WO2012162777A1 - Composition pharmaceutique orale comprenant un inhibiteur de la pompe à protons et un agent prokinétique, à utiliser en cas de troubles liés à l'excès d'acide gastrique - Google Patents

Composition pharmaceutique orale comprenant un inhibiteur de la pompe à protons et un agent prokinétique, à utiliser en cas de troubles liés à l'excès d'acide gastrique Download PDF

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Publication number
WO2012162777A1
WO2012162777A1 PCT/BR2012/000168 BR2012000168W WO2012162777A1 WO 2012162777 A1 WO2012162777 A1 WO 2012162777A1 BR 2012000168 W BR2012000168 W BR 2012000168W WO 2012162777 A1 WO2012162777 A1 WO 2012162777A1
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WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
oral pharmaceutical
composition according
agents
gastric acid
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Application number
PCT/BR2012/000168
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English (en)
Portuguese (pt)
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WO2012162777A9 (fr
Inventor
Maurizio BILLI
Original Assignee
Eurofarma Laboratórios S.A
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Publication date
Application filed by Eurofarma Laboratórios S.A filed Critical Eurofarma Laboratórios S.A
Publication of WO2012162777A1 publication Critical patent/WO2012162777A1/fr
Publication of WO2012162777A9 publication Critical patent/WO2012162777A9/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—Poly(meth)acrylates
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Definitions

