, fexofenadine, fenethazine hydrochloride, promethazine hydrochloride, promethazine methylenedisalicylate, bepotastine besilate, homochlorcyclizine hydrochloride, mequitazine, methdilazine hydrochloride, mebhydroline napadisilate, loratadine, and rupatadine fumarate.

[0023] Examples of antitussives include alloclamide hydrochloride, eprazinone hydrochloride, carbetapentane citrate, cloperastine hydrochloride, cloperastine fendizoate, dibunate sodium, dimemorfan phosphate, tipepidine citrate, tipepidine hibenzate and the like.

[0024] Examples of noscapines include noscapine hydrochloride and noscapine. Bronchodilators include, for example, phenylephrine hydrochloride, methoxyphenamine hydrochloride, etc.

[0025] Examples of expectorants include ammonia-fennel extract, ethylcysteine ​​hydrochloride, ammonium chloride, carbocysteine, potassium guaiacolsulfonate, potassium cresolsulfonate, methylcysteine ​​hydrochloride, l-menthol, and lysozyme hydrochloride.

[0026] Examples of hypnotics and sedatives include allylisopropylacetylurea and bromvalerylurea. Examples of vitamins include vitamin B2, vitamin B5, vitamin C, hesperidin and its derivatives and salts thereof (e.g., riboflavin, riboflavin phosphate, riboflavin butyrate, riboflavin sodium phosphate, panthenol, pantethine, sodium pantothenate, ascorbic acid, sodium ascorbate, calcium ascorbate, hesperidin, etc.).

[0027] Examples of aminocarboxylic acids include L-arginine hydrochloride, L-isoleucine, carnitine chloride, glycine, L-glutamic acid, diisopropylamine dichloroacetate, choline bitartrate, taurine, L-threonine, L-valine, L-histidine hydrochloride hydrate, DL-methionine, yoke lecithin, L-lysine hydrochloride, L-leucine, orotic acid, and choline orotate. Examples of sterols include ursodeoxycholic acid, gamma oryzanol, and dehydrocholic acid. Examples of calcium salts, magnesium salts, and iron salts include calcium citrate, calcium glycerophosphate, calcium gluconate hydrate, calcium carbonate, precipitated calcium carbonate, calcium lactate hydrate, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate hydrate, ferrous ammonium citrate, ferrous fumarate, and magnesium carbonate.

[0028] Examples of glucuronic acids include glucuronolactone, glucuronic acid, and glucuronic acid amide. Examples of sugar alcohols include inositol, gluconic acid and salts thereof. Examples of glycosides include rutin hydrate. Examples of thioctic acids include thioctic acid and thioctic acid amide.

[0029] Anti-inflammatory agents include, for example, glycyrrhizinic acid and its derivatives and salts thereof (e.g., dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.), seaprose, semi-alkaline proteinase, serrapeptase, proctase, pronase, bromelain, etc.

[0030] Examples of gastric mucosa protecting agents include gefarnate, cetraxate hydrochloride, sofalcone, teprenone, etc. Examples of antacids include aminoacetic acid, magnesium aluminosilicate, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, magnesium oxide, dihydroxyaluminum aminoacetate, magnesium alumina hydroxide, aluminum hydroxide gel, dried aluminum hydroxide gel, dried mixed gel of aluminum hydroxide and magnesium carbonate, co-precipitation product of aluminum hydroxide and sodium hydrogen carbonate, co-precipitation product of aluminum hydroxide, calcium carbonate and magnesium carbonate, magnesium hydroxide, co-precipitation product of magnesium hydroxide and aluminum potassium sulfate, magnesium carbonate, sodium hydrogen carbonate, precipitated calcium carbonate, magnesium aluminometasilicate, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate, squid bone, stone jelly, and sea urchin.

[0031] Examples of anticholinergic agents include oxyphencyclamine hydrochloride, dicyclomine hydrochloride, methixene hydrochloride, scopolamine hydrobromide, Datura extract, tipepidium bromide, methylatropine bromide, methylanisotropine bromide, methylscopolamine bromide, methyl-l-hyoscyamine bromide, methylbenactydium bromide, butylscopolamine bromide, belladonna alkaloids, belladonna extract, belladonna total alkaloids, isopropamide iodide, diphenylpiperidinomethyldioxolane iodide, Scopolia extract, Scopolia root, and Scopolia root total alkaloid citrate. Examples of xanthine-based components include diprophylline and proxyphylline.

