Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
  • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/13—Amines
  • A61K31/132—Amines having two or more amino groups, e.g. spermidine, putrescine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/7012—Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/08—Solutions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/02—Nutrients, e.g. vitamins, minerals
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• the present invention relates to an internal use solution containing dalcronolatone and dichloroacetic acid diisopropylamine, and more particularly to a composition having an improving effect on liver function and a fatigue recovery effect.
• dalchronolaton has been used to improve liver function, treat urticaria, eczema, poisoning eruption, pregnancy embarrassment, pregnancy toxemia and the like.
• the internal use solution containing muscular dalcronolaton which is a useful drug known to be effective as a preventive agent for alcoholic fatty liver caused by a large intake of alcohol and fat, further improves liver function.
• Patent Document 1 Japanese Patent Laid-Open No. 10-298093
• the present invention has been made in view of the above circumstances, and contains dalchronolaton.
• the purpose of this solution is to further improve the liver function improving effect and fatigue recovery effect at a specific compounding ratio that will impair the flavor of the liquid drug while ensuring the stability of dalcronolaton in the liquid drug.
• the present inventors do not impair the flavor of the liquid agent! /, A component that can stably coexist with dalcronolaton, which is stable on the acidic side, and can further improve the liver function improving action.
• the present invention provides a liquid for internal use characterized by containing glucuronolatatone and diisopropylamine dichloroacetate.
• the formulation pH of the liquid for internal use is 1.5 to 3.0.
• the blending ratio (mass ratio) of dalcronolaton and dichloroacetate diisopropylamine is 3
• the formulation pH means the pH of a liquid for internal use that is stored as a final product and used for taking.
• the liquid for internal use of the present invention contains (A) dalcronolatone and (B) diisopropylamine dichloroacetate.
• Dalcronolaton is used as a general term for dalcronolatone and dalucoric acid or salts thereof.
• Dalcronolaton is a component that improves the liver's function. Specifically, it has the effect of increasing the blood flow of the liver and enhancing the detoxification ability, and has few side effects. It can also be applied to urticaria, eczema and pregnancy poisoning.
• Dalcronolatone may be a commercial product or may be appropriately synthesized.
• the method for synthesizing dull chronoraton can be appropriately selected according to the purpose without any particular limitation.
• the content of (A) dalcronolaton in the internal use liquid preparation of the present invention can be appropriately selected according to the purpose without any particular limitation.
• mass% for example, 0.01 to 10.0 mass% is preferable, and 0.1 to 5.0 mass% is more preferable.
• mgZmL unit for example, 10 mgZ100 mL to 2,000 mgZ20 mL, preferably 100 mg / 100 mL to 1, OOOmg Z20 mL is more preferable.
• the content is at least the lower limit of the above content, a good effect of dalchronolaton can be obtained.
• the unpleasant taste (bitter taste) peculiar to dalcronolaton is suppressed, and the flavor of the liquid preparation is not impaired.
• Diisopropylamine dichloroacetate is a component that improves the function of the liver. Specifically, it promotes the formation of liver cells.
• Diisopropylamine dichloroacetate may be a commercially available product or an appropriately synthesized product.
• the method for synthesizing diisopropylamine dichloroacetate can be appropriately selected according to the purpose without any particular limitation.
• the content of (B) dichloroacetate diisopropylamine in the internal use liquid preparation of the present invention is not particularly limited and can be appropriately selected according to the purpose.
• the mass percent for example, 0.003 to 0.5 mass 0/0 Power
• mass percent for example, 0.003 to 0.15 mass 0/0 force ⁇ preferably from! / ⁇ .
• 3mgZlOOmL to 100mgZ20mL is preferred 3mg / 100mL to 30mgZ20mL force is preferred! /.
• a good effect by diisopropylamine dichloroacetate can be obtained.
• the burden on the liver can be reduced, and liver cell neoplasia can be promoted more efficiently.
• (A) dalchronolatone and (B) dichloroacetic acid diisopropylamine are not particularly limited in their blending ratio, and within the preferred ranges of the respective contents described above. They can be used in appropriate combinations according to the purpose.
• the preparation pH (25 ° C) of the liquid for internal use of the present invention is preferably 1.5 to 3.0, and a pH adjuster is added as necessary.
• a more preferable range of the preparation pH is 2.0 to 3.0, and a particularly preferable range is 2.2 to 2.8.
• the formulation pH is at least the lower limit of the above range, the acidity is not too strong and the flavor of the solution is not impaired.
• Good stability of (A) dalchronolaton can be obtained by adjusting the formulation pH to not more than the upper limit of the above range.
• (B) dichloroacetate disopropylamine has good stability.
• the pH adjuster is not particularly limited and may be appropriately selected according to the purpose. Examples thereof include hydrochloric acid, dilute hydrochloric acid, citrate, sodium citrate, glycine, darcono ⁇ -latathone, succinic acid, Acetic acid, tartaric acid, D tartaric acid, sodium hydroxide, potassium hydroxide, magnesium hydroxide, lactic acid, calcium lactate, glacial acetic acid, sodium fumarate, maleic acid, anhydrous citrate, DL-malic acid, aspartic acid, glutamic acid PH adjusters such as adipic acid, darconic acid, fumaric acid, sodium hydrogen carbonate, and the like.
