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WO2003063855A1 - Comprime a macher contenant des acides amines ramifies - Google Patents

Comprime a macher contenant des acides amines ramifies Download PDF

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Publication number
WO2003063855A1
WO2003063855A1 PCT/JP2003/000580 JP0300580W WO03063855A1 WO 2003063855 A1 WO2003063855 A1 WO 2003063855A1 JP 0300580 W JP0300580 W JP 0300580W WO 03063855 A1 WO03063855 A1 WO 03063855A1
Authority
WO
WIPO (PCT)
Prior art keywords
chewable
isoleucine
leucine
amino acids
chewable tablet
Prior art date
Application number
PCT/JP2003/000580
Other languages
English (en)
Japanese (ja)
Inventor
Mitsuyasu Ida
Hiroyuki Higuchi
Akira Yabuki
Original Assignee
Ajinomoto Co., Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ajinomoto Co., Inc. filed Critical Ajinomoto Co., Inc.
Publication of WO2003063855A1 publication Critical patent/WO2003063855A1/fr

Links

Classifications

    • 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
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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

Definitions

  • the present invention relates to a medicinal readable drug having excellent stability during handling and storage, comprising three kinds of branched-chain amino acids of isoleucine, leucine and palin as active ingredients.
  • compositions containing three types of branched-chain amino acids consisting of isoleucine, leucine and palin as active ingredients are effective remedies for liver diseases, and currently commercially available preparations are mainly granules.
  • granules containing the above three kinds of branched-chain amino acid particles as an active ingredient a single dose was about 5 g, which was significantly larger than that of a general preparation, and had a drawback that it was difficult to take.
  • a chewable preparation which is taken or dissolved or taken in the mouth can be said to be a preferable dosage form.
  • a chewable preparation which is taken or dissolved or taken in the mouth
  • it is required to have both the property of rapidly disintegrating in the mouth and the property of having the strength not to disintegrate due to the impact in the manufacturing process and distribution process, and at the same time the chemical alone or the drug
  • the additives have stability during storage such that they do not cause deterioration due to oxygen, moisture, temperature, etc.-browning phenomenon. Disclosure of the invention
  • An object of the present invention is to provide a tiable agent containing three types of branched chain amino acids of isoleucine, leucine and palin as active ingredients, which are not colored during storage and have good storage stability.
  • the present inventors have conducted intensive studies and as a result, in the case of a tiable agent containing three kinds of branched-chain amino acids of iso- mouth, leucine and valine, a magnesium compound is contained. And preserved without coloring even during storage The inventors have found that a tunable agent containing a branched-chain amino acid having good stability can be prepared, and have completed the present invention.
  • the present invention includes the following inventions.
  • a chewable preparation comprising three kinds of branched-chain amino acids of isoleucine, leucine and palin as an active ingredient and a magnesium compound.
  • the magnesium compound is at least one selected from magnesium stearate, talc, and magnesium aluminate methacrylate.
  • the chewable preparation contains at least one flavoring / flavoring agent selected from sweeteners, sour agents, menthol, etc. in order to improve ingestibility.
  • the chewable preparation of the present invention is a chewable preparation manufactured using three types of branched-chain amino acids consisting of isoleucine, leucine and palin as active ingredients.
  • Isoleucine which is one of the active ingredients in the chewable preparation of the present invention, is generally a particle having a particle size of 1 mm or less produced by a fermentation method, and is selected from the Japanese Pharmacopoeia, the United States Pharmacopeia, and the European Pharmacopoeia. Those that meet the standards of are used, but there is no particular restriction on the particle size.
  • leucine which is one of the active ingredients
  • leucine is generally manufactured by a fermentation method or an extraction method and has a particle size of lmm or less, and can be any of the standards of the Japanese Pharmacopoeia, the United States Pharmacopeia, and the European Pharmacopoeia. Are used, but there is no particular restriction on the granularity.
  • palin one of the active ingredients, is generally manufactured by a fermentation method or a synthesis method and has a particle size of 1 mm or less, and is selected from the Japanese Pharmacopoeia, the United States Pharmacopeia, and the European Pharmacopoeia. Is used, but there is no particular restriction on the particle size.
  • the magnesium compound used in the pharmaceutical preparation of the present invention is preferably one or more selected from magnesium stearate, talc, and magnesium aluminate metasilicate.
  • the magnesium compound is added in an amount of 0.05 to 10% by mass, and preferably 0.1 to 5% by mass, in the chewable preparation.
  • Various flavoring / flavoring substances can be added to the medicable chewable of the present invention.
  • various flavor substances and various sweeteners can be used.
  • Flavor substances include, for example, lemon flavor, green range flavor, grapefruit flavor, chocolate flavor, d-menthol, 1-menthol, and the like.
  • sweetener examples include aspartame, saccharin, saccharin sodium, glycyrrhizic acid, monoammonium glycyrrhizinate, diammonium glycyrrhizinate, diammonium glycyrrhizinate, sodium glycyrrhizinate, trisodium glycyrrhizinate, trisodium glycyrrhizinate, acetanilfam K, acesulfame lysium Toles, sorbitol, xylitol, trehalose, etc. are used.
  • the granulation method of the chewable agent of the present invention a commonly used production method such as a wet method and a dry method can be applied.
  • the granulation equipment include a high-speed stirring granulator and a fluidized bed granulator.
  • Granulators, planetary mixers, dry pressing granulators, crushing granulators, extrusion granulators, tumbling granulators, spray drying granulators, coating granulators, etc. are used.
  • Example 1 This was dried with a tray drying machine (DN600, manufactured by Yamato Scientific Co., Ltd.), and further added to a granulator (ND-10, manufactured by Seika Okada Co., Ltd.). It was sized at 00 rpm to produce granules for chewables. The granules were tableted with a breaker (HT-AP 6 SS-II, manufactured by Hattetsu Corporation) at 0.5 tons to produce chewable tablets.
  • a tray drying machine DN600, manufactured by Yamato Scientific Co., Ltd.
  • ND-10 manufactured by Seika Okada Co., Ltd.
  • the granules were tableted with a breaker (HT-AP 6 SS-II, manufactured by Hattetsu Corporation) at 0.5 tons to produce chewable tablets.
  • HT-AP 6 SS-II manufactured by Hattetsu Corporation
  • a stirring mixer (Fukae) was used. It was charged into an industrial company 10 J) and mixed at an agitate rotation speed of 300 rpm and a chopper rotation speed of 360 rpm. Separately, a solution obtained by dissolving 37.5 g of cunic anhydride in about 150.0 g of water was added thereto, and mixed well. This was dried with a fluid bed granulator (FLO-5, manufactured by Freund) and further added to a sizing machine (ND-10, manufactured by Seika Okada).
  • FLO-5 fluid bed granulator
  • ND-10 sizing machine
  • the screen was sized at a screen size of 850 im and a rotation speed of 2000 rpm.
  • To 247.5 g of the granules 39.7 g of talc and 13.2 g of magnesium stearate were added and mixed to produce granules for chewable.
  • the granules were tableted at 0.7 tons with a tableting machine (HT-AP 6 SS-II manufactured by Hata Iron Works) to produce chewable tablets.
  • the granules are dried with a fluidized bed granulator (FLO-5, manufactured by Freund Corporation), and then added to a sizing machine (ND-10, manufactured by Seika Okada), at a screen size of 850 rn and a rotation speed of 2000 rpm. It was sized. To 1243.4 g of the granules, 39.7 g of evening luke and 13.2 g of magnesium stearate were added and mixed to produce granules for chewable. The granules were tableted with a tableting machine (HT-APSS-II, manufactured by Hattetsu Corporation) at 0.7 tons to produce chewable tablets. Test example
  • Each of the chewable tablets obtained in each of the above Examples and Reference Examples was filled in an aluminum laminate, left at 40 ° C. for 1 month and 60 t: for 2 weeks, and then visually observed for color of the chewable tablets.
  • the chewable agent containing a branched-chain amino acid produced according to the present invention does not discolor even during long-term storage, so that it has good storage stability and good disintegration in the mouth, and is useful for pharmaceutical applications. is there.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne un comprimé à mâcher contenant trois acides aminés ramifiés, c'est-à-dire, l'isoleucine, la leucine et la valine, en tant qu'ingrédients actifs, lequel ne se colore pas pendant sa conservation et présente une stabilité de conservation satisfaisante. Le comprimé à mâcher est caractérisé en ce qu'il contient trois acides aminés ramifiés, c'est-à-dire l'isoleucine, la leucine et la valine, en tant qu'ingrédients actifs et contenant un composé magnésium.
PCT/JP2003/000580 2002-01-25 2003-01-23 Comprime a macher contenant des acides amines ramifies WO2003063855A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002016480A JP3341769B1 (ja) 2002-01-25 2002-01-25 分岐鎖アミノ酸含有チュアブル剤
JP2002-16480 2002-01-25

