JP4667244B2 - Pharmaceutical composition - Google Patents

Description

  The present invention relates to a pharmaceutical composition that quickly improves unpleasant symptoms such as irritations, nausea, and hangover after alcohol consumption.

In general, excessive consumption of alcohol is known to cause unpleasant symptoms such as irritations, nausea, and hangovers. For this reason, many gastrointestinal drugs in combination with herbal medicines and antacids are commercially available to improve these unpleasant symptoms such as hangover. However, various researches on new drugs have been conducted due to the problem that sufficient effects are not yet obtained. As such researches, for example, a blend of processed potato, carrot and antacid (Patent Document 1), a blend of oxon, turmeric and shochu (Patent Document 2) are known. However, it cannot be said that sufficient effects have been obtained in these studies. In addition, in order to obtain a sufficient effect, it is necessary to increase the dose, which causes problems such as a decrease in compliance and restrictions on the combination of other medicinal ingredients, which are not always satisfactory.
JP-A-8-99890 JP 2003-226650 A

  Accordingly, an object of the present invention is to provide a pharmaceutical composition that quickly improves unpleasant symptoms such as irritations, nausea, and hangover after alcohol consumption.

  In view of such circumstances, the present inventors have conducted intensive research, and as a result, unexpectedly found that the combined use of processed garlic and turmeric promotes a decrease in blood alcohol concentration, and the present invention has been completed.

That is, the present invention provides a pharmaceutical composition containing processed garlic and turmeric.
The present invention also provides a method for promoting reduction in blood alcohol concentration, which comprises administering an effective amount of processed garlic and turmeric.
The present invention also provides the use of processed garlic and turmeric for the production of a pharmaceutical composition.

  In addition, the effects of processed garlic are known to be fatigue recovery, nourishing tonic, gastric contraction enhancing action, metabolism promoting action, blood flow promoting action, liver protecting action, etc. However, there are no known examples that promptly improve unpleasant symptoms such as irritations, nausea, and hangover after alcohol consumption.

  The pharmaceutical composition of the present invention can quickly improve unpleasant symptoms such as irritations, nausea, and hangover after ingesting alcohol by combining a processed garlic product and turmeric.

It is a figure which shows the blood alcohol concentration reduction effect | action of each chemical | medical agent sample after ethanol administration.

  The processed garlic used in the present invention is obtained by processing bulbs of Allium sativum l. Garlic. Processing is, for example, by drying raw garlic into powder, extracting raw garlic with steam distillation, oil, water, hot water, water-soluble organic solvent, etc., or treating raw garlic with heating, etc. is there. Examples of the oil used for the extraction include edible vegetable oils such as rapeseed oil, olive oil, and soybean oil. Examples of the water-soluble organic solvent include lower alcohols such as ethanol and isopropanol; glycols such as propylene glycol and diethylene glycol.

  The garlic processed product is not particularly limited as long as it is as described above, but, for example, processed potato, garlic extract, garlic extract, dried garlic and the like are preferable, and processed potato is particularly preferable. Here, the processed oat is a garlic powder or extract obtained by extracting a heat-treated garlic extract through a process such as lower alcohol extraction. For example, oxoamidin (registered trademark) (manufactured by Riken Chemical Industry Co., Ltd.), oxoamidin powder (Registered trademark) (manufactured by Riken Chemical Industry Co., Ltd.), oxoresin (registered trademark) (manufactured by Riken Chemical Industry Co., Ltd.), oxoresin powder (registered trademark) (manufactured by Riken Chemical Industry Co., Ltd.) and the like are commercially available. As the garlic extract, for example, garlic extract (manufactured by Alps Pharmaceutical Co., Ltd.), garlic extract (manufactured by Nippon Powder Chemical Co., Ltd.) and the like are commercially available. As the dried garlic, for example, garlic powder, roasted garlic powder EX (manufactured by Riken Chemical Industry Co., Ltd.) and the like are commercially available. Among these commercially available garlic products, oxoamidin (registered trademark) (manufactured by Riken Chemical Industry Co., Ltd.), oxoamidin powder (registered trademark) (manufactured by Riken Chemical Industry Co., Ltd.), oxoresin (registered trademark) (RIKEN CHEMICAL CO., LTD.) Kogyo Kogyo Co., Ltd.) Oxoresin powder (registered trademark) (manufactured by Riken Chemical Co., Ltd.) is preferred.

