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WO1995001780A1 - Combinaisons alginate-antagoniste de h¿2? - Google Patents

Combinaisons alginate-antagoniste de h¿2? Download PDF

Info

Publication number
WO1995001780A1
WO1995001780A1 PCT/US1994/007521 US9407521W WO9501780A1 WO 1995001780 A1 WO1995001780 A1 WO 1995001780A1 US 9407521 W US9407521 W US 9407521W WO 9501780 A1 WO9501780 A1 WO 9501780A1
Authority
WO
WIPO (PCT)
Prior art keywords
gastrointestinal
disorders
relief
famotidine
alginate
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/US1994/007521
Other languages
English (en)
Inventor
Robert T. Sims
William Slivka
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.)
Kenvue Brands LLC
Merck and Co Inc
Original Assignee
McNeil PPC Inc
Merck and 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 McNeil PPC Inc, Merck and Co Inc filed Critical McNeil PPC Inc
Priority to AU72182/94A priority Critical patent/AU7218294A/en
Publication of WO1995001780A1 publication Critical patent/WO1995001780A1/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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/74—Synthetic polymeric materials
    • A61K31/80—Polymers containing hetero atoms not provided for in groups A61K31/755 - A61K31/795

Definitions

  • H2 antagonists are commonly prescribed to treat and prevent ulcers in the walls of the stomach, duodenum or esophagus. H2 antagonists are also used to treat non-ulcerative conditions. Damage to the mucus lining surrounding these tissues enables destructive action of stomach acids which erodes the underlying tissue. Commonly known H2 antagonists for the treatment of ulcers include cimetidine, ranitidine, nizatidine, roxatidine and famotidine.
  • GER gastroesophageal reflux
  • H2 antagonist selected from famotidine or its salts, hydrates, steroisomers or polymorphs thereof, to treat and prevent the discomfort associated with indigestion, sour stomach, heartburn or other gastrointestinal disorders including GER.
  • Additional antoxidants may be added to the claimed famotidine/alginate combination to prevent oxidation of famotidine to a less active metabolite.
  • the present invention therefore provides an effective dual and synergistic treatment of gastrointestinal disorders such as GER using the combination of famotidine and its salts, hydrates, or pharmacolo ⁇ gically active stereoisomers or polymorphs with an alginate.
  • the claimed combination is particularly useful for treating gastroesophageal reflux disorder at nightime since famotidine or the biologically active forms of famotidine has a long-lasting effect (9 hours) thereby aiding in the prevention of heartburn and other gastrointestinal distress while the alginate aids in eliminating the rafting effect.
  • Other H2 antagonists that may be employed in this invention include cimeditine, ranitidine, nizatidine, and roxatidine.
  • the composition comprises:
  • This invention is also directed to a method of preventing and treating indigestion, sour stomach, heartbum, overindulgence, gastro ⁇ esophageal reflux and other gastrointestinal disorders in mammals, including humans, in need of treatment thereof, comprising administering to such organism:
  • mammals or mammalian organism includes but is not limited to man, dog, cat, horse and cow.
  • Famotidine may be purchased in bulk quantities as it is currently available on the market and formulated via typical formulation processes with alginates selected from alginic acid which is suitable for tablet formulations or sodium alginate which is suitable for liquid formulations of the claimed combination or other pharmaceutically acceptable salts of alginic acid. Famotidine as a prescription drug product is sold under the trademark PEPCID®. Simethicone, an optional anti-flatulent, is also readily available in commercial quantities.
  • compositions of the present invention are useful in the treatment of various mild gastrointestinal disorders including indigestion, sour stomach, overindulgence and heartbum.
  • an alginate combined with an H2 antagonist selected from famotidine, a compound of the formula:
  • the claimed combination is used to treat the symptoms associated with gastric acid secretion while simultaneously treating the symptoms of gastroesophageal reflux.
  • the animal, patient, or organism in need of treatment thereof therefore benefits from the claimed pharmaceutical composition.
  • H2 antagonists are well known in the treatment of ulcers and other gastrointestinal disorders and may be used, according to the present invention, in combination with an alginate and an optional anti-flatulent such as simethicone.
  • H2 antagonists used for ulcer therapy fall into four major structural classes: imidazole derivatives; substituted furans; aminoalkylphenoxy derivatives and guanidinothiazole compounds.
  • Famotidine N'-(ammosulfonyl)-3-[[[2-[(diamino-methylene)amino]-4- thiazolyl]methyl]thio]propanimidamide
  • Famotidine N'-(ammosulfonyl)-3-[[[2-[(diamino-methylene)amino]-4- thiazolyl]methyl]thio]propanimidamide
  • Famotidine N'-(ammosulfonyl)-3-[[[2-[(diamino-methylene)amino]-4- thiazolyl
  • Famotidine suppresses both the acid concentration and the volume of gastric acid secretion. Famotidine is well tolerated and has minimal side effects and thus advantageously may be used in the present invention in combination with an alginate. Famotidine is also the most potent and selective H2 antagonist.