Publications (1)

Publication Number Publication Date
WO2003063855A1 true WO2003063855A1 (fr) 2003-08-07

Family

ID=19192005

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2003/000580 WO2003063855A1 (fr) 2002-01-25 2003-01-23 Comprime a macher contenant des acides amines ramifies

Country Status (2)

Country Link
JP (1) JP3341769B1 (fr)
WO (1) WO2003063855A1 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1541140A1 (fr) * 2002-08-12 2005-06-15 Kyowa Hakko Kogyo Co., Ltd. Produit a macher contenant un acide amine
WO2007043363A1 (fr) 2005-10-12 2007-04-19 Otsuka Pharmaceutical Factory, Inc. Composition à utiliser pour la prévention d'un état hypoglycémique
TWI397418B (zh) 2006-10-10 2013-06-01 Otsuka Pharma Co Ltd 抗憂鬱劑
TN2010000251A1 (fr) * 2010-06-03 2011-11-11 Rekik Raouf N-acetyl-dl-leucine medicament neuro et retino protecteur

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0995457A (ja) * 1995-10-02 1997-04-08 Sunstar Inc 塩化ナトリウムおよび塩化マグネシウム含有口腔用組成物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0995457A (ja) * 1995-10-02 1997-04-08 Sunstar Inc 塩化ナトリウムおよび塩化マグネシウム含有口腔用組成物

Also Published As

Publication number Publication date
JP2003221327A (ja) 2003-08-05
JP3341769B1 (ja) 2002-11-05

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