  The processed garlic product used in the present invention is preferably 0.01 to 20% by weight, particularly preferably 0.05 to 10% by weight, based on the preparation. If the blending amount is less than 0.01% by weight, the intended effect cannot be obtained. If the blending amount exceeds 20% by weight, the odor is strong, and it is not preferable because a separate odor masking technique needs to be introduced.

  The turmeric used in the present invention is the one obtained by passing the rhizome of the ginger family Curcuma longa, Curcuma aromatica as it is or boiled except the pericarp, turmeric, turmeric powder, turmeric extract, turmeric dry extract, turmeric dry extract, turmeric Examples thereof include soft extracts, fermented turmeric, and the like, for example, turmeric powder (manufactured by Nippon Powder Chemical Co., Ltd.), turmeric extract (manufactured by Nippon Powder Chemical Co., Ltd., Maruzen Pharmaceutical Co., Ltd.) and the like are commercially available.

  The turmeric used in the present invention is preferably from 0.1 to 60% by weight, particularly preferably from 0.5 to 30% by weight, based on the drug product, in terms of the drug substance. If the blending amount is less than 0.1% by weight, the effect cannot be obtained. If the blending amount exceeds 60% by weight, the astringency is increased, which is not preferable from the viewpoint of taking feeling.

  The weight ratio of the processed garlic and turmeric in the pharmaceutical composition of the present invention is 1: 300 to 1: 0.3, more preferably 1:15 to 1: 1, particularly 1:12 to 1: 3. preferable. Within this range, side effects are reduced and turmeric is excellent at low doses. In calculating the weight ratio, the weight of the processed garlic product is the weight excluding the extraction solvent in the case of a solvent extract, and the dry weight excluding moisture in other cases.

  In the pharmaceutical composition of the present invention, other drugs and additives can be used as necessary. Examples of other drugs include antacids, healthy stomachs, digestives, intestinal regulating agents, antipruritics, analgesics and antispasmodic agents, gastric mucosal repair agents, vitamins, antifoaming agents and the like.

  Examples of the antacid include magnesium hydroxide, sodium bicarbonate, calcium carbonate, magnesium carbonate, aminoacetic acid, funnel extract, magnesium silicate and the like.

  Examples of the stomachic agent include, for example, aniseed fruit, aloe, fennel, cypress, life-prolonging grass, cormorant, duckweed, auren, gadget, cuckoo, calamus root, dry rice, chaff, pheasant, caihi, gentian, kojin, koboku, goshuyu, cucumber, Colombo, Consulango, Salamander, Yamana, Shisoshi, Shukusha, Shoyo, Shozuk, Blue peel, Stone root, Centaurium grass, Assembly, Sojutsu, Soyo, Daimuka, Daiou, Chikutsujinjin, Choji, Chimpi, Pepper, Spruce, Animal Gall (including Yutan), Nigaki, Nikuzuku, carrot, mint (including Atlantic mint), repellent (Prunus), peanut, hop, Homika extract, sleepy leaf (Saisai), mokko, Yakuchi, Ryutan, Ryokyo, fennel Oil, cinnamon oil, sho Kyo oil, cardamom oil, clove oil, spruce oil, peppermint oil, lemon oil, l-menthol, dl-menthol, betaine hydrochloride, glutamic acid hydrochloride, carnitine chloride, bethanechol chloride, dry yeast and the like.

  Examples of the digestive agent include starch digestive enzyme, protein digestive enzyme, fat digestive enzyme, fibrin digestive enzyme, ursodesoxycholic acid, oxycoranoates, cholic acid, bile powder, bile extract (powder), dehydrocol Acid, animal gall (including yutan) and the like.