  • the combination of famotidine or its pharmaceutically effective salts, hydrates, stereoisomers or polymorphs with an alginate provides a combination which simultaneously and selectively provides relief from and prevention of discomfort and injury to the stomach, esophagus, or duodenum from excess production of gastric acid.
  • famotidine in combination with an alginate may not interact with alcohol so that it may be administered prior to or during ingestion of meals or beverages which contain alcohol and, therefore, a patient in need of rapid treatment of gastrointestinal distress may take the drug combination at an appropriate time which may be during a meal in which alcohol was consumed.
  • the combination of an alginate with famotidine provides relief of gastroesophageal reflux while also providing long acting relief from and treatment of gastrointestinal disorders associated with gastric acid secretion.
  • a therapeutically active stereoisomer or polymorph of famotidine may be employed substantially free of other stereoisomeric forms or polymorphs. Substantially free should be taken to mean at least 90% of one distinct stereoisomer or polymorph.
  • famotidine which is a highly potent H2 antagonist with an alginate reduces the size and weight of all pharmaceutical delivery forms or combination formulations and therefore improves patient compliance or tolerance.
  • the tablet or capsule form of this combination is more readily swallowable by patients in need of treatment thereof.
  • Famotidine or its pharmaceutically acceptable salts, hydrates, stereoisomers or polymorphs is advantageously used in the present invention in combination with alginic acid or sodium alginate.
  • the amount of famotidine used in the present invention in humans may range from 2.5 mg/day to 80 mg/day.
  • 2.5 to 40 mgs/day is administered in combination with 200-500 mgs/day of an alginate.
  • the amount of simethicone added, if employed, may range in humans from 10-1,000 mgs/day.
  • the quantity of simethicone added varies depending upon the desired anti-flatulent strength. It is sold commercially and utilized in various forms and dosages and combinations. Maximum strength simethicone administered alone may be 125 mgs/tablet and taken 4-5 times daily.
  • ADG may be employed as an anti-flatulent in doses of 290 to 31,000 Galactosidase International Units (GalU), particularly 675 to 2250 GaIU. (WO 90/14101)
  • GalU Galactosidase International Units
  • the quantities of each of the active ingredients may vary depending upon the severity of the condition and the particular biochemistry and need of the patient or other organism in need of treatment thereof.
  • the quantities of the active ingredient may also vary depending upon whether the active ingredients are administered in tablet or liquid form or via some other suitable delivery method.
  • a physician or clinician or veterinarian of ordinary skill in the art may readily determine suitable dosages of any prescription medication containing the claimed invention.
  • the combination claimed in the instant invention is advantageously administered orally.
  • the present composition may be administered in the form of tablets, lozenges, wafers, caplets, gelcaps, capsules, elixirs, effervescent formulations, chewable tablets, syrups or suspensions or via other known and effective delivery methods.
  • the active ingredients may be admixed with a pharmaceutically acceptable diluent such as lactose, sucrose, cellulose, dicalcium phosphate, calcium sulfate, mannitol, and, in a liquid composition, ethyl alcohol.
  • Acceptable emulsifying or suspending agents such as PVP, gelatin, natural sugars, com sweeteners, natural and synthetic gums such as acacia, sodium alginate, guar gum, agar, bentonite, carboxymethylcellulose sodium, polyethylene glycol and waxes, may also be admixed with the active components.
  • lubricants such as magnesium stearic acid talc or magnesium stearate, and disintegrators or superdisintegrators such as starch, sodium starch glycolate or cross-linked PVP may also be included.
  • Electrolytes such as dicalcium phosphate, sodium benzoate, sodium acetate and sodium chloride may also be used.
  • Other inactive ingredients that may be added to the claimed active combination include sodium or potassium bicarbonate, magnesium trisilicate, aluminum trisilicate, aluminum hydroxide gel, lactose, sorbitol, aspartame and sodium saccharide.
  • the active components may also be formulated in sustained release or effervescent formulations.
  • the sustained release formulations also include layered formulations which provide for distinct release ratio and thus may be more effective in allowing for short and long term relief.
  • Simethicone may be added to each of the above formulations or examples to provide anti-flatulent relief.
  • the quantity of simethicone administered to a patient in need of treatment thereof is the typical known dosage range to treat flatulence (20-40 mgs per tablet or 5 ml liquid dosage form).
  • the inactive ingredients in the tablet form may further include dextrates, mannitol, magnesium stearate, Yellow 10, collodial silicon dioxide and Blue 1 or Red 27 while the liquid form(s) may further include inactives such as butylparaben, carboxymethylcellulose sodium, flavors, hydroxypropyl methylcellulose, microcrystalline cellulose, propylparaben, and purified water.

