AQUEOUS LIQUID PREPARATION CONTAINING 2-AMINO-3-(4-BROMOBENZOYL)PHENYLACETIC ACID
First Claim
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1. A stable aqueous liquid preparation consisting essentially of:
- (a) a first component;
(b) a second component;
wherein the first component is 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof;
(c) boric acid;
(d) sodium tetraborate; and
(e) water;
wherein the hydrate is at least one selected from a 1/2 hydrate, 1 hydrate, and 3/2 hydrate;
the first component is the sole pharmaceutical active ingredient contained in the preparation and is present in the preparation at a concentration from about 0.05 w/v % to about 0.2 w/v %;
the second component is tyloxapol and is present in said liquid preparation in an amount sufficient to stabilize said first component; and
wherein said stable liquid preparation is formulated for ophthalmic administration.
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Abstract
An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. An embodiment of said liquid preparation does not include any preservative. Said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
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Citations
25 Claims
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1. A stable aqueous liquid preparation consisting essentially of:
- (a) a first component;
(b) a second component;
wherein the first component is 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof;
(c) boric acid;
(d) sodium tetraborate; and
(e) water;
wherein the hydrate is at least one selected from a 1/2 hydrate, 1 hydrate, and 3/2 hydrate;
the first component is the sole pharmaceutical active ingredient contained in the preparation and is present in the preparation at a concentration from about 0.05 w/v % to about 0.2 w/v %;
the second component is tyloxapol and is present in said liquid preparation in an amount sufficient to stabilize said first component; and
wherein said stable liquid preparation is formulated for ophthalmic administration. - View Dependent Claims (2, 3, 4, 5, 22, 25)
- (a) a first component;
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6. A stable aqueous liquid preparation consisting essentially of:
- (a) a first component;
(b) a second component;
wherein the first component is 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof;
(c) boric acid;
(d) sodium tetraborate; and
(e) water;
wherein the hydrate is at least one selected from a 1/2 hydrate, 1 hydrate, and 3/2 hydrate;
the first component is the sole pharmaceutical active ingredient contained in the preparation and is present in the preparation at a concentration from about 0.04 w/v % to about 0.1 w/v %;
the second component is tyloxapol;
wherein said stable liquid preparation is formulated for ophthalmic administration; and
wherein the stable aqueous liquid preparation is characterized in that at least about 89% of the original amount of the first component remains in the preparation after storage at about 60°
C. for 4 weeks. - View Dependent Claims (7, 8, 9, 10, 23)
- (a) a first component;
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11. A stable aqueous liquid preparation consisting essentially of:
- (a) a first component; and
(b) a second component;
wherein the first component is 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof;
(c) boric acid;
(d) sodium tetraborate; and
(e) water;
wherein the hydrate is at least one selected from a 1/2 hydrate, 1 hydrate, and 3/2 hydrate;
the first component is the sole pharmaceutical active ingredient contained in the preparation and is present in the preparation at a concentration from about 0.04 w/v % to about 0.2 w/v %;
the second component is tyloxapol;
wherein said stable liquid preparation is formulated for ophthalmic administration;
provided that the liquid preparation does not include mannitol. - View Dependent Claims (12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 24)
- (a) a first component; and
Specification
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Current AssigneeSenju Pharmaceutical Company Limited
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Original AssigneeSenju Pharmaceutical Company Limited
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InventorsSAWA, Shirou, FUJITA, Shuhei, BAKLAYAN, George A., PADILLA, Angeliqueo E.
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/567
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CPC Class CodesA61K 31/196 the amino group being direc...A61K 47/02 Inorganic compoundsA61K 47/10 Alcohols; Phenols; Salts th...A61K 47/14 Esters of carboxylic acids,...A61K 47/32 Macromolecular compounds ob...A61K 47/34 Macromolecular compounds ob...A61K 9/0043 NoseA61K 9/0048 Eye, e.g. artificial tearsA61P 27/02 Ophthalmic agentsA61P 27/16 OtologicalsA61P 29/00 Non-central analgesic, anti...
