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WO2018127594A1 - Forme posologique pour la voie orale permettant d'améliorer la solubilisation d'un agent actif faiblement soluble, et procédé de préparation - Google Patents

Forme posologique pour la voie orale permettant d'améliorer la solubilisation d'un agent actif faiblement soluble, et procédé de préparation Download PDF

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Publication number
WO2018127594A1
WO2018127594A1 PCT/EP2018/050383 EP2018050383W WO2018127594A1 WO 2018127594 A1 WO2018127594 A1 WO 2018127594A1 EP 2018050383 W EP2018050383 W EP 2018050383W WO 2018127594 A1 WO2018127594 A1 WO 2018127594A1
Authority
WO
WIPO (PCT)
Prior art keywords
magnesium
dosage form
granular phase
oral dosage
granular
Prior art date
Application number
PCT/EP2018/050383
Other languages
English (en)
Inventor
Bart Rossel
Original Assignee
Oystershell Nv
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 EP17150552.2A external-priority patent/EP3345591A1/fr
Application filed by Oystershell Nv filed Critical Oystershell Nv
Priority to US16/476,019 priority Critical patent/US12115175B2/en
Priority to ES18700116T priority patent/ES2870011T3/es
Priority to EP18700116.9A priority patent/EP3565525B1/fr
Priority to BR112019013995-8A priority patent/BR112019013995A2/pt
Publication of WO2018127594A1 publication Critical patent/WO2018127594A1/fr

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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/08—Oxides; Hydroxides
    • 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
    • A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Definitions

  • the present invention provides an oral dosage form comprising a granular phase and a non-granular phase, wherein said granular phase is comprised of a pharmaceutically active agent, a gas forming agent and a hydrophilic polymer.
  • Exemplary disintegrants include, by way of example and without limitation, starches such as corn starch, potato starch, pre-gelatinized and modified starches thereof, sweeteners, clays, bentonite, microcrystalline cellulose (e.g., Avicel), carboxymethylcellulose calcium, croscarmellose sodium, alginic acid, sodium alginate, cellulose polyacrilin potassium (e.g ., Amberlite), alginates, sodium starch glycolate, gums, agar, guar, locust bean, karaya, pectin, tragacanth, crospovidone and other materials known to one of ordinary skill in the art.
  • starches such as corn starch, potato starch, pre-gelatinized and modified starches thereof, sweeteners, clays, bentonite, microcrystalline cellulose (e.g., Avicel), carboxymethylcellulose calcium, croscarmellose sodium, alginic acid, sodium alginate, cellulose polyacrilin potassium (e.g
  • said inorganic salt is selected from the group consisting of magnesium oxide, magnesium carbonate, magnesium hydroxide, magnesium fluoride and magnesium chloride. These salts provide a high fractional content of the elemental additive. Most preferably, said inorganic salt is magnesium oxide.
  • the present invention also includes all of the non-hydrated, hydrated, and polymorphic forms of the above-identified salts. Suppliers often use different processes for making such salts and most notably of magnesium salts. I.e., MgO from one supplier will likely have a different particle size, bulk density and/or porosity than MgO from another suppler.
  • the present invention includes magnesium salts available in any pharmaceutically acceptable particle size range.
  • buffering agent is intended to mean a compound used to resist change in pH upon dilution or addition of acid or alkali.
  • Such compounds include, by way of example and without limitation, acetic acid, sodium acetate, adipic acid, benzoic acid, sodium benzoate, boric acid, sodium borate, citric acid, glycine, maleic acid, monobasic sodium phosphate, dibasic sodium phosphate, HEPES, lactic acid, tartaric acid, potassium metaphosphate, potassium phosphate, monobasic sodium acetate, sodium bicarbonate, tris-sodium tartrate and sodium citrate anhydrous and dihydrate and others known to those of ordinary skill in the art.
  • the formulation of the invention can also include oils, for example, fixed oils, such as peanut oil, sesame oil, cottonseed oil, com oil and olive oil; fatty acids, such as oleic acid, stearic acid and isostearic acid; and fatty acid esters, such as ethyl oleate, isopropyl myristate, fatty acid glycerides and acetylated fatty acid glycerides.
  • fixed oils such as peanut oil, sesame oil, cottonseed oil, com oil and olive oil
  • fatty acids such as oleic acid, stearic acid and isostearic acid
  • fatty acid esters such as ethyl oleate, isopropyl myristate, fatty acid glycerides and acetylated fatty acid glycerides.
  • the present invention provides a method for preparing an oral dosage form, comprising the steps of:
  • the present invention provides an oral dosing form obtained by a method according to the second aspect of the invention.
  • Comparative Example 1 shows a nearly complete dissolution of the elemental magnesium.
  • the powder of Comparative Example 1 consists of an organic magnesium salt, in a non compressed powder formulation which are known to provide faster dissolution rates.
  • Such dosage forms have, however, a relatively low magnesium content and are unwieldy in use in that the user either needs to consume several doses per day in the case of compacted or encapsulated dosage forms or in the case of powder dosage forms, needs to consume these as a water soluble powder in bulk sachets or stick packs.

