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WO1993000097A1 - Compositions pharmaceutiques contenant de la torasemide - Google Patents

Compositions pharmaceutiques contenant de la torasemide Download PDF

Info

Publication number
WO1993000097A1
WO1993000097A1 PCT/EP1992/001437 EP9201437W WO9300097A1 WO 1993000097 A1 WO1993000097 A1 WO 1993000097A1 EP 9201437 W EP9201437 W EP 9201437W WO 9300097 A1 WO9300097 A1 WO 9300097A1
Authority
WO
WIPO (PCT)
Prior art keywords
parts
weight
torasemide
pharmaceutical composition
cellulose
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP1992/001437
Other languages
German (de)
English (en)
Inventor
Masahiro Kikuchi
Hiroko Shu
Nobuo Kondo
Kouichi Yamanouchi
Kazumasa Yokoyama
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Roche Diagnostics GmbH
Original Assignee
Boehringer Mannheim GmbH
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 Boehringer Mannheim GmbH filed Critical Boehringer Mannheim GmbH
Priority to EP92913781A priority Critical patent/EP0591363A1/fr
Publication of WO1993000097A1 publication Critical patent/WO1993000097A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Definitions

  • the invention relates to torasemide-containing pharmaceutical compositions which, for. B. are effective as prophylactic or therapeutic agents against hypertension and edema, or as diuretics.
  • Torasemide [chemical name: l-isopropyl-3- (4-m-toluidino-3-pyridyl) sulfonyl) urea] is e.g. B. effective as a diuretic in the context of hypertension therapy.
  • Orally administered preparations containing torasemide are produced by a generally customary process by adding, for example, sugar, starch, starch derivatives, cellulose, cellulose derivatives, mold release agents, non-stick agents or other customary auxiliaries; they are applied, for example, as tablets to which lactose, corn starch, silicon oxide or magnesium stearate is added (EP-A-0,212,537).
  • compositions are desired in which the storage stability of the torase itself is improved, especially when stored over a longer period of time, changes in the appearance of the preparation caused by moisture absorption are avoided, and the absorption of the torasemide is avoided is further improved by the digestive tract and which have good bioavailability. It has been found that changes in the formulations which have occurred can be caused by corn starch present in the formulation. Accordingly, this invention aims to solve such problems as are encountered in the conventional art and to make better torasemide-containing preparations available for oral administration. To solve the problems described above, numerous commonly used components, such as. B. binders and disintegrants, tests carried out.
  • torasemide-containing compositions which contain hydroxypropyl cellulose or polyvinylpyrrolidone (PVP) as binders, sodium croscarmellose or crospovidone as disintegrants and customary shaping agents, such as, for. B. lactose and / or crystalline cellulose and lubricants such as. B. magnesium stearate, have excellent properties as preparations for oral administration.
  • PVP polyvinylpyrrolidone
  • customary shaping agents such as, for. B. lactose and / or crystalline cellulose and lubricants such as. B. magnesium stearate
  • the active ingredient, the binder and the disintegrant are to be used in certain ratios to one another.
  • the invention therefore relates to pharmaceutical compositions containing torasemide or a compatible salt thereof, a binder selected from the products hydroxypropyl cellulose and polyvinylpyrrolidone (PVP), a disintegrant selected from the products sodium croscarmellose, crospovidone, calcium carboxymethyl cellulose, contain low-substituted hydroxypropyl cellulose, modified starch and sodium carboxymethyl starch and conventional shaping agents and lubricants.