  Examples of the intestinal regulating agent include live intestinal fungi components, red buds, asenyaku, bai, tsutsumeishi, genokosho and the like.

  Antidiarrheal agents include, for example, acrinol, berberine chloride, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, berberine tannate, bismuth subsalicylate, bismuth subnitrate, bismuth subcarbonate, bismuth subgallate, tannic acid, albumin tannate , Methylene thymol tannin, kaolin, pectin, medicinal charcoal, calcium lactate, Acacia yam, buckwheat, duckweed, auren, kudin, ganodermone, pentaploid, hawthorn, yellowtail, ivy.

  Examples of analgesic antispasmodic agents include oxyphencyclimine hydrochloride, dicyclomine hydrochloride, methixene hydrochloride, scopolamine hydrobromide, methyl atropine bromide, methyl anisotropine bromide, methyl scopolamine bromide, methyl-1-hyostiamine bromide, Methylbenactidium bromide, belladonna extract, isopropamide iodide, diphenylpiperidinomethyldioxolane iodide, funnel extract, funnel root total alkaloid citrate, papaverine hydrochloride, ethyl aminobenzoate, engosaku, licorice, kuboku, peonies, etc. Is mentioned.

  Examples of the gastric mucosa repairing agent include sodium azulenesulfonate, aldioxa, glycyrrhizic acid and salts thereof, and licorice extract, L-glutamine, copper chlorophyllin potassium, copper chlorophyllin sodium, histidine hydrochloride, porcine gastric wall pepsin degradation product, porcine gastric wall acid Examples include hydrolysates, methylmethionine sulfonium chloride, red buds, engosaku, and licorice.

Examples of vitamins include nicotinamide, calcium pantothenate, biotin, vitamin B ₁ or a derivative or salt thereof, vitamin B ₂ or a derivative or salt thereof, vitamin B ₆ or a derivative or salt thereof, vitamin C or Examples thereof include derivatives thereof and salts thereof.

  Examples of the antifoaming agent include dimethylpolysiloxane.

Examples of additives include excipients, binders, disintegrants, lubricants, colorants, and flavoring agents.
Examples of the excipient include lactose, starches, crystalline cellulose, sucrose, mannitol, light anhydrous silicic acid and the like. Examples of the binder include hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, pregelatinized starch, polyvinylpyrrolidone, polyvinyl alcohol, pullulan and the like. Examples of the disintegrant include carmellose, carmellose calcium, croscarmellose sodium, crospovidone, corn starch, and low-substituted hydroxypropylcellulose. Examples of the lubricant include magnesium stearate and talc. Examples of the colorant include tar pigments and iron sesquioxide. Examples of the corrigent include stevia, aspartame, and fragrances.

  The pharmaceutical composition of the present invention is a dosage form for oral administration such as liquid, powder, granule, tablet, chewable tablet, film-coated tablet, sugar-coated tablet, soft capsule, hard capsule, jelly and the like according to the purpose. Can be manufactured. Of these dosage forms, a liquid for internal use or a granule is particularly preferred.

  The pharmaceutical composition of the present invention, as shown in Examples below, has the effect of promoting a decrease in blood alcohol concentration after alcohol intake, and improves various unpleasant symptoms such as irritations, nausea and hangover after alcohol intake Useful as a medicine.

The pharmaceutical composition of the present invention is preferably used internally as such a symptom improving agent.
Garlic processed products and turmeric components are restricted in daily usage and for reasons of efficacy, garlic processed products range up to 0.2 g / day, turmeric is 6 g / day in terms of bulk drug substance However, the single dose is preferably in the range of 0.01 to 0.1 g for processed garlic and in the range of 0.1 to 2 g in terms of active ingredient for turmeric.

  The pharmaceutical composition of the present invention can be taken after alcohol intake (especially the next day), before or during ingestion, and is taken in 1 to 3 times per day depending on the degree of discomfort or prevention expected. It is preferable to do.