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  • 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)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne les compositions pharmaceutiques utilisables pour le traitement et le soulagement des indigestions, des aigreurs d'estomac, des brûlures d'estomac et autres troubles gastro-intestinaux chez les mammifères, y compris l'homme. Le traitement comprend l'administration de compositions contenant: (i) une quantité efficace pour le soulagement des troubles gastro-intestinaux ou des troubles de l'÷sophage, d'un antagoniste de H2 sélectionné à partir d'un composé de formule (I), et de ses sels, hydrates, stéréoisomères et composés polymorphes pharmaceutiquement acceptables; (ii) une quantité efficace pour le soulagement des troubles gastro-intestinaux ou des troubles de l'÷sophage, d'au moins un alginate; et, éventuellement, (iii) une quantité empêchant les flatulences de diméthicone.
PCT/US1994/007521 1993-07-06 1994-07-05 Combinaisons alginate-antagoniste de h¿2? Ceased WO1995001780A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU72182/94A AU7218294A (en) 1993-07-06 1994-07-05 H2 antagonist-alginate combinations

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8793493A 1993-07-06 1993-07-06
US087,934 1993-07-06

Publications (1)

Publication Number Publication Date
WO1995001780A1 true WO1995001780A1 (fr) 1995-01-19

Family

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Family Applications (1)

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PCT/US1994/007521 Ceased WO1995001780A1 (fr) 1993-07-06 1994-07-05 Combinaisons alginate-antagoniste de h¿2?

Country Status (2)

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AU (1) AU7218294A (fr)
WO (1) WO1995001780A1 (fr)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0707484A4 (fr) * 1993-07-06 1998-07-01 Merck & Co Inc Combinaison antiacide-alginate-antagoniste h 2?
WO2000025754A3 (fr) * 1998-11-04 2000-09-08 Mcneil Ppc Inc Formes posologiques solides a administration par voie orale renfermant de l'acide alginique et de la famotidine
US6183776B1 (en) 1996-01-08 2001-02-06 Astra Aktiebolag Oral pharmaceutical dosage forms comprising a proton pump inhibitor and an antacid agent or alginate
WO2001093863A3 (fr) * 2000-06-06 2002-05-02 Richter Gedeon Vegyeszet Compositions pharmaceutique pour le traitement de la depression ou des symptomes de la depression
WO2002083132A1 (fr) * 2001-04-18 2002-10-24 Orexo Ab Composition inhibant la secretion d'acides gastriques
WO2004009077A1 (fr) * 2002-07-17 2004-01-29 Reliant Pharmaceuticals, Llc Composition pharmaceutique liquide a gout masque, comprenant un complexe d'un antagoniste h2 d'histamine et un alginate
EP1563837A1 (fr) * 2004-02-03 2005-08-17 Ferrer Internacional, S.A. Compositions hypocholesterolemiques comprenant une statine et un médicament antiflatulent
WO2007102726A1 (fr) * 2006-03-09 2007-09-13 World-Trade Import-Export, Wtie, Ag. Combinaison synergique d'inhibiteurs des récepteurs h2, de silicone inerte et d'un complexe d'aluminate d'hydroxymagnésium
RU2351332C2 (ru) * 2006-06-05 2009-04-10 Лабораториос Баго С.А. Порошкообразная антацидная фармацевтическая композиция, содержащий ее фармацевтический препарат и способ ее получения
EP3162371A1 (fr) * 2015-10-27 2017-05-03 Przemyslaw Taciak Une composition comprenant simethicone, des neutralisants de l'acide gastrique et des enzymes gastriques (pancreatine) pour l'utilisation dans le traitement des troubles digestives
WO2018083583A1 (fr) * 2016-11-01 2018-05-11 Johnson & Johnson Consumer Inc. Forme posologique pharmaceutique orale liquide comprenant un antagoniste du récepteur h2 à l'histamine et un antiacide
EP3752202A1 (fr) * 2018-02-13 2020-12-23 Drugs Minerals and Generics Italia S.R.L. In Forma Abbreviata D.M.G. Italia S.R.L. Composition sous forme solide destin& xc9;e & xc0; & xca;tre utilis& xc9;e dans le traitement de sympt& xd4;mes extra-& x152;sophagiens du reflux gastrique