  • An oral pharmaceutical composition comprising a proton pump inhibitor and a prokinetic agent for use in gastric acid excess disorders.
  • the present invention relates to an oral pharmaceutical composition containing at least one gastric acid suppressing agent, particularly a proton pump inhibitor (PPI), and a prokinetic agent (PA), intended for use in excess acid related disorders.
  • gastric disease for example, gastroesophageal reflux disease.
  • Gastric acid-related disorders including gastroesophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer, have pathogenesis related to gastric motility and excessive emission of gastric acid.
  • Such disorders are typically treated with gastric acid inhibitors such as ranitidine and omeprazole, which are acid suppressing agents.
  • Prokinetic agents including bromopride, cisapride, alizapride, clebopride, domperidone, and metoclopramide have been known to increase gastrointestinal motility, preventing duodenogastric reflux, which is known to treat gastroesophageal reflux disease.
  • Proton pump inhibitors including omeprazole, lansoprazole and pantoprazole, have rapidly replaced H2 receptor antagonists in the treatment of esophageal reflux because they are highly effective, with better resolution of symptoms.
  • Combination therapy of a prokinetic agent and a gastric acid lowering agent has already been shown to be more effective than proton pump inhibitor monotherapy.
  • Administration of cisapride and ranitidine has been shown to decrease esophageal exposure to acidity (Inauen W. et al., Gut. 1993; 34: 1025-1031).
  • Such therapy has also been shown to improve the speed of healing (de Boer WA et al., Alimeht Pharmacol. Ther. 1994; 8: 147-157).
  • PI 9607344-6 discloses a fixed unit dosage form, tablet or capsule, in pellet form enteric coating.
  • PI 0401556-8 relates to a combination of PPI and prokinetic agent, particularly lanzoprazole + bromopride.
  • PI 0506704-9 mentions a delayed release composition, bimodal prokinetic release agent.
  • the present invention relates to a pharmaceutical composition containing one or more gastric acid suppressing agents, particularly a proton pump inhibitor, one or more prokinetic agents, and pharmaceutically acceptable excipients.
  • gastric acid suppressing agents particularly a proton pump inhibitor
  • prokinetic agents particularly a proton pump inhibitor
  • pharmaceutically acceptable excipients such as heartburn, gastroesophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer, and the like.
  • composition refers to either mixing all components together in a unit dosage form or to two or more individual and autonomous component formulations within a unit dosage form, e.g. a gelatin capsule, hydroxypropyl methyl cellulose (HPMC) capsule and the like.
  • a gelatin capsule e.g. a gelatin capsule, hydroxypropyl methyl cellulose (HPMC) capsule and the like.
  • HPMC hydroxypropyl methyl cellulose
  • one capsule contains a PPI and excipients
  • another capsule contains a PA and excipients
  • such two capsules in turn are contained in a single capsule
  • a capsule contains a PPI and excipients
  • a tablet contains a PA and excipients
  • said capsule and said tablet are both contained in a single capsule.
  • the capsule may contain a PA and the tablet may contain a PPI;
  • one tablet contains a PPI and excipients
  • another tablet contains a PA and excipients, and such two tablets are contained in a single capsule; .
  • a two layer tablet one layer containing a PPI and another layer containing a PA.
  • the invention relates to an oral composition, characterized in that it comprises in a single unit dosage form, particularly in a capsule, tablets distinct from (a) one or more slurry pump inhibitors. protons chosen from omeprazole, esomeprazole, pantoprazole, lansoprazole and rabeprazole, with their respective excipients and (b) one or more prokinetic agents chosen from bromopride, cisapride, alizapride, clebopride, domperidone, and metoclopramide, with their excipients.
  • protons chosen from omeprazole, esomeprazole, pantoprazole, lansoprazole and rabeprazole, with their respective excipients
  • prokinetic agents chosen from bromopride, cisapride, alizapride, clebopride, domperidone, and metoclopramide, with their excipients.
  • Such a particular configuration provides:
  • proton pump inhibitors are known to be unstable in acidic medium and therefore subject to degradation and may be protected by specific coating;
  • each tablet may have specific, same or distinct characteristics as:
  • release rate (immediate, slow, delayed, controlled, and the like);
  • Proton pump inhibitors present in the dosage forms of the invention may be used in neutral or alkaline salt form, for example as magnesium, calcium, sodium, potassium or lithium salts. Where applicable, proton pump inhibitors may be used in racemic form as pure enantiomer or alkaline salts of enantiomers.
  • the preferred proton pump inhibitor is chosen from pantoprazole, its salts, esters, hydrates, derivatives, prodrugs or metabolites in any polymorphic form. More particularly, pantoprazole sodium is used sesquihydrate.
  • the preferred prokinetic agent is chosen from domperidone, its salts, esters, hydrates, derivatives, prodrugs or metabolites in any polymorphic form.
  • composition of the invention in its broad sense, and particularly in the realization of two separate tablets contained in a gelatin capsule, hydroxypropyl methylcellulose (HPMC) capsules and the like, contains pharmaceutically acceptable excipients such as diluents, binders, disintegrants, colorants, nonstick, lubricants, plasticizers, sequestrants, coating agents, antioxidants, opacifiers, flavorings, sweeteners, and the like, used alone or in combination with each other.
  • pharmaceutically acceptable excipients for man is in the book "Remington's Pharmaceutical Sciences” 18th Edition, (1990), Mack Publishing Co., USA.
  • diluents suitable for the invention are chosen from microcrystalline cellulose, lactose monohydrate or anhydrous, dibasic calcium phosphate, saccharides such as mannitol, sorbitol, sucrose and glucose,
  • alkalinizing agents suitable for the invention are selected from magnesium oxide, sodium hydroxide, sodium bicarbonate, sodium carbonate and mixtures thereof.
  • Suitable binding agents for without excluding any others, are chosen from povidone, crospovidone and hydroxypropylcellulose.
  • disintegrants suitable for the invention are selected from cross-linked polyvinylpyrrolidone, starch (corn, potato, and the like), modified starches, croscarmellose, croscarmellose sodium, sodium starch glycolate, hydroxypropyl methylcellulose, hydroxypropylcellulose low substitution, and mixtures thereof.
  • lubricants suitable for the invention are colloidal silicon dioxide, talc, stearic acid, magnesium stearate, calcium stearate, zinc stearate, sodium stearyl fumarate, and mixtures thereof.
  • Examples suitable for the invention of coating materials and their supplements for tablets, without excluding any others, are hydroxypropyl methylcellulose, Eudragit (manufactured by Evonik), Opadry (manufactured by Colorcon), triethylcitrate, propylene glycol and the like.
  • the amounts of the actives in the compositions of the invention in their free form are:
  • domperidone 10mg.
  • the invention relates to the use of the composition described above in the manufacture of a medicament used in the treatment of disorders caused by gastric acid, particularly heartburn, reflux disease. gastroesophageal, reflux esophagitis, peptic ulcer, gastric ulcer.

