WO1988003023A1 - Composition de medicament contre les maladies du foie et procede de preparation - Google Patents

Composition de medicament contre les maladies du foie et procede de preparation Download PDF

Info

Publication number
WO1988003023A1
WO1988003023A1 PCT/JP1987/000829 JP8700829W WO8803023A1 WO 1988003023 A1 WO1988003023 A1 WO 1988003023A1 JP 8700829 W JP8700829 W JP 8700829W WO 8803023 A1 WO8803023 A1 WO 8803023A1
Authority
WO
WIPO (PCT)
Prior art keywords
magnesium
parts
weight
salt
group
Prior art date
Application number
PCT/JP1987/000829
Other languages
English (en)
Japanese (ja)
Inventor
Yoshinori Matsuoka
Hisatoshi Emori
Original Assignee
Mitsubishi Chemical Industries Limited
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
Priority claimed from JP25965086A external-priority patent/JPS63115815A/ja
Priority claimed from JP26470086A external-priority patent/JPS63119426A/ja
Application filed by Mitsubishi Chemical Industries Limited filed Critical Mitsubishi Chemical Industries Limited
Publication of WO1988003023A1 publication Critical patent/WO1988003023A1/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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines

Definitions

  • the present invention is useful for enhancing the bioavailability of Tritoqualin (Bioavailatility, the rate for biological IJ).
  • Tritriquat-containing liver disease The present invention relates to a therapeutic composition and a method for producing the same. Background technology
  • Tritoqualine is a compound represented by the following structural formula (I): 7-amino,, triethoxy, J-(",, 7, f TRAHYDRO-METHY-METHYRU /,...? Oh La Lee de (C 26 H 32 N 2 0 8), door re-door mosquito Li emissions (Tritocaline) or Bruno, also referred to as the i port scan data Mi emissions (Hypo stamine). Tritoqualin has been used as an anti-alergic drug in lip citrus but has recently been found to be effective in treating liver disease.
  • this tritoqualine is poorly soluble in water D.
  • bioavailability B io ava i lalJil lty (bioavailability) was low.
  • the gist of the present invention is the Salt, light silicic anhydride, synthetic aluminum silicate, magnesium magnesium silicate, crystalline cellulose, cyclodextrin Or a species selected from the group consisting of linoleic acid and cyclodextrin linkers, or ⁇ the therapeutic composition for a liver disease characterized by comprising two or more species; Exist.
  • Figure / shows the dissolution properties of the composition obtained in Example / and Example ⁇ 2 and the bulk of tritoqualine.
  • tritoqualin or a salt thereof may be converted to triethyl quaternary anhydride, synthetic aluminum silicate, magnesium silicate aluminum magnesium or the like.
  • Crystalline cellulose, cyclodextrin, and methyl dextrin which are mixed with those selected from the group consisting of: May be used singly or in combination with two or more.
  • silica gel anhydride and / or crystalline cellulose are particularly preferred. These amounts are based on tritoline / parts by weight./ ⁇ /parts by weight, preferably ⁇ parts by weight, more preferably ⁇ 3 parts by weight. You.
  • tritoqualin or a salt thereof is dissolved in an organic solvent, and the solution is mixed with the above-mentioned components such as light caustic anhydride.
  • the surface absorption method After removing the solvent after adsorbing it on the surface (hereinafter referred to as the surface absorption method), or using the above components together with Triquarine or its salt, vibrating mill or ball mill A method of mixing and milling for about several minutes to several hours by using is preferably employed.
  • Organic solvents that dissolve tritoqualin or its salts in the surface absorption method include clot mouth holme, dichloromethan, acetate, ether, and meta-solvent. Knol or ethanol may be mentioned, but from the viewpoint of solubility, black mouth home, dichloromethane or acetate is preferred.
  • the salt of tritoqualin may be any substance that does not interfere with its medicinal properties and that forms a salt, such as hydrochloric acid, bromate, citrate, tartrate, and sulfate. Salts, phosphates, sulfonates and the like are used.
  • the tritoquatrine composition obtained according to the present invention can be used as such, or it can be any other pharmacologically acceptable / species or more than one type. Oral mixed with carriers, excipients, binders, lubricants, disintegrants, etc. to form powders (powder), granules, tablets, tablets, suppositories, etc. Alternatively, it can be administered transmucosally.
  • Tritoqualin The dosage of Tritoqualin is usually adult / daily! )
  • Tritoquatrine / ⁇ is dissolved in black mouth por- tion /; ⁇ , and light silica (zero, "Aerosil # 2 R” manufactured by Nihon Aerogel Co., Ltd.) and J "are dissolved.
  • the kneaded product was vacuum-dried at ⁇ ° C for ⁇ f hours to obtain a composition of the present invention.
  • the dissolution properties of the composition of the present invention obtained in Examples 1 and 2 were tested.
  • Is the test solution a Platinum Robinson buffer of pH 4 ⁇ . 0 k / ⁇ was used.
  • the test temperature is j ⁇ ⁇ /. C
  • the paddle rotation speed was / rpin
  • each composition was a powder of f-mesh pass, and was added in an amount equivalent to / 0 as a triquat.
  • each sample was sampled at 10, 20, 30 3 ⁇ 4 and a few minutes, and the high-performance liquid chromatography (HPLC) The phosphorus concentration was measured.
  • HPLC high-performance liquid chromatography
  • One group of beagle dogs male, // to ⁇ J was treated as a group, to which the composition of the present invention obtained in Examples / and -2 was administered, and the blood concentration was measured over time.
  • the dose was Tritoqualin / ri ⁇ for Z beagle dogs, and the dose was administered j minutes after the feed was fed.
  • the present invention can provide a remedy for liver disease with improved solubility of poorly soluble tritoqualin and improved bioavailability.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette composition comprend de la tritoqualine ou son sel et un ou plusieurs membres du groupe comprenant l'acide silicique anhydre léger, le silicate d'aluminium synthétique, le métasilicoaluminate de magnésium, la cellulose cristalline, la cyclodextrine et la cyclodextrine méthylée. Est également décrit un procédé de production de cette composition.
PCT/JP1987/000829 1986-10-31 1987-10-29 Composition de medicament contre les maladies du foie et procede de preparation WO1988003023A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP61/259650 1986-10-31
JP25965086A JPS63115815A (ja) 1986-10-31 1986-10-31 肝疾患治療薬組成物
JP61/264700 1986-11-06
JP26470086A JPS63119426A (ja) 1986-11-06 1986-11-06 肝疾患治療薬組成物