[0032] The use of the "composition" herein is not particularly limited, but since it contains one or more compounds selected from the group consisting of bilastine, its salts, and solvates thereof, it can be suitably used as a pharmaceutical composition. The dosage form of the "composition" is not particularly limited, and it may be any of a solid, semi-solid, or liquid preparation, and can be selected depending on the intended use, etc. Examples of the dosage form of the composition include those described in the General Provisions for Preparations in the 18th Edition of the Japanese Pharmacopoeia. For example, dosage forms for oral administration include solid preparations such as tablets (including, for example, regular tablets, orally disintegrating tablets, chewable tablets, effervescent tablets, dispersible tablets, dissolving tablets, etc.), capsules, granules (including, for example, effervescent granules, etc.), powders, and pills; semi-solid preparations such as oral jellies; and liquid preparations such as oral liquids (including, for example, elixirs, suspensions, emulsions, lemonades, etc.). Dosage forms for parenteral administration include injections, inhalants, eye drops, ear drops, nasal drops, suppositories, solid preparations for external use, liquid preparations for external use, sprays, ointments, creams, gels, patches, etc.

[0033] The dosage form of the composition is preferably a solid preparation from the viewpoint of ease of administration, and is particularly preferably a solid preparation selected from tablets (including, for example, normal tablets, orally disintegrating tablets, chewable tablets, effervescent tablets, dispersible tablets, dissolving tablets, etc.), capsules, granules (including, for example, effervescent granules, etc.), powders, and pills.

[0034] The composition can be manufactured by known methods, such as those described in the General Provisions for Preparations of the Japanese Pharmacopoeia (18th Edition), depending on the dosage form. In this case, a pharmaceutically acceptable carrier (formulation additive) may be added to the composition. Examples of such formulation additives include, but are not limited to, excipients, disintegrants, binders, lubricants, plasticizers, film-forming agents, powders, poorly water-soluble polymeric substances, antioxidants, pH adjusters, flavoring agents, and sweeteners. These formulation additives include, for example, those listed in the Pharmaceutical Additives Dictionary 2021 (published by Yakuji Nippo Co., Ltd.) and the Handbook of Pharmaceutical Excipients, Seventh Edition (published by Pharmaceutical Press).

[0035] Examples of excipients include inorganic excipients such as aluminum silicate, anhydrous sodium sulfate, anhydrous calcium hydrogen phosphate, sodium chloride, calcium silicate, light anhydrous silicic acid, heavy anhydrous silicic acid, calcium sulfate, calcium monohydrogen phosphate, calcium hydrogen phosphate, sodium hydrogen phosphate, potassium dihydrogen phosphate, calcium dihydrogen phosphate, and sodium dihydrogen phosphate; and organic excipients such as candy powder, starch (wheat starch, rice starch, corn starch, partially pregelatinized starch, etc.), fructose, caramel, agar, xylitol, paraffin, crystalline cellulose, sucrose, maltose, lactose, lactose hydrate, sucrose, glucose, pullulan, polyoxyethylene hydrogenated castor oil, maltitol, reduced maltose syrup, powdered reduced maltose syrup, erythritol, sorbitol, mannitol, lactitol, trehalose, reduced palatinose, aminoalkyl methacrylate copolymer E, polyvinyl acetal diethylaminoacetate, and calcium citrate. These may be used alone or in combination of two or more.

[0036] Examples of disintegrants include super disintegrants such as sodium starch glycolate, croscarmellose sodium, and crospovidone, as well as carmellose, carmellose calcium, starch, sucrose fatty acid esters, gelatin, sodium hydrogen carbonate, dextrin, dehydroacetic acid and its salts, povidone, and polyoxyethylene hydrogenated castor oil 60. These can be used alone or in combination of two or more.

[0037] Examples of binders include fats and oils such as hardened beef tallow oil, hardened oil, hydrogenated vegetable oil, hardened soybean oil, carnauba wax, white beeswax, beeswax, and Japan wax, as well as methyl cellulose, hydroxypropyl cellulose, hypromellose, carmellose sodium, starch (wheat starch, rice starch, corn starch, partially pregelatinized starch, etc.), dextrin, pullulan, gum arabic, agar, gelatin, tragacanth, sodium alginate, povidone, polyvinyl alcohol, aminoalkyl methacrylate copolymer E, polyvinyl acetal diethylaminoacetate, etc. These may be used alone or in combination of two or more.