  Hereinafter, the present invention will be specifically described by way of examples, but the present invention is not limited thereto.

Experimental example 1
The blood ethanol concentration lowering effect was examined according to the following experimental method.
<Experiment method>
Using Wistar male rats (8-9 weeks old) fasted overnight, a drug sample was orally administered, and 1 hour later, pentobarbital (30 mg / kg) was intraperitoneally administered and anesthetized. Furthermore, 0.5 hours after that, ethanol physiological saline (0.5 g / kg) was intravenously administered, and blood was collected from the tip of the tail 40 minutes after administration of ethanol physiological saline. The alcohol concentration in the collected blood was measured using F kit ethanol (manufactured by JK International). There are 4 groups of drug samples: control, turmeric powder 100 mg / kg, oxoamidin powder 10 mg / kg and turmeric powder 100 mg / kg + oxoamidin powder 10 mg / kg (invention). These were dissolved or suspended in water and administered (10 mL / kg). The result is shown in FIG.

  In contrast to the control, 100 mg / kg of turmeric powder decreased the blood concentration of alcohol (ethanol), but the same effect was hardly observed with 10 mg / kg of oxoamidin powder. In preliminary experiments, it has been confirmed that the effect of turmeric blood alcohol concentration reduction reaches equilibrium at 100 mg / kg of turmeric powder. However, the combined use of turmeric powder 100 mg / kg and oxoamidin powder 10 mg / kg was confirmed to promote a stronger blood alcohol concentration lowering effect than turmeric powder 100 mg / kg alone. The average blood alcohol concentration ratio of each group is 0.818 for the turmeric powder group and 0.949 for the oxoamidin powder group when the control is 1, and the product (0.776) is the turmeric powder and oxoamidin powder combination group. The effect of turmeric in reducing blood alcohol concentration was greatly promoted by the combined use with oxoamidin powder (Burgi method).

Production Example 1
To 500 L of purified water (80 to 90 ° C.), 500 g of sodium benzoate and 40 g of ethyl paraoxybenzoate, 70 kg of purified white sugar and 3 kg of carmellose sodium are added and dissolved while stirring. After cooling this solution, 377 g of thiamine nitrate and 100 g of sodium hydrogen phosphate are added and dissolved while stirring. Separately, 200 g of purified water (80-90 ° C.), 1.4 kg of ginseng dry extract (20 kg as ginseng), 1.3 kg of oxoamidin powder, 970 g of pepper extract (10 kg as pepper), 11 L of turmeric extract (11 kg as turmeric), Add 1.5 kg of citric acid and 1.5 kg of tartaric acid, cool the solution dissolved with stirring, and filter. After these two liquids are mixed, 167 g of mint oil, 33 g of fennel oil, and 33 g of clove oil are added and mixed while stirring. An internal liquid was prepared by adding an appropriate amount of purified water to this mixed solution to bring the total amount to 1000 L.

Production Example 2
To 500 L of purified water (80 to 90 ° C.), 0.7 kg of sodium benzoate and 0.14 kg of butyl paraoxybenzoate, 70 kg of purified white sugar and 6 kg of carmellose sodium are added and dissolved while stirring. After cooling this liquid, dried carrot extract 1.8 kg (25 kg as carrot) and oxoamidin powder 0.6 kg, pepper extract 6 L (6 kg as pepper), turmeric extract 6 L (6 kg as turmeric), fennel extract 6 L (6 kg as fennel), 6L clove extract 6L (6kg as clove) and 0.5L fragrance are added and dissolved by stirring. Separately, 6 kg of synthetic hydrotalcite is added to 300 L of purified water (80 to 90 ° C.), stirred and mixed, and then circulated and dispersed with a high-pressure homogenizer. After cooling the dispersion, an appropriate amount of purified water was added to the mixture with the previous mixture to make the total volume 1000 L, whereby an internal liquid was prepared.

