WO2016091805A3 - Naloxone monopreparation and multi-layer tablet - Google Patents

Naloxone monopreparation and multi-layer tablet Download PDF

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Publication number
WO2016091805A3
WO2016091805A3 PCT/EP2015/078827 EP2015078827W WO2016091805A3 WO 2016091805 A3 WO2016091805 A3 WO 2016091805A3 EP 2015078827 W EP2015078827 W EP 2015078827W WO 2016091805 A3 WO2016091805 A3 WO 2016091805A3
Authority
WO
WIPO (PCT)
Prior art keywords
composition
naloxone
active ingredient
max
layer tablet
Prior art date
Application number
PCT/EP2015/078827
Other languages
German (de)
French (fr)
Other versions
WO2016091805A2 (en
Inventor
Hélène Rey
Olaf MUNDSZINGER
Isabelle GOLFIER
Silvia JAKOB
Oliver RUSCH
Original Assignee
Develco Pharma Schweiz Ag
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 Develco Pharma Schweiz Ag filed Critical Develco Pharma Schweiz Ag
Priority to EP15817094.4A priority Critical patent/EP3229785A2/en
Priority to CN201580074337.XA priority patent/CN107205943A/en
Publication of WO2016091805A2 publication Critical patent/WO2016091805A2/en
Publication of WO2016091805A3 publication Critical patent/WO2016091805A3/en

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
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • 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
    • 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
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • 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
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids

Abstract

The present invention relates to a solid, oral pharmaceutical composition comprising naloxone, or a pharmaceutically acceptable salt thereof as the active ingredient, the composition having a delayed release of said active ingredient. The composition can comprise a matrix containing glycerol di-behenic acid esters as matrix formers, with a mass ratio of naloxone to matrix former(s) of between 1:1 and 1:10, whereby the active ingredient naloxone has a delayed release. According to the invention, in order to provide a composition suitable for a dosage covering at least twelve hours for treating opioid-induced obstipation, the composition has an in-vitro release rate of the active ingredient, measured using a vane stirrer method according to Eur. Ph. at 75 U/min in 500 ml of 0.1 N hydrochloric acid at 37 °C, of 0 % to 75 % in 2 h, 3 % to 95 % in 4 h, 20 % to 100 % in 10 h, 30 % to 100 % in 16 h, 50 % to 100 % in 24 h and more than 80 % in 36 h, said composition having an IC50/Cmax value of at least 40. Preferably, the composition comprises a value for tmax (naloxone) / tmax (naloxone-3-glucuronoid) of at least 5. In an alternative embodiment, the composition can take the form of a multi-layer tablet.
PCT/EP2015/078827 2014-12-08 2015-12-07 Naloxone monopreparation and multi-layer tablet WO2016091805A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP15817094.4A EP3229785A2 (en) 2014-12-08 2015-12-07 Naloxone monopreparation and multi-layer tablet
CN201580074337.XA CN107205943A (en) 2014-12-08 2015-12-07 Naloxone single dose and multilayer tablet

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14196775 2014-12-08
EP14196775.2 2014-12-08

Publications (2)

Publication Number Publication Date
WO2016091805A2 WO2016091805A2 (en) 2016-06-16
WO2016091805A3 true WO2016091805A3 (en) 2016-12-15

Family

ID=52015950

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2015/078827 WO2016091805A2 (en) 2014-12-08 2015-12-07 Naloxone monopreparation and multi-layer tablet

Country Status (3)

Country Link
EP (1) EP3229785A2 (en)
CN (1) CN107205943A (en)
WO (1) WO2016091805A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115252583B (en) * 2022-07-11 2023-08-08 河北奥星集团药业有限公司 Compound telithromycin hydrochloride slow-release preparation and preparation method thereof
CN115120568B (en) * 2022-07-11 2023-08-22 河北奥星集团药业有限公司 Compound telithromycin hydrochloride sustained-release tablet and preparation method thereof

Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0960619A1 (en) * 1998-05-28 1999-12-01 Krewel Meuselbach GmbH Sustained release analgesic compositions comprising tilidine
WO2001032180A2 (en) * 1999-11-01 2001-05-10 Rodeva Limited Composition for treatment of constipation and irritable bowel syndrome
WO2001058447A1 (en) * 2000-02-08 2001-08-16 Euro-Celtique, S.A. Controlled-release compositions containing opioid agonist and antagonist
WO2002092059A1 (en) * 2001-05-11 2002-11-21 Endo Pharmaceuticals, Inc. Abuse-resistant opioid dosage form
EP1492506A2 (en) * 2002-04-05 2005-01-05 Euro-Celtique S.A. Matrix for sustained, invariant and independent release of active compounds
US20070281017A1 (en) * 2006-06-06 2007-12-06 Endo Pharmaceuticals Inc., A Delaware Corporation Sustained release oxycodone composition with acrylic polymer and metal hydroxide
WO2008027442A2 (en) * 2006-08-30 2008-03-06 Theraquest Biosciences, Llc Abuse deterrent oral pharmaceutical formulations of opioid agonists and method of use
EP2042176A1 (en) * 2007-09-26 2009-04-01 Euro-Celtique S.A. Use of a combination of an opioid agonist and an opioid antagonist for the treatment of Crohn's disease
WO2010003963A1 (en) * 2008-07-07 2010-01-14 Euro-Celtique S.A. Use of opioid antagonists for treating urinary retention
WO2010105672A1 (en) * 2009-03-18 2010-09-23 Evonik Röhm Gmbh Controlled release pharmaceutical composition with resistance against the influence of ethanol employing a coating comprising neutral vinyl polymers and excipients
WO2010121600A2 (en) * 2009-04-22 2010-10-28 Lars Holger Hermann Particulate pharmaceutical composition having an opioid and an opioid antagonist
WO2011117306A1 (en) * 2010-03-24 2011-09-29 L. Molteni & C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Double-layer pharmaceutical formulations containing opioid agonists and antagonists
WO2011141489A1 (en) * 2010-05-10 2011-11-17 Euro-Celtique S.A. Manufacturing of active-free granules and tablets comprising the same
WO2011141488A2 (en) * 2010-05-10 2011-11-17 Euro-Celtique S.A. Pharmaceutical compositions comprising hydromorphone and naloxone
WO2013050539A2 (en) * 2011-10-06 2013-04-11 Grünenthal GmbH Tamper-resistant oral pharmaceutical dosage form comprising opioid agonist and opioid antagonist
US20130129826A1 (en) * 2011-11-17 2013-05-23 Gruenenthal Gmbh Tamper-resistant oral pharmaceutical dosage form comprising opioid antagonist and/or aversive agent, polyalkylene oxide and anionic polymer
WO2013084059A1 (en) * 2011-12-09 2013-06-13 Purdue Pharma L.P. Pharmaceutical dosage forms comprising poly (epsilon- caprolactone) and polyethylene oxide
US20130245054A1 (en) * 2010-08-13 2013-09-19 Derek Allan Prater Use of binders for manufacturing storage stable formulations
US20140322321A1 (en) * 2011-12-06 2014-10-30 Ethypharm Tablet capable of combatting misuse by injection
WO2015086528A1 (en) * 2013-12-11 2015-06-18 Develco Pharma Schweiz Ag Naloxone mono-product and multi-layer tablet

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1416842E (en) * 2001-07-18 2009-03-31 Euro Celtique Sa Pharmaceutical combinations of oxycodone and naloxone
UA91376C2 (en) * 2005-08-24 2010-07-26 Рубикон Рисеч Пвт Лтд. Controlled release formulation