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5204118A (en) * 1989-11-02 1993-04-20 Mcneil-Ppc, Inc. Pharmaceutical compositions and methods for treating the symptoms of overindulgence
US5229137A (en) * 1992-05-06 1993-07-20 Brigham And Women's Hospital, Inc. Methods and pharmaceutical compositions for treating episodic heartburn
US5244670A (en) * 1991-04-04 1993-09-14 The Procter & Gamble Company Ingestible pharmaceutical compositions for treating upper gastrointestinal tract distress
US5260072A (en) * 1990-08-30 1993-11-09 Mcneil-Ppc, Inc. Rotogranulations and taste masking coatings for preparation of chewable pharmaceutical tablets

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5204118A (en) * 1989-11-02 1993-04-20 Mcneil-Ppc, Inc. Pharmaceutical compositions and methods for treating the symptoms of overindulgence
US5260072A (en) * 1990-08-30 1993-11-09 Mcneil-Ppc, Inc. Rotogranulations and taste masking coatings for preparation of chewable pharmaceutical tablets
US5244670A (en) * 1991-04-04 1993-09-14 The Procter & Gamble Company Ingestible pharmaceutical compositions for treating upper gastrointestinal tract distress
US5229137A (en) * 1992-05-06 1993-07-20 Brigham And Women's Hospital, Inc. Methods and pharmaceutical compositions for treating episodic heartburn

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0707484A4 (fr) * 1993-07-06 1998-07-01 Merck & Co Inc Combinaison antiacide-alginate-antagoniste h 2?
EP0813424B2 (fr) † 1996-01-08 2009-08-05 AstraZeneca AB Formes galeniques par voie orale comprenants un inhibiteur de la pompe a protons et un agent antacide ou un alginate
US6183776B1 (en) 1996-01-08 2001-02-06 Astra Aktiebolag Oral pharmaceutical dosage forms comprising a proton pump inhibitor and an antacid agent or alginate
WO2000025754A3 (fr) * 1998-11-04 2000-09-08 Mcneil Ppc Inc Formes posologiques solides a administration par voie orale renfermant de l'acide alginique et de la famotidine
WO2001093863A3 (fr) * 2000-06-06 2002-05-02 Richter Gedeon Vegyeszet Compositions pharmaceutique pour le traitement de la depression ou des symptomes de la depression
US7815940B2 (en) 2001-04-18 2010-10-19 Orexo Ab Gastric acid secretion inhibiting composition
WO2002083132A1 (fr) * 2001-04-18 2002-10-24 Orexo Ab Composition inhibant la secretion d'acides gastriques
US6930119B2 (en) 2002-07-17 2005-08-16 Reliant Pharmaceuticals, Inc. Liquid pharmaceutical composition
WO2004009077A1 (fr) * 2002-07-17 2004-01-29 Reliant Pharmaceuticals, Llc Composition pharmaceutique liquide a gout masque, comprenant un complexe d'un antagoniste h2 d'histamine et un alginate
EP1563837A1 (fr) * 2004-02-03 2005-08-17 Ferrer Internacional, S.A. Compositions hypocholesterolemiques comprenant une statine et un médicament antiflatulent
WO2005074915A1 (fr) * 2004-02-03 2005-08-18 Ferrer Internacional, S.A. Compositions hypocholesterolemiques comprenant une statine et un agent antiflatulent
WO2007102726A1 (fr) * 2006-03-09 2007-09-13 World-Trade Import-Export, Wtie, Ag. Combinaison synergique d'inhibiteurs des récepteurs h2, de silicone inerte et d'un complexe d'aluminate d'hydroxymagnésium
RU2351332C2 (ru) * 2006-06-05 2009-04-10 Лабораториос Баго С.А. Порошкообразная антацидная фармацевтическая композиция, содержащий ее фармацевтический препарат и способ ее получения
EP3162371A1 (fr) * 2015-10-27 2017-05-03 Przemyslaw Taciak Une composition comprenant simethicone, des neutralisants de l'acide gastrique et des enzymes gastriques (pancreatine) pour l'utilisation dans le traitement des troubles digestives
WO2018083583A1 (fr) * 2016-11-01 2018-05-11 Johnson & Johnson Consumer Inc. Forme posologique pharmaceutique orale liquide comprenant un antagoniste du récepteur h2 à l'histamine et un antiacide
EP3752202A1 (fr) * 2018-02-13 2020-12-23 Drugs Minerals and Generics Italia S.R.L. In Forma Abbreviata D.M.G. Italia S.R.L. Composition sous forme solide destin& xc9;e & xc0; & xca;tre utilis& xc9;e dans le traitement de sympt& xd4;mes extra-& x152;sophagiens du reflux gastrique

Also Published As

Publication number Publication date
AU7218294A (en) 1995-02-06

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