  • PVP polyvinylpyrrolidone
  • a disintegrant selected from the products sodium croscarmellose, crospovidone, calcium carboxymethyl cellulose
  • torasemide preferably the active ingredient in modification 1
  • the torasemide salts are not subject to any particular restriction if they are pharmacologically acceptable substances; as examples, salts with organic acids, such as. B. acetic acid, suberic acid, maleic acid, fumaric acid, malic acid, tartaric acid or methanesulfonic acid, and salts with inorganic acids, such as. As hydrochloric acid, hydrobromic acid, phosphoric acid or sulfuric acid.
  • hydroxypropyl cellulose is preferred as the binder; in particular, it was found that especially those with a high degree of substitution are suitable.
  • the degree of substitution of such a highly substituted hydroxypropyl cellulose is normally 50-80%, preferably 60-70%, expressed as a content (%) of hydroxypropoxyl groups.
  • Commercial hydroxypropyl cellulose is used specifically.
  • Polyvinylpyrrolidone is also preferred.
  • Sodium croscarmellose, crospovidone, calcium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, modified starch or sodium carboxymethyl starch are preferably used as disintegrants.
  • sodium croscarmellose or crospovidones are preferred.
  • Sodium croscarmellose is usually understood to mean sodium carboxy ethyl cellulose, crosslinked, crosprovidone polyvinylpyrrolidone, crosslinked.
  • a modified starch is preferably a starch converted to the position.
  • Shaping agents or lubricants will also be added to the pharmaceutical composition according to this invention; as shaping agents are preferred z.
  • the mixing ratio of the individual components in the pharmaceutical composition of this invention is normally 0.1-50 parts (here and hereinafter: parts by weight), preferably 0.5-15 parts, more preferably 1-10 parts of torasemide; 1-10 parts, preferably 2-5 parts binder; 1-20 parts, preferably 3-15 parts, more preferably 5-10 parts of disintegrant.
  • the proportions of the other components that are mixed into the pharmaceutical composition of this invention are 10-150 parts, preferably 70-140 parts, more preferably 100-130 parts of shaping agents, and 0.1-5 parts, preferably 0.2-2 Parts, more preferably 0.5-1.5 parts of lubricant.
  • the pharmaceutical composition of this invention is e.g. B. as a prophylactic or therapeutic against hypertension and edema, or ideally administered orally as a diuretic.
  • the pharmaceutical composition of this invention is processed into a powder, granule, tablet or pellet by conventional methods.
  • the application of the pharmaceutical composition according to the invention varies depending on the sex, body weight, age, disease state, etc. of the patient; Usually, a daily dose of approximately 1 to 200 mg of torasemide is administered to an adult, preferably 1 to 30 mg, divided into one to several times a day.
  • 40 g torasemide were mixed with 1,064 g lactose, 32 g hydroxypropyl cellulose (content of hydroxypropoxyl groups 62%) and 24 g sodium croscarmellose, pelleted with water, dried and then sieved. 12.9 g of sodium croscarmellose and 3.2 g of magnesium stearate were mixed with 466 g of this substance and the whole was then processed into tablets by a customary process. About 2,300 tablets containing 4 mg of torasemide per tablet were produced in this way.
  • the numbers indicate the weight (mg) of the ingredients in the tablet.