Publications (1)

Publication Number Publication Date
WO1988003023A1 true WO1988003023A1 (fr) 1988-05-05

Family

ID=26544221

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1987/000829 WO1988003023A1 (fr) 1986-10-31 1987-10-29 Composition de medicament contre les maladies du foie et procede de preparation

Country Status (1)

Country Link
WO (1) WO1988003023A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1089232C (zh) * 1995-08-11 2002-08-21 日产化学工业株式会社 将微水溶性药物转化为非晶态的方法
WO2002080904A1 (fr) * 2001-04-05 2002-10-17 Kyowa Hakko Kogyo Co., Ltd. Agent de protection ou d'amelioration de fonction hepatique
US7160555B2 (en) 1999-05-21 2007-01-09 Kissei Pharmaceutical Co., Ltd. Immediate release medicinal compositions for oral use
EP2659890A1 (fr) * 2012-04-30 2013-11-06 Orphan Synergy Europe - Pharma Procédé et compositions de traitement de la fibrose

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5486607A (en) * 1977-12-23 1979-07-10 Yoshinobu Nakai Solid pharmaceutical composition
JPS5835968B2 (ja) * 1974-02-25 1983-08-05 帝人株式会社 サイクロデキストリン包接化合物の製造法
JPS60226811A (ja) * 1984-04-25 1985-11-12 Mitsubishi Chem Ind Ltd 抗動脈硬化剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5835968B2 (ja) * 1974-02-25 1983-08-05 帝人株式会社 サイクロデキストリン包接化合物の製造法
JPS5486607A (en) * 1977-12-23 1979-07-10 Yoshinobu Nakai Solid pharmaceutical composition
JPS60226811A (ja) * 1984-04-25 1985-11-12 Mitsubishi Chem Ind Ltd 抗動脈硬化剤