[0038] Examples of lubricants include calcium stearate, magnesium stearate, sodium stearyl fumarate, sucrose fatty acid esters, etc. These can be used alone or in combination of two or more.

[0039] Examples of plasticizers include triethyl citrate, glycerin, sesame oil, sorbitol, castor oil, polysorbate 80 (polyoxyethylene (20) sorbitan oleate), etc. These may be used alone or in combination of two or more.

[0040] Examples of film-forming agents include alkylcelluloses such as methyl cellulose and ethyl cellulose; alginic acid or a salt thereof such as sodium alginate; carrageenan; carboxyalkylcelluloses such as sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, potassium carboxymethyl cellulose, carboxymethyl cellulose, and carboxymethyl ethyl cellulose; xanthan gum; hydroxyalkylcelluloses such as hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, and hypromellose (hydroxypropyl methylcellulose); hydroxyalkylcellulose phthalates such as hydroxypropyl methylcellulose phthalate; pullulan; polyvinyl acetate; polyvinyl acetate phthalate; and polyvinylpyrrolidone. These may be used alone or in combination of two or more.

[0041] Examples of powders include organic or inorganic powders such as talc, titanium oxide, yellow ferric oxide, ferric oxide, legal pigments, etc. These can be used alone or in combination of two or more.

[0042] Examples of poorly water-soluble polymeric substances include carboxyvinyl polymers, aminoalkyl methacrylate copolymers, etc. These may be used alone or in combination of two or more.

[0043] Examples of antioxidants include ascorbic acid, sodium hydrogen sulfite, sodium sulfite, sodium edetate, erythorbic acid, tocopherol acetate, dibutylhydroxytoluene, natural vitamin E, tocopherol, butylhydroxyanisole, etc. These can be used alone or in combination of two or more.

[0044] Examples of pH adjusters include organic acids or salts thereof such as citric acid, sodium citrate, anhydrous citric acid, malic acid, maleic acid, succinic acid, fumaric acid, tartaric acid, sodium tartrate, lactic acid, calcium lactate, sodium lactate, acetic acid, sodium acetate, and glacial acetic acid; inorganic acids or salts thereof such as hydrochloric acid, sulfuric acid, phosphoric acid, sodium hydrogen phosphate, potassium dihydrogen phosphate, sodium dihydrogen phosphate, sodium carbonate, and sodium hydrogen carbonate; alkali hydroxides such as sodium hydroxide, potassium hydroxide, calcium hydroxide, and magnesium hydroxide; and amines such as triethanolamine, diethanolamine, and diisopropanolamine.

[0045] Examples of flavoring agents include terpenes such as limonene, pinene, camphene, cymene, cineole, citronellol, geraniol, nerol, linalool, menthol, terpineol, rhodinol, borneol, isoborneol, menthone, camphor, eugenol, and cinzeylanol; terpene-containing essential oils such as spruce oil, orange oil, peppermint oil, camphor oil, eucalyptus oil, turpentine oil, lemon oil, ginger oil, clove oil, cinnamon oil, lavender oil, fennel oil, chamomile oil, perilla oil, and spearmint oil; and acidulants such as ascorbic acid, tartaric acid, citric acid, malic acid, and salts thereof. These may be used alone or in combination of two or more.

[0046] Examples of sweeteners include aspartame, stevia, sucralose, thaumatin, acesulfame potassium, saccharin, and saccharin sodium, and these can be used alone or in combination of two or more.

[0047] The composition can be prepared by a known method depending on the dosage form. For example, when the composition is a solid preparation, it can be produced by appropriately combining unit operations such as pulverization, mixing, granulation, drying, sizing, classification, filling, tableting, and coating. More specifically, when the composition is in the form of a granular preparation such as granules, powders, or pills, the composition can be produced by mixing all or a part of component (A) and component (B), and optionally other active ingredients, formulation additives such as excipients, binders, disintegrants, and lubricants, and then granulating the mixture by a known granulation method such as extrusion granulation, tumbling granulation, stirring granulation, fluidized bed granulation, spray granulation, melt granulation, or crushing granulation to obtain a granulated product, which can then be further classified, sized, etc., as necessary. The obtained granulated product can also be coated with a coating agent or the like by a known method. When the composition is in the form of a tablet, it can be produced by mixing all or part of component (A) and component (B), and, if necessary, other active ingredients, and appropriate formulation additives such as excipients, binders, disintegrants, and lubricants, to obtain a mixture, which is then directly compressed (tableted) (direct powder compression method), or by compressing (tableted) the above-mentioned granules after classification, sizing, etc., as necessary (semi-dry granule compression method, dry granule compression method, wet granule compression method, etc.). The obtained compressed product (tablet) can also be coated with a coating agent or the like by a known method. Furthermore, when the dosage form of the composition is a capsule, the above-mentioned granulated or compressed product may be filled into a capsule.