Patent Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0960619A1 (en) * 1998-05-28 1999-12-01 Krewel Meuselbach GmbH Sustained release analgesic compositions comprising tilidine
WO2001032180A2 (en) * 1999-11-01 2001-05-10 Rodeva Limited Composition for treatment of constipation and irritable bowel syndrome
WO2001058447A1 (en) * 2000-02-08 2001-08-16 Euro-Celtique, S.A. Controlled-release compositions containing opioid agonist and antagonist
WO2002092059A1 (en) * 2001-05-11 2002-11-21 Endo Pharmaceuticals, Inc. Abuse-resistant opioid dosage form
EP1492506A2 (en) * 2002-04-05 2005-01-05 Euro-Celtique S.A. Matrix for sustained, invariant and independent release of active compounds
US20070281017A1 (en) * 2006-06-06 2007-12-06 Endo Pharmaceuticals Inc., A Delaware Corporation Sustained release oxycodone composition with acrylic polymer and metal hydroxide
WO2008027442A2 (en) * 2006-08-30 2008-03-06 Theraquest Biosciences, Llc Abuse deterrent oral pharmaceutical formulations of opioid agonists and method of use
EP2042176A1 (en) * 2007-09-26 2009-04-01 Euro-Celtique S.A. Use of a combination of an opioid agonist and an opioid antagonist for the treatment of Crohn's disease
WO2010003963A1 (en) * 2008-07-07 2010-01-14 Euro-Celtique S.A. Use of opioid antagonists for treating urinary retention
WO2010105672A1 (en) * 2009-03-18 2010-09-23 Evonik Röhm Gmbh Controlled release pharmaceutical composition with resistance against the influence of ethanol employing a coating comprising neutral vinyl polymers and excipients
WO2010121600A2 (en) * 2009-04-22 2010-10-28 Lars Holger Hermann Particulate pharmaceutical composition having an opioid and an opioid antagonist
WO2011117306A1 (en) * 2010-03-24 2011-09-29 L. Molteni & C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. Double-layer pharmaceutical formulations containing opioid agonists and antagonists
WO2011141489A1 (en) * 2010-05-10 2011-11-17 Euro-Celtique S.A. Manufacturing of active-free granules and tablets comprising the same
WO2011141488A2 (en) * 2010-05-10 2011-11-17 Euro-Celtique S.A. Pharmaceutical compositions comprising hydromorphone and naloxone
US20130245054A1 (en) * 2010-08-13 2013-09-19 Derek Allan Prater Use of binders for manufacturing storage stable formulations
WO2013050539A2 (en) * 2011-10-06 2013-04-11 Grünenthal GmbH Tamper-resistant oral pharmaceutical dosage form comprising opioid agonist and opioid antagonist
US20130129826A1 (en) * 2011-11-17 2013-05-23 Gruenenthal Gmbh Tamper-resistant oral pharmaceutical dosage form comprising opioid antagonist and/or aversive agent, polyalkylene oxide and anionic polymer
US20140322321A1 (en) * 2011-12-06 2014-10-30 Ethypharm Tablet capable of combatting misuse by injection
WO2013084059A1 (en) * 2011-12-09 2013-06-13 Purdue Pharma L.P. Pharmaceutical dosage forms comprising poly (epsilon- caprolactone) and polyethylene oxide
WO2015086528A1 (en) * 2013-12-11 2015-06-18 Develco Pharma Schweiz Ag Naloxone mono-product and multi-layer tablet

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"POLYOX (TM) Application Data Water Soluble Resins The Influence of In Vitro Dissolution Method on the Release of a Highly Water Soluble Drug from Polyethylene Oxide and Hypromellose Hydrophilic Extended Release Matrices", 1 March 2010 (2010-03-01), XP055174636, Retrieved from the Internet <URL:http://www.colorcon.com/literature/marketing/mr/Extended Release/POLYOX/English/ads_polyox_influ_in_vitro_diss_meth.pdf> [retrieved on 20150306] *
D O OPOTA ET AL: "The Efficiency Of Glyceryl Behenate As Sustained-Release Agent Compared With Hydroxypropylcellulose In Tablets", INTERNATIONAL JOURNAL OF PHARMTECH RESEARCH CODEN (USA): IJPRIF ISSN, 1 April 2013 (2013-04-01), pages 974 - 4304, XP055256810, Retrieved from the Internet <URL:http://sphinxsai.com/2013/pharmAJ13/pdf/PT=44(622-628)AJ13.pdf> [retrieved on 20160309] *
OBAIDAT A A ET AL: "Controlled release of tramadol hydrochloride from matrices prepared using glyceryl behenate", EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, ELSEVIER SCIENCE PUBLISHERS B.V., AMSTERDAM, NL, vol. 52, no. 2, 1 September 2001 (2001-09-01), pages 231 - 235, XP004301072, ISSN: 0939-6411, DOI: 10.1016/S0939-6411(01)00173-4 *

Also Published As

Publication number Publication date
EP3229785A2 (en) 2017-10-18
CN107205943A (en) 2017-09-26
WO2016091805A2 (en) 2016-06-16

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