Patent application EP16461520A (EP), filed 2016-05-09
Publication number: EP3243506A1
Title: PHARMACEUTICAL COMPOSITION
Abstract: The present invention relates to a pharmaceutical composition comprising rosuvastatin and ezetimibe for oral administration in the form of a blend of a first component comprising rosuvastatin or a pharmaceutically acceptable salt thereof, wherein the component is dry-granulated, a second component comprising ezetimibe or a pharmaceutically acceptable salt thereof, wherein the component is wet-granulated, and an optionally extragranular phase component, characterized in that the pharmaceutical composition is free from any rosuvastatin stabilizers, and d 90  value for granules of the first component is 800 µm or less. The invention relates also to an uncoated tablet comprising the composition, and a method of manufacturing the composition.
IPC codes: A61K  31/    00            A I
A61K   9/    16            A I
A61K   9/    20            A I
Claims: number: 1
text: A pharmaceutical composition comprising rosuvastatin and ezetimibe for oral administration in the form of a blend of:
number: 2
text: The pharmaceutical composition of claim 1 characterized in that the pharmaceutical composition consists of:
number: 3
text: The pharmaceutical composition of claim 1 - 2 characterized in that d<90> value for granules of the first component is 500 µm or less.
number: 4
text: The pharmaceutical composition of claim 1-3 characterized in that rosuvastatin or a pharmaceutically acceptable salt thereof is rosuvastatin calcium, and ezetimibe or a pharmaceutically acceptable salt thereof is ezetimibe.
number: 5
text: The pharmaceutical composition of claim 1-4 characterized in that the first component comprising rosuvastatin or a pharmaceutically acceptable salt thereof consists of rosuvastatin or a pharmaceutically acceptable salt thereof, at least one filler, at least one disintegrant, at least one binder, and/or at least one lubricant.
number: 6
text: The pharmaceutical composition of claim 1-5 characterized in that the second component comprising ezetimibe or a pharmaceutically acceptable salt thereof consists of ezetimibe or a pharmaceutically acceptable salt thereof, at least one filler, at least one disintegrant, at least one binder and/or at least one surfactant.
number: 7
text: The pharmaceutical composition of claim 1-6 characterized in that the extragranular phase component consists of excipients selected form at least one filler, at least one binder, at least one disintegrant, at least one surfactant, and/or at least one lubricant.
number: 8
text: The pharmaceutical composition of claim 5-7 characterized in that at least one filler is selected from lactose monohydrate, microcrystalline cellulose, or a mixture thereof
number: 9
text: The pharmaceutical composition of claim 5-7 characterized in that at least one binder is selected from hydroxypropyl cellulose, polyvinylpyrrolidone or a mixture thereof.
number: 10
text: The pharmaceutical composition of claim 5-7 characterized in that at least one disintegrant is selected from sodium carboxymethyl cellulose, crospovidone or a mixture thereof.
number: 11
text: An uncoated tablet comprising a pharmaceutical composition as described in claims 1-10.
number: 12
text: Method for obtaining the pharmaceutical composition as defined in any of claims 1-10 characterized in that it comprises the following steps:
Office action: search_report, dated 2017-11-15
Rejection reasons: inventive_step_epc_56
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ref_id: - "Handbook of Pharmaceutical Excipients", PHARMACEUTICAL PRESS
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ref_id: - "DRY GRANULATION PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION", IP.COM JOURNAL, IP.COM INC., WEST HENRIETTA, NY, US, 22 June 2010 (2010-06-22), XP013138810, ISSN: 1533-0001
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severity: background
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severity: obviousness
ref_id: - "DRY GRANULATION PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION", IP.COM JOURNAL, IP.COM INC., WEST HENRIETTA, NY, US, (20100622), ISSN 1533-0001, XP013138810 [Y] 1-12 * page  2, line  16  - line  27 * * page  3, line  13  - line  18 * * examples 1-2 *
ref_type: npl
severity: obviousness
Final disposition: pending (2017-11-15)