[0048] The composition may further be housed in an airtight package (hereinafter, in this specification, an airtight package containing the composition will be referred to as an "article"). In addition to the airtight package, the article may further include packaging that does not fall under the category of "airtight package" below, and the composition may be housed directly or indirectly in the airtight package. As used herein, the term "airtight packaging" refers to packaging that can prevent the intrusion of solid or liquid foreign matter under normal handling, transportation, storage, and other conditions, and is a concept that encompasses "airtight containers" and "sealed containers" as defined in the General Rules of the 18th Edition of the Japanese Pharmacopoeia. Airtight packaging can be of either a fixed or irregular shape, and examples include bottle packaging, SP (Strip Package) packaging, PTP (Press-Through Package) packaging, pillow packaging, and stick packaging. The airtight packaging may also be a combination of these, such as a configuration in which a composition is first packaged in a PTP package and then packaged in a pillow packaging. From the viewpoint of suppressing the unpleasant odor of the composition, the airtight packaging is preferably one or more types selected from the group consisting of bottle packaging, SP packaging, PTP packaging, pillow packaging, and stick packaging, and is particularly preferably one having at least PTP packaging (a combination of PTP packaging and, if necessary, other packaging such as bottle packaging, SP packaging, pillow packaging, or stick packaging), or one having at least bottle packaging.

[0049] The packaging material (raw material) of the airtight packaging body is not particularly limited, and for example, materials used in the fields of pharmaceuticals, food, etc., such as glass, plastics (polyesters such as polyethylene terephthalate and polyethylene naphthalate; polyethylene (including low density (LDPE), medium density (MDPE), and high density (HDPE)), polyolefins such as polypropylene; polycarbonate; polystyrene, etc.), and metals (aluminum, etc.), can be used alone or in combination of two or more types as appropriate.

[0050] For example, packaging materials used for bottle packaging are not particularly limited, and examples include glass, plastic, metal, etc., and one or more of these can be combined as appropriate. Preferred materials for bottle packaging are glass, polyethylene, and polypropylene, more preferably glass, low-density polyethylene (LDPE), and high-density polyethylene (HDPE), and particularly preferably glass and high-density polyethylene (HDPE). For bottle packaging, for example, an appropriate amount of the composition may be placed in a bottle, which may then be sealed with an appropriate stopper or lid. The size of the bottle may be selected appropriately depending on the amount of composition to be placed, and the capacity of the bottle may be, for example, about 10 to 500 mL, preferably 14 to 400 mL, and more preferably 24 to 350 mL.

[0051] Furthermore, packaging materials used for SP packaging, PTP packaging, pillow packaging, stick packaging, etc. are not particularly limited, and examples thereof include biaxially oriented polypropylene (OPP), biaxially oriented polyester (PET), glycol-modified PET (PET-G), biaxially oriented nylon (ONy, PA), cellophane, paper, low-density polyethylene (LDPE), linear low-density polyethylene (L-LDPE), ethylene-vinyl acetate copolymer (EVA), unoriented polypropylene (CPP, IPP), ionomer resin (IO ), ethylene-methacrylic acid copolymer (EMAA), polyacrylonitrile (PAN), biaxially oriented polyvinylidene chloride (PVDC), ethylene-vinyl alcohol copolymer resin (EVOH), polyvinyl chloride (PVC), cyclic polyolefin (COC), unstretched nylon (CNy), polycarbonate (PC), polystyrene (PS), rigid polyvinyl chloride (VSC), and other resins, as well as metal foils such as aluminum foil (AL), and one or more of these can be used in combination as appropriate.