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

Abstract

La présente invention concerne une composition pharmaceutique orale contenant au moins un agent de suppression d'acide gastrique, et notamment un inhibiteur de la pompe à protons (IPP), ainsi qu'un agent prokinétique (PA), à utiliser en cas de troubles liés à l'excès d'acide gastrique, tels que, par exemple, le reflux gastro-oesophagien pathologique.
PCT/BR2012/000168 2011-06-03 2012-05-29 Composition pharmaceutique orale comprenant un inhibiteur de la pompe à protons et un agent prokinétique, à utiliser en cas de troubles liés à l'excès d'acide gastrique WO2012162777A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
BRPI1103093-3A BRPI1103093A2 (pt) 2011-06-03 2011-06-03 composiÇço farmacÊutica oral e uso da composiÇço farmacÊutica oral
BRPI1103093-3 2011-06-03

Publications (2)

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WO2012162777A1 true WO2012162777A1 (fr) 2012-12-06
WO2012162777A9 WO2012162777A9 (fr) 2013-07-25

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Country Status (2)

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BR (1) BRPI1103093A2 (fr)
WO (1) WO2012162777A1 (fr)

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997025065A1 (fr) * 1996-01-08 1997-07-17 Astra Aktiebolag Formes galeniques par voie orale comprenant un inhibiteur de la pompe a protons et un agent pro-cinetique
WO2001051039A1 (fr) * 2000-01-13 2001-07-19 Osmotica Corp. Dispositif osmotique contenant du ranitidine et un agent procinetique
WO2004071374A2 (fr) * 2003-02-11 2004-08-26 Torrent Pharmaceuticals Limited Compositions pharmaceutiques d'administration orale une fois par jour
BRPI0401553A (pt) * 2004-03-02 2004-11-23 Marchesan Implement & Maquin Acionamento de um dosador de adubo por motor elétrico controlado eletronicamente
WO2005065664A1 (fr) * 2004-01-06 2005-07-21 Panacea Biotec Ltd. Compositions pharmaceutiques comprenant un inhibiteur de pompe a protons et un agent pro-cinetique
WO2005117870A2 (fr) * 2004-04-16 2005-12-15 Santarus, Inc. Combinaison d'un inhibiteur de la pompe a protons, d'un agent tampon et d'un agent prokinetique
CN101305995A (zh) * 2007-05-17 2008-11-19 北京利乐生制药科技有限公司 一种含有多潘立酮泮托拉唑钠的缓释制剂及其制备方法
CN102125689A (zh) * 2010-01-12 2011-07-20 上海中邦斯瑞生物药业技术有限公司 质子泵抑制剂和多潘立酮的复方制剂

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997025065A1 (fr) * 1996-01-08 1997-07-17 Astra Aktiebolag Formes galeniques par voie orale comprenant un inhibiteur de la pompe a protons et un agent pro-cinetique
WO2001051039A1 (fr) * 2000-01-13 2001-07-19 Osmotica Corp. Dispositif osmotique contenant du ranitidine et un agent procinetique
WO2004071374A2 (fr) * 2003-02-11 2004-08-26 Torrent Pharmaceuticals Limited Compositions pharmaceutiques d'administration orale une fois par jour
WO2005065664A1 (fr) * 2004-01-06 2005-07-21 Panacea Biotec Ltd. Compositions pharmaceutiques comprenant un inhibiteur de pompe a protons et un agent pro-cinetique
BRPI0401553A (pt) * 2004-03-02 2004-11-23 Marchesan Implement & Maquin Acionamento de um dosador de adubo por motor elétrico controlado eletronicamente
WO2005117870A2 (fr) * 2004-04-16 2005-12-15 Santarus, Inc. Combinaison d'un inhibiteur de la pompe a protons, d'un agent tampon et d'un agent prokinetique
CN101305995A (zh) * 2007-05-17 2008-11-19 北京利乐生制药科技有限公司 一种含有多潘立酮泮托拉唑钠的缓释制剂及其制备方法
CN102125689A (zh) * 2010-01-12 2011-07-20 上海中邦斯瑞生物药业技术有限公司 质子泵抑制剂和多潘立酮的复方制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
AGARWAL, S. ET AL.: "Bioequivalence study of a sustained release fixed dose combination capsule containing esomeprazole and domperidone in healthy subjects.", ARZNEIMITTELFORSCHUNG., vol. 57, no. 05, 2007, pages 274 - 277 *

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WO2012162777A9 (fr) 2013-07-25
BRPI1103093A2 (pt) 2013-07-02

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