• the above pH adjusters can be used alone or in combination of two or more.
• the internal use liquid preparation of the present invention can contain optional components as long as the effects of the present invention are not impaired.
• optional ingredients include vitamins, sweeteners, preservatives (preservatives), stabilizers, preservatives, solubilizers, solvents, solubilizers, suspension agents, antioxidants, and flavoring agents.
• Perfumes refreshing agents, coloring agents, buffering agents, herbal medicines, caffeine, royal jelly, etc.
• the addition amount of these arbitrary components can be blended in a normal amount within a range not hindering the effects of the present invention.
• the vitamins are not particularly limited and can be appropriately selected according to the purpose.
• vitamin A vitamin Bl such as thiamine nitrate
• vitamin B2 such as riboflavin sodium phosphate
• nicotinamide Vitamin B6
• pyridoxine hydrochloride vitamin B12
• vitamin D vitamin D
• vitamin E vitamin C
• vitamins such as calcium pantothenate.
• the above vitamins can be used alone or in combination of two or more.
• the sweetener is not particularly limited and may be appropriately selected depending on the purpose.
• the preservative is not particularly limited and may be appropriately selected depending on the purpose.
• benzoic acid sodium benzoate, ethanol, sodium edetate, dried sodium sulfite, agar, dl —Camphor, citrate, sodium citrate, glycerin, salicylic acid, sodium salicylate, salicylic acid phenol, dibutylhydroxytoluene, D Sorbitol, sorbic acid, potassium sorbate, sodium dehydroacetate, sucrose, honey honey, isoptyl noroxybenzoate, isopropyl noroxybenzoate, ethyl parabenzoate, ptyl noroxybenzoate, propyl noroxybenzoate, paraoxy Preservatives such as methyl benzoate, propylene glycol, 1 menthol and eucalyptus oil.
• the above preservatives can be used alone or in combination of two or more.
• the stabilizer can be appropriately selected according to the purpose without any particular limitation.
• a known method for preparing the liquid for internal use of the present invention a known method without particular limitation can be appropriately used.
• it can be produced according to the section of the Japanese Pharmacopoeia General Formulation “Liquid”, filtered and sterilized.
• the liquid for internal use of the present invention is taken orally as a liquid internal preparation.
• the intake is not particularly limited and can be selected appropriately according to the purpose. However, for adults, (A) Dalcronolaton per dose is 30 to 10,000 mg (0.03 to 10 g ) And (B) Diisopropylamine diacetamine is preferably taken once a day within a range of 3 to 500 mg (0.003 to 0.5 g).
• the liquid for internal use of the present invention is a component that improves the function of the liver and has high stability in the acidic region.
• A In addition to dalcronolaton, it is a component that improves the function of the liver and is acidic. Since it contains diisopropylamine dichloroacetate, which is highly stable under the conditions, the stability of the active ingredient is high, and an excellent liver function improving effect and fatigue recovery effect can be obtained.
• (B) Addition of diisopropylamine dichloroacetate does not significantly reduce the flavor.
• Diisopropylamine dichloroacetate is preferred as described above. ⁇ .
• the obtained liquid for internal use was evaluated for stability and liver function improving action (7-step sensory evaluation as fatigue recovery effect) and fatigue recovery effect (flicker value) by the following methods.
• the evaluation results are shown in the following table.
• a brown glass bottle was filled with the solution for internal use and stored at 60 ° C for 3 weeks, and the content of darcronoraton before and after storage was measured.
• the ratio (mass basis) of the content after storage to the content value (initial value) before storage (immediately after preparation) was determined, and the stability was evaluated based on the following evaluation criteria. It is determined that the effect of the present invention has been confirmed with an evaluation of “ ⁇ ” or higher.
• A Very stable (remaining rate is 95% or more and 100% or less with respect to the initial value).
• ⁇ Stable (remaining rate is 90% or more and less than 95% with respect to the initial value).
• liver function improving action (fatigue recovery effect) was evaluated by the following method.
• the liquid solution for internal use was filled in a brown glass bottle, which was taken by 10 panelists, and the degree of recovery of fatigue the next day was sensory evaluated based on the following evaluation criteria, and the average value of 10 people was obtained. It is judged that the effect of the present invention was confirmed with an average value of 5.0 or more.
• the liver function improving effect (fatigue recovery effect) was evaluated by the following method using a flicker measuring device (Takei Kikai Kogyo Co., Ltd., trade name: Digital Flicker T. K. K. 502).
• the flicker value represents the boundary at which blinking light is recognized as continuous light, not as intermittent light, in terms of light frequency (Hz). It can be assumed that the larger this value, the less visual fatigue. A typical normal value was 35 Hz, and the initial value in this measurement was about 35 Hz.
• Polyvinyl alcohol 200 200 Sodium benzoate 60 60 60 60 60 Sucrose 15000 15000 15000 15000 10000 Fragrance 10 10 10 10 10 Dilute hydrochloric acid ⁇ Suitable ⁇
• liquid for internal use of this invention can be utilized in field

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• 2006
  • 2006-09-28 JP JP2007552867A patent/JP5295571B2/ja active Active
  • 2006-09-28 WO PCT/JP2006/319315 patent/WO2007077656A1/ja active Application Filing
  • 2006-09-28 CN CN2006800468994A patent/CN101330920B/zh active Active
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