Landscapes

  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Une composition pharmaceutique stable au stockage contient de la torasémide en tant que substance active, un liant et un agent désintégrant, ainsi que des agents de moulage et de lubrification usuels.
PCT/EP1992/001437 1991-06-25 1992-06-25 Compositions pharmaceutiques contenant de la torasemide Ceased WO1993000097A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP92913781A EP0591363A1 (fr) 1991-06-25 1992-06-25 Compositions pharmaceutiques contenant de la torasemide

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP181820/91 1991-06-25
JP18182091A JP3586471B2 (ja) 1991-06-25 1991-06-25 トラセミド含有医薬組成物

Publications (1)

Publication Number Publication Date
WO1993000097A1 true WO1993000097A1 (fr) 1993-01-07

Family

ID=16107395

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1992/001437 Ceased WO1993000097A1 (fr) 1991-06-25 1992-06-25 Compositions pharmaceutiques contenant de la torasemide

Country Status (3)

Country Link
EP (1) EP0591363A1 (fr)
JP (1) JP3586471B2 (fr)
WO (1) WO1993000097A1 (fr)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1280534B1 (fr) * 2000-03-17 2008-07-16 Abbott Laboratories Preparations pharmaceutiques stables au stockage contenant du torasemide
US8071128B2 (en) 1996-06-14 2011-12-06 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US8367111B2 (en) 2002-12-31 2013-02-05 Aptalis Pharmatech, Inc. Extended release dosage forms of propranolol hydrochloride
US8580313B2 (en) 2009-12-02 2013-11-12 Aptalis Pharma Limited Fexofenadine microcapsules and compositions containing them
US8747895B2 (en) 2004-09-13 2014-06-10 Aptalis Pharmatech, Inc. Orally disintegrating tablets of atomoxetine
US9040086B2 (en) 2001-10-04 2015-05-26 Aptalis Pharmatech, Inc. Timed, sustained release systems for propranolol
US9161919B2 (en) 2005-05-02 2015-10-20 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9884014B2 (en) 2004-10-12 2018-02-06 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10471017B2 (en) 2004-10-21 2019-11-12 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions with gastrosoluble pore-formers

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2364145T3 (es) * 1996-11-15 2011-08-25 Ajinomoto Co., Inc. Composición de nateglinida en comprimidos.
CN1259909C (zh) * 2002-01-16 2006-06-21 兴和株式会社 含有2,2－二氯－12－(4－氯苯基)－十二烷酸的药物组合物
US7109242B2 (en) 2003-05-23 2006-09-19 Kowa Company, Ltd. Carboxylic compound and medicine comprising the same
ES2244324B1 (es) * 2004-03-25 2006-11-16 Ferrer Internacional, S.A. Composiciones diureticas de liberacion prolongada.
JP5617382B2 (ja) 2010-06-28 2014-11-05 トヨタ紡織株式会社 インテークマニホールド

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0212537A1 (fr) * 1985-08-17 1987-03-04 Roche Diagnostics GmbH Procédé pour la préparation d'une modification stable de torasémide ainsi que médicaments le contenant

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0212537A1 (fr) * 1985-08-17 1987-03-04 Roche Diagnostics GmbH Procédé pour la préparation d'une modification stable de torasémide ainsi que médicaments le contenant

Cited By (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8071128B2 (en) 1996-06-14 2011-12-06 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US8945618B2 (en) 1996-06-14 2015-02-03 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US8956650B2 (en) 1996-06-14 2015-02-17 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
EP1280534B1 (fr) * 2000-03-17 2008-07-16 Abbott Laboratories Preparations pharmaceutiques stables au stockage contenant du torasemide
US9040086B2 (en) 2001-10-04 2015-05-26 Aptalis Pharmatech, Inc. Timed, sustained release systems for propranolol
US9358214B2 (en) 2001-10-04 2016-06-07 Adare Pharmaceuticals, Inc. Timed, sustained release systems for propranolol
US8367111B2 (en) 2002-12-31 2013-02-05 Aptalis Pharmatech, Inc. Extended release dosage forms of propranolol hydrochloride
US8747895B2 (en) 2004-09-13 2014-06-10 Aptalis Pharmatech, Inc. Orally disintegrating tablets of atomoxetine
US9884014B2 (en) 2004-10-12 2018-02-06 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US11452689B2 (en) 2004-10-12 2022-09-27 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10568832B2 (en) 2004-10-12 2020-02-25 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10130580B2 (en) 2004-10-12 2018-11-20 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10471017B2 (en) 2004-10-21 2019-11-12 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
US10952971B2 (en) 2004-10-21 2021-03-23 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
US9579293B2 (en) 2005-05-02 2017-02-28 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9566249B2 (en) 2005-05-02 2017-02-14 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US10045946B2 (en) 2005-05-02 2018-08-14 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9161918B2 (en) 2005-05-02 2015-10-20 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US10500161B2 (en) 2005-05-02 2019-12-10 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9161919B2 (en) 2005-05-02 2015-10-20 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US11147772B2 (en) 2005-05-02 2021-10-19 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9233105B2 (en) 2009-12-02 2016-01-12 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
US10166220B2 (en) 2009-12-02 2019-01-01 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
US10729682B2 (en) 2009-12-02 2020-08-04 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
US8580313B2 (en) 2009-12-02 2013-11-12 Aptalis Pharma Limited Fexofenadine microcapsules and compositions containing them

Also Published As

Publication number Publication date
JPH05952A (ja) 1993-01-08
JP3586471B2 (ja) 2004-11-10
EP0591363A1 (fr) 1994-04-13

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