[0052] When SP packaging, PTP packaging, pillow packaging, stick packaging, etc. are produced, a sheet using one or more of the above-mentioned packaging materials may be produced by a known method, and in this case, the packaging materials may be appropriately combined to form a multilayer structure. A method for producing a multilayer structure using two or more packaging materials as a sheet includes a method of laminating the packaging materials to produce a laminated sheet. Laminated sheets can be produced by known methods such as extrusion lamination, dry lamination, co-extrusion lamination, thermal lamination, wet lamination, non-solvent lamination, and heat lamination. Furthermore, sheets for SP packaging, PTP packaging, pillow packaging, and stick packaging can also be commercially available products.

[0053] Among the above-mentioned sheets, examples of single-layer sheets using one type of packaging material include PVC sheets and CPP sheets, and examples of laminated sheets using two or more types of packaging materials include, but are not limited to, sheets laminated with PVC and PVDC (PVC / PVDC; hereinafter the same abbreviation), PVC / PVDC / PE / PVC, PVC / PVDC / PE / PVDC / PVC, CPP / COC / CPP, PVC / PCTFE, CPP / PCTFE, PVC / AL / PA, PVC / AL, CPP / AL, and CPP / CPP / CPP (the above-mentioned sheets use two or more types of CPP).

[0054] As a form of PTP packaging, the composition is stored one by one or in one dosage unit in a desired number of pockets formed in a resin sheet or the like by a known method, and then the composition is covered with a sheet containing a metal foil such as aluminum foil as a lid material. Note that so-called double-sided aluminum PTP packaging, in which a sheet containing aluminum foil as a constituent material is also used as the sheet forming the pocket, may also be used. In the present invention, from the viewpoint of suppressing the unpleasant odor of the composition, it is preferable to further package the PTP packaging in pillow packaging (e.g., aluminum pillow packaging, etc.). Examples of the SP packaging, pillow packaging, and stick packaging forms include packaging the composition individually or in individual dosage units using a known method using a resin sheet, a sheet made of aluminum foil, etc. In the present invention, it is preferable to use a sheet made of aluminum foil from the viewpoint of suppressing the unpleasant odor of the composition.

[0055] In this specification, the occupancy rate (volume rate) of the composition in the package of an article is typically 25 to 90%, preferably 28 to 75%, and more preferably 30 to 50% when the package is a bottle package. Furthermore, when the package is a SP package, PTP package, pillow package, or stick package, the occupancy rate is typically 30 to 98%, preferably 40 to 95%, more preferably 45 to 93%, and particularly preferably 50 to 90%. In this case, the occupancy rate refers to the occupancy rate of the composition relative to the total volume inside the package; fillers, inner stoppers, and the like used to prevent damage to the composition stored inside the package are not taken into consideration when calculating the space occupancy rate.

[0056] As the airtight packaging body, commercially available packaging bodies may be used as they are, or commercially available packaging materials may be processed and used. Examples of commercially available bottle packaging bodies include glass bottles (manufactured by Isoya Glass Industry Co., Ltd.), tablet bottles (manufactured by Tokyo Glass Co., Ltd.), and the Z-series (manufactured by Hanshin Chemical Industry Co., Ltd.). Examples of commercially available pillow packaging bodies include Lamizip (registered trademark) (manufactured by Seisan Nippon Sha). Examples of packaging materials for SP packaging, PTP packaging, pillow packaging, and stick packaging include SUMILITE VSS, SUMILITE VSL, SUMILITE NS, and SUMILITE FCL (all manufactured by Sumitomo Bakelite Co., Ltd.), the TAS series (manufactured by Taisei Chemical Co., Ltd.), PTP vinyl foil, and PTP super foil (manufactured by Mitsubishi Plastics, Inc.), Nippaku aluminum foil (manufactured by Nippon Foil Co., Ltd.), and plain silver aluminum foil (manufactured by Daiwa Chemical Industry Co., Ltd.).

[0057] The method for placing the composition in the airtight package is not particularly limited, and can be achieved by placing the composition in the package by any appropriate means, such as by pouring the composition into the package. In this case, a desiccant (for example, a cylindrical (tablet) or sheet-shaped desiccant) may be poured into the package together with the composition.