Production Example 3
Add 12 parts by mass of ethanol to a mixed powder consisting of 40 parts by mass of oxoamidin powder, 25 parts by mass of vitamin B ₁ , 50 parts by mass of hardened oil, 20 parts by mass of glyceryl monostearate, 15 parts by mass of corn starch, and 15 parts by mass of carmellose calcium. A kneaded product was made. The kneaded product was extruded and granulated (φ0.8 mm), dried, sized and classified to obtain granules (hereinafter referred to as A granules).
Also, 450 parts by weight of dry aluminum hydroxide gel, 325 parts by weight of magnesium hydroxide, 450 parts by weight of synthetic hydrotalcite, 75 parts by weight of licorice extract powder, 200 parts by weight of fennel powder, 200 parts by weight of turmeric powder, 20 parts by weight of carrot dry extract Parts of polyvinyl alcohol, 70 parts by weight of polyvinyl alcohol, 30 parts by weight of carmellose calcium, 40 parts by weight of crystalline cellulose, and 1545 parts by weight of xylitol were added with 800 parts by weight of 70% ethanol to prepare a kneaded product. The kneaded product was extruded and granulated (φ0.8 mm), dried, sized and classified to obtain granules (hereinafter referred to as B granules).
Furthermore, 6 parts by mass of l-menthol was adsorbed on 24 parts by mass of magnesium aluminate metasilicate to obtain a fragrance powder (hereinafter referred to as C fragrance powder).
165 parts by mass of A granule, 3405 parts by mass of B granule and 30 parts by mass of C fragrance powder were mixed with a mixer, and further packaged with a packaging machine to obtain a granule having a single dose of 1.2 g.

Production Example 4
Add 12 parts by mass of ethanol to a mixed powder consisting of 30 parts by mass of oxoamidin powder, 25 parts by mass of vitamin B ₁ , 55 parts by mass of hardened oil, 25 parts by mass of glyceryl monostearate, 15 parts by mass of corn starch and 15 parts by mass of carmellose calcium. A kneaded product was made. The kneaded product was extruded and granulated (φ0.5 mm), dried and sized to obtain granules (hereinafter referred to as D granules).
Also, 450 parts by weight of dry aluminum hydroxide gel, 325 parts by weight of magnesium hydroxide, 450 parts by weight of synthetic hydrotalcite, 75 parts by weight of licorice extract powder, 200 parts by weight of fennel powder, 200 parts by weight of turmeric powder, 100 parts by weight of ginger powder Parts, carrot dry extract 20 parts by weight, hydroxypropylcellulose 90 parts by weight, carmellose calcium 30 parts by weight, crystalline cellulose 30 parts by weight, erythritol 1445 parts by weight, and 90% ethanol 700 parts by weight. Made. The kneaded product was dried and sized to obtain granules (hereinafter referred to as E granules).
Furthermore, 4 parts by mass of l-menthol was adsorbed on 16 parts by mass of magnesium aluminate metasilicate to obtain a fragrance powder (hereinafter referred to as F fragrance powder).
165 parts by mass of D granules, 3415 parts by mass of E granules, and 20 parts by mass of F fragrance powder were mixed with a mixer, and further packaged with a packaging machine to obtain a granule having a single dose of 1.2 g.
In addition, when the internal use liquid of Production Examples 1 and 2 and the granules of Production Examples 3 and 4 were taken, unpleasant symptoms such as irritations, nausea and hangover after alcohol intake can be quickly improved for any preparation. It was.

Claims (4)

A pharmaceutical composition for promoting a decrease in blood alcohol concentration after alcohol intake , comprising a processed garlic product and turmeric in a weight ratio of 1:15 to 1: 1 . Nikuniku workpiece machining garlic der Ru pharmaceutical composition of claim 1. The pharmaceutical composition according to claim 1 or 2 , which is an oral preparation for oral administration. The pharmaceutical composition according to any one of claims 1 to 3 , which improves the unpleasant symptoms of irritations, nausea or hangover after alcohol intake .

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