Patent application EP16461511A (EP), filed 2016-03-21
Publication number: EP3222279A1
Title: ORAL PHARMACEUTICAL FORMULATION OF MONTELUKAST AND LEVOCETIRIZINE AND METHOD FOR ITS PRODUCTION
Abstract: A pharmaceutical formulation for oral administration for treating asthma and accompanying allergic rhinitis comprising (a) levocetirizine or a pharmaceutically acceptable salt thereof mixed together with (b) montelukast or a pharmaceutically acceptable salt thereof, placed together in a single standard coated tablet with good long-term storage stability.  A method for preparing the above stable tablet formulation is also disclosed.
IPC codes: A61K  31/    47            A I
A61K  31/   495            A I
A61P  11/    02            A I
A61P  11/    06            A I
A61K   9/    20            A I
A61K   9/    28            A I
Claims: number: 1
text: A pharmaceutical formulation for oral administration for treating asthma and accompanying allergic rhinitis which comprises
number: 2
text: The pharmaceutical formulation according to claim 1 wherein the pharmaceutically acceptable salt of levocetirizine is levocetirizine dihydrochloride and the pharmaceutically acceptable salt of montelukast is montelukast sodium.
number: 3
text: The pharmaceutical formulation according to any preceding claim comprising
number: 4
text: The pharmaceutical formulation according to any preceding claim comprising
number: 5
text: The pharmaceutical formulation according to claim 3 or 4 comprising levocetirizine dihydrochloride in the amount of 5 mg and montelukast sodium in the amount equivalent to 10 mg of the montelukast free acid.
number: 6
text: The pharmaceutical formulation according to claim 3 or 4, wherein the significant change is the content of montelukast impurity C of formula (III) higher than 0.5% based on nominal montelukast content.
number: 8
text: A method for preparing the pharmaceutical formulation for oral administration for treating asthma and accompanying allergic rhinitis which comprises levocetirizine or a pharmaceutically acceptable salt thereof and montelukast or a pharmaceutically acceptable salt thereof as defined in claim 1, characterized in that the method comprises the steps of:
number: 9
text: The method of claim 8 wherein the pharmaceutically acceptable additive is selected from a group comprising: microcrystalline cellulose, powdered cellulose, silicified microcrystalline cellulose, ethers of cellulose including hydroxypropyl cellulose and hydroxypropyl methylcellulose, lactose, lactose monohydrate, lactose anhydrous, spray dried lactose, croscarmellose or its salt.
number: 10
text: The method of claim 8 or 9 wherein blending steps (I), (II) and (III) are followed by sieving.
number: 11
text: The method of any of the claims 8-10 wherein the stages (I) and (II) are preceded by manually mixing of the ingredients.
number: 12
text: The method of any of the claims 8-11 wherein the pharmaceutically acceptable salt of levocetirizine is levocetirizine dihydrochloride and the pharmaceutically acceptable salt of montelukast is montelukast sodium.
Office action: search_report, dated 2017-09-27
Rejection reasons: novelty_epc_54
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ref_id: BR102013004720A2
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severity: background
ref_id: - RATHOD R T ET AL: "FDC of montelukast with levocetirizine: focus on bilayer technology", JOURNAL OF THE INDIAN MEDICAL ASSOCIATION, INDIAN MEDICAL ASSOCIATION, CALCUTTA, IN, vol. 107, no. 8, 1 August 2009 (2009-08-01), pages 562 - 564, XP008173253, ISSN: 0019-5847
ref_type: npl
severity: background
ref_id: BR102013004720
ref_type: patent
severity: novelty_destroying
ref_id: - RATHOD R T ET AL, "FDC of montelukast with levocetirizine: focus on bilayer technology", JOURNAL OF THE INDIAN MEDICAL ASSOCIATION, INDIAN MEDICAL ASSOCIATION, CALCUTTA, IN, (20090801), vol. 107, no. 8, ISSN 0019-5847, pages 562 - 564, XP008173253 [AD] 1-12 * the whole document *
ref_type: npl
severity: background
Final disposition: pending (2017-09-27)