[0058] In the present invention, the composition or article contains bilastine, which has histamine H1 receptor antagonistic activity and antiallergic activity, and is therefore particularly effective in treating or alleviating allergy and cold symptoms. Therefore, the pharmaceutical composition or article can be suitably used for treating or alleviating allergy and cold symptoms, more specifically, for treating or alleviating hives, itching and swelling due to eczema, rash, and pruritus, symptoms caused by acute rhinitis, allergic rhinitis, or sinusitis (sneezing, runny nose (excessive nasal discharge), nasal congestion, watery eyes, sore throat, heavy head, etc.), or cold symptoms (runny nose, nasal congestion, sneezing, etc.), and can be used, for example, as an oral allergy medication, oral rhinitis medication, or cold medicine. The present invention can also be used to treat or alleviate symptoms of rhinitis not caused by colds, particularly allergic symptoms of the nose (sneezing, runny nose, stuffy nose) caused by pollen, house dust (indoor dust), etc.

[0059] The route of administration of the pharmaceutical composition is not particularly limited and can be determined appropriately depending on the disease to be treated, the type of formulation, the gender, age, symptoms, etc. of the recipient, but oral administration is preferred from the viewpoint of ease of administration. Furthermore, the pharmaceutical composition can be taken in divided doses about 1 to 4 times a day, before meals, between meals, after meals, before bedtime, etc.

[0060] The present invention also relates to a deodorizer containing one or more compounds selected from the group consisting of bilastine, its salts, and solvates thereof (preferably, a deodorizer for an unpleasant odor containing (A) a component having an unpleasant odor). The ingredients and containers of the deodorizer may be those described above or those commonly used for deodorizers, medicines, foods, etc., as appropriate. The present invention also relates to a deodorizing method using one or more members selected from the group consisting of bilastine, its salts, and solvates thereof (preferably, (A) a method for deodorizing the unpleasant odor of a component having an unpleasant odor). Furthermore, the present invention provides a composition comprising the following components (A) and (B): (A) ingredients having an unpleasant odor; (B) one or more selected from the group consisting of bilastine, a salt thereof, and a solvate thereof; The present invention also relates to a method for suppressing an increase in unpleasant odors in a composition when the composition is sealed in an airtight package and stored, the method comprising the step of incorporating component (A) and component (B) into the same composition. In this aspect of the invention, the order of the step of incorporating component (A) and the step of incorporating component (B) is not particularly limited, as long as a composition containing component (A) and component (B) is produced directly or indirectly. In this aspect of the invention, the meanings of various terms, the amounts of each component, etc. are all the same as those explained for the "composition" above.

[0061] The present specification discloses the following embodiments, for example, but is not limited to these. [1A] The following components (A) and (B): (A) ingredients having an unpleasant odor; (B) one or more selected from the group consisting of bilastine, a salt thereof, and a solvate thereof; A composition comprising: [2A] The composition according to [1A], wherein component (A) is one or more members selected from the group consisting of pyridoxine, derivatives thereof, and salts thereof. [3A] The composition according to [1A] or [2A], which is packaged in an airtight package. [4A] The composition according to any one of [1A] to [3A], wherein the composition is a solid formulation. [5A] The composition according to any one of [1A] to [4A], wherein the composition is in the form of a tablet, capsule, granule, powder, or pill. [6A] A deodorant containing at least one member selected from the group consisting of bilastine, its salts, and solvates thereof. [7A] A deodorizing method using one or more compounds selected from the group consisting of bilastine, its salts, and solvates thereof. [8A] The following components (A) and (B): (A) ingredients having an unpleasant odor; A method for suppressing the increase of unpleasant odors when component (A) in a composition is sealed in an airtight package and stored, the method comprising the step of incorporating into the same composition component (A) and one or more members selected from the group consisting of bilastine, its salts, and solvates thereof. [Example]

[0062] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples. In the following test examples, the amount of each component used is the amount of the indicated component itself, unless otherwise specified as a converted amount.

[0063] [Test example] Mixing test After preparing each of the following samples 1 and 2, a sensory evaluation was conducted by a specialist panel member to check whether the samples had an unpleasant odor.

[0064] [Sample 1] Pyridoxine (manufactured by BASF Japan, trade name: pyridoxine hydrochloride) was placed in a transparent vial (manufactured by Thermo Fisher Scientific: screw cap bottle C5000-192W, internal volume 1.5 mL), and this was designated as Sample 1. [Sample 2] One part by mass of pyridoxine (manufactured by BASF Japan, trade name: Pyridoxine Hydrochloride) and one part by mass of bilastine (manufactured by Sumitomo Chemical, trade name: Bilastine) were placed in a transparent vial (manufactured by Thermo Fisher Scientific: screw cap bottle C5000-192W, internal volume 1.5 mL) and mixed; this was designated Sample 2.