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1089232C (zh) * 1995-08-11 2002-08-21 日产化学工业株式会社 将微水溶性药物转化为非晶态的方法
US7160555B2 (en) 1999-05-21 2007-01-09 Kissei Pharmaceutical Co., Ltd. Immediate release medicinal compositions for oral use
US7160556B2 (en) 1999-05-21 2007-01-09 Kissei Pharmaceutical Co., Ltd. Immediate release medicinal compositions for oral use
US7166301B1 (en) 1999-05-21 2007-01-23 Kissei Pharmaceutical Co., Ltd. Immediate release medicinal compositions for oral use
CN1352558B (zh) * 1999-05-21 2012-06-13 橘生药品工业株式会社 即释型口服用药物组合物
WO2002080904A1 (fr) * 2001-04-05 2002-10-17 Kyowa Hakko Kogyo Co., Ltd. Agent de protection ou d'amelioration de fonction hepatique
EP2659890A1 (fr) * 2012-04-30 2013-11-06 Orphan Synergy Europe - Pharma Procédé et compositions de traitement de la fibrose
WO2013164204A1 (fr) * 2012-04-30 2013-11-07 Orphan Synergy Europe - Pharma Tritoqualine pour son utilisation dans le traitement de la mucoviscidose
US9301955B2 (en) 2012-04-30 2016-04-05 Orphan Synergy Europe-Pharma Tritoqualine for use in the treatment of cystic fibrosis

Similar Documents

Publication Publication Date Title
CN1102046C (zh) 口服抗菌组合物
JP2009197020A (ja) 薬剤組成物
JP2001511156A (ja) 高いバイオアベイラビリティーを有するフェノフィブレート医薬組成物及びそれを調製するための方法
HU204994B (en) Process for producint new ranitidine derivatives and pharmaceutical compositions comprising same
WO1999034832A1 (fr) Compositions de cephalosporine amorphes, stables du point de vue cristallographique et procede de preparation de ces compositions
JP2003503380A (ja) 無定形硝酸エステルおよびその製剤組成物
WO2006118210A1 (fr) Procede de prevention de la degradation d'un compose dihydropyridine
CN1105240A (zh) 药物组合物
JP2004131393A (ja) 易溶出性製剤
CN1061415A (zh) 含s(+)-苯基链烷酸和氨基糖类的配合物
WO1988003023A1 (fr) Composition de medicament contre les maladies du foie et procede de preparation
TWI224004B (en) Pediatric formulation of gatifloxacin
CN103845332B (zh) 一种达沙替尼药用组合物及其制备方法
JPH0249720A (ja) 難溶性薬剤組成物
JP2000086509A (ja) ソファルコン含有製剤の製造方法
EP2529742B1 (fr) Composition pharmaceutique comportant de la dapagliflozine et cyclodextrine
KR101019769B1 (ko) 경구 흡수성이 개선된 항균성 약제학적 조성물
JPS63119426A (ja) 肝疾患治療薬組成物
JP2007106684A (ja) 抗菌性医薬組成物
JP2003300885A (ja) 抗菌性医薬組成物
JPH02206A (ja) エキシホンと水溶性高分子化合物とを含有することを特徴とする新規製剤
JP3546208B2 (ja) 経口吸収性が改善された抗菌性医薬組成物
JP2005035973A (ja) 安定なアジスロマイシン非二水和物経口懸濁剤
EP2224914B1 (fr) Compositions de diacereine
CN110314240B (zh) 一种缬沙坦环糊精-金属有机骨架组合物及其制备方法

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): US

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): AT BE CH DE FR GB IT LU NL SE