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une forme posologique pour la voie orale comprenant une phase granulaire et une phase non granulaire, ladite phase granulaire étant constituée d'une quantité thérapeutiquement efficace d'un agent pharmaceutiquement actif, d'un agent capable de former un gaz, et d'un polymère hydrophile. Il a été montré que de telles formes posologiques procurent des vitesses de dissolution rapides à des ingrédients ayant une faible solubilité dans l'eau. De plus, la présente invention concerne un procédé de préparation de ces dernières.
PCT/EP2018/050383 2017-01-06 2018-01-08 Forme posologique pour la voie orale permettant d'améliorer la solubilisation d'un agent actif faiblement soluble, et procédé de préparation WO2018127594A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
US16/476,019 US12115175B2 (en) 2017-01-06 2018-01-08 Oral dosage form for enhanced solubilization of a poorly soluble active agent and method of preparation
ES18700116T ES2870011T3 (es) 2017-01-06 2018-01-08 Formulación oral para mejorar la solubilización de un agente activo poco soluble, y método de preparación
EP18700116.9A EP3565525B1 (fr) 2017-01-06 2018-01-08 Forme posologique pour la voie orale permettant d'améliorer la solubilisation d'un agent actif faiblement soluble, et procédé de préparation
BR112019013995-8A BR112019013995A2 (pt) 2017-01-06 2018-01-08 Forma de dosagem oral para solubilização melhorada de um agente ativo pouco solúvel e método de preparação

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP17150552.2A EP3345591A1 (fr) 2017-01-06 2017-01-06 Forme posologique orale pour améliorer la solubilisation d'un agent actif peu soluble et procédé de préparation
EP17150552.2 2017-01-06
BEBE2017/5106 2017-02-21
BE20175106A BE1024879B9 (nl) 2017-01-06 2017-02-21 Orale doseringsvorm voor verbeterde oplosbaarheid van een zwak oplosbare, werkzame stof en bereidingswijze

Publications (1)

Publication Number Publication Date
WO2018127594A1 true WO2018127594A1 (fr) 2018-07-12

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2018/050383 WO2018127594A1 (fr) 2017-01-06 2018-01-08 Forme posologique pour la voie orale permettant d'améliorer la solubilisation d'un agent actif faiblement soluble, et procédé de préparation

Country Status (1)

Country Link
WO (1) WO2018127594A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102342514B1 (ko) * 2021-01-14 2021-12-23 주식회사유한양행 글리세로인산마그네슘을 포함하는 경구투여용 수성 용액 형태의 약학 조성물

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001015665A1 (fr) 1999-09-02 2001-03-08 Nostrum Pharmaceuticals, Inc. Dosage oral a liberation regulee destine a l'administration orale
WO2004032906A1 (fr) * 2002-10-11 2004-04-22 Depomed Development, Ltd. Forme gastro-retentive pour administrer du levodopa
US20040180088A1 (en) * 2001-07-04 2004-09-16 Dudhara Kamlesh Mohanlal Gastric retention controlled drug delivery system
US20050220865A1 (en) * 2004-04-02 2005-10-06 Koleng John J Compressed composition comprising magnesium salt
WO2009150323A1 (fr) 2008-05-20 2009-12-17 Fabienne Joanny Utilisation d'une matrice pour administration orale de magnesium a liberation prolongee, et composition contenant cette matrice

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001015665A1 (fr) 1999-09-02 2001-03-08 Nostrum Pharmaceuticals, Inc. Dosage oral a liberation regulee destine a l'administration orale
US20040180088A1 (en) * 2001-07-04 2004-09-16 Dudhara Kamlesh Mohanlal Gastric retention controlled drug delivery system
WO2004032906A1 (fr) * 2002-10-11 2004-04-22 Depomed Development, Ltd. Forme gastro-retentive pour administrer du levodopa
US20050220865A1 (en) * 2004-04-02 2005-10-06 Koleng John J Compressed composition comprising magnesium salt
WO2005097078A1 (fr) 2004-04-02 2005-10-20 Blaine Pharmaceuticals Composition comprimee contenant du sel de magnesium
WO2009150323A1 (fr) 2008-05-20 2009-12-17 Fabienne Joanny Utilisation d'une matrice pour administration orale de magnesium a liberation prolongee, et composition contenant cette matrice

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
"Handbook of Pharmaceutical Excipients", 2003, PHARMACEUTICAL PRESS
"Remington's Pharmaceutical Sciences", 1990, MACK PUBLISHING COMPANY, pages: 291 - 294
A.T. FLORENCE; D. ALTWOOD: "Physicochemical Principles of Pharmacy", 1988, MACMILLAN PRESS, pages: 281 - 334
ALFRED MARTIN; JAMES SWARBRICK; ARTHUR COMMARATA: "Physical Pharmacy. Physical Chemical Principles in Pharmaceutical Sciences", 1983, pages: 592 - 638
SINGH B N ET AL: "Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention", JOURNAL OF CONTROLLED RELE, ELSEVIER, AMSTERDAM, NL, vol. 63, no. 3, 3 February 2000 (2000-02-03), pages 235 - 259, XP004244475, ISSN: 0168-3659, DOI: 10.1016/S0168-3659(99)00204-7 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102342514B1 (ko) * 2021-01-14 2021-12-23 주식회사유한양행 글리세로인산마그네슘을 포함하는 경구투여용 수성 용액 형태의 약학 조성물

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