[0065] Sample 1 had an odor similar to that of rotten fish, whereas Sample 2, which contained bilastine, had no such odor.

[0066] [Test example] Preservation test Samples 3 and 4 shown below were prepared and stored at 40°C and 75% RH, and a specialist panel member performed a sensory evaluation to check for the presence or absence of an unpleasant odor and any change in its intensity after 14 days. The results are shown in Table 1.

[0067] [Sample 3] Pyridoxine (manufactured by BASF Japan, trade name: pyridoxine hydrochloride) was placed in a transparent vial (manufactured by Thermo Fisher Scientific: screw cap vial C5000-192W, capacity 1.5 mL), and the vial was capped. This was designated Sample 3. [Sample 4] One part by mass of pyridoxine (manufactured by BASF Japan, trade name: Pyridoxine Hydrochloride) and one part by mass of bilastine (manufactured by Sumitomo Chemical, trade name: Bilastine) were placed in a transparent vial (manufactured by Thermo Fisher Scientific: screw cap vial C5000-192W, internal volume 1.5 mL), mixed, and the vial was capped. This was designated Sample 4.

[0068] [Table 1]

[0069] An increase in odor intensity was observed after 14 days of storage in Sample 3. On the other hand, no such odor was observed in Sample 4 containing bilastine even after 14 days of storage.

[0070] The above test results demonstrate that the unpleasant odor caused by component (A), such as pyridoxine, can be suppressed by incorporating component (B), such as bilastine.

[0071] Manufacturing Example 1 (Tablets) Tablets containing the following ingredients and amounts per daily dose are manufactured in a conventional manner and packed in PTP packages. Bilastine 20mg Dipotassium glycyrrhizinate 25mg Pyridoxine hydrochloride 15mg Caffeine anhydrous 20mg Microcrystalline cellulose, sodium starch glycolate, light anhydrous silicic acid, magnesium stearate

[0072] Manufacturing Example 2 (Tablets) Tablets containing the following ingredients and amounts per daily dose are manufactured in a conventional manner and packed in PTP packages. Pyridoxine hydrochloride 15mg Belladonna total alkaloids 0.2mg Bilastine 20mg Dipotassium glycyrrhizinate 25mg Microcrystalline cellulose, sodium starch glycolate, light anhydrous silicic acid, magnesium stearate

[0073] Manufacturing Example 3 (Tablets) Tablets containing the following ingredients and amounts per daily dose are manufactured in a conventional manner and packed in PTP packages. Pyridoxine hydrochloride 15mg Bilastine 20mg Dipotassium glycyrrhizinate 25mg Riboflavin 6mg Microcrystalline cellulose, sodium starch glycolate, light anhydrous silicic acid, magnesium stearate

[0074] Manufacturing Example 4 (Tablets) Tablets containing the following ingredients and amounts per daily dose are manufactured in a conventional manner and packed in PTP packages. Pyridoxine hydrochloride 15mg dl-methylephedrine 10mg Bilastine 20mg Riboflavin 6mg Microcrystalline cellulose, sodium starch glycolate, light anhydrous silicic acid, magnesium stearate [Industrial Applicability]

[0075] According to the present invention, by incorporating one or more components selected from the group consisting of bilastine, its salts, and solvates thereof, it is possible to provide a composition in which the unpleasant odor of components having an unpleasant odor is suppressed, and the composition can be used, for example, in the pharmaceutical industry.

Claims

1. The following components (A) and (B): (A) a component having an unpleasant odor; (B) one or more selected from the group consisting of bilastine, a salt thereof, and a solvate thereof; A composition comprising:

2. 2. The composition according to claim 1, wherein component (A) is one or more selected from pyridoxine, its derivatives, and salts thereof.

3. The composition according to claim 1 or 2, wherein the composition is a solid formulation.

4. The composition according to claim 1 or 2, wherein the composition is in the form of a tablet, capsule, granule, powder or pill.

5. A deodorizer containing at least one member selected from the group consisting of bilastine, its salts, and solvates thereof.

6. A deodorizing method using one or more members selected from the group consisting of bilastine, its salts, and solvates thereof.

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