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Bromfenac ophthalmic formulations and methods of use

a technology of bromfenac and ophthalmic composition, which is applied in the field of bromfenac ophthalmic formulation and method of use, can solve the problems of incompatibility of benzalkonium chloride and other quaternary ammonium compounds with ophthalmic composition, topical corticosteroids are also known to slow or delay healing, so as to reduce the preservative

Inactive Publication Date: 2007-12-13
SENJU PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0021] It is also an object of the present invention to provide an aqueous liquid preparation comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof, which is stable within a pH range giving minimal or no irritation to eyes and in which, when a preservative such as benzalkonium chloride is incorporated therein, preservative effect of the preservative does not substantially deteriorate.

Problems solved by technology

However, benzalkonium chloride and other quaternary ammonium compounds are generally considered to be incompatible with ophthalmic compositions of drugs with acidic groups, such as nonsteroidal anti-inflammatory drugs (NSAIDs).
All topical NSAIDs may slow or delay healing.
Topical corticosteroids are also known to slow or delay healing.
Concomitant use of topical NSAIDs and topical steroids may increase the potential for healing problems.
Use of topical NSAIDs may result in keratitis.
In some susceptible patients, continued use of topical NSAIDs may result in epithelial breakdown, corneal thinning, corneal ulceration or corneal perforation.
These events may be sight threatening.
Postmarketing experience with topical NSAIDs suggests that patients with complicated ocular surgeries, corneal denervation, corneal epithelial defects, diabetes mellitus, ocular surface diseases (e.g., dry eye syndrome), rheumatoid arthritis, or repeat ocular surgeries within a short period of time may be at increased risk for corneal adverse events which may become sight-threatening.

Method used

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  • Bromfenac ophthalmic formulations and methods of use
  • Bromfenac ophthalmic formulations and methods of use

Examples

Experimental program
Comparison scheme
Effect test

experimental example 1

Stability Test of Sodium 2-amino-3-(4-bromobenzoyl)phenylacetate

[0147] Four eye drops of sodium 2-amino-3-(4-bromobenzoyl)phenylacetate comprising the components as shown in Table 1 were prepared, filled respectively into a polypropylene container and subjected to stability test at 60.degree. C.

TABLE 1ComparisonComponentExample 1A-01A-02A-03Sodium 2-amino-3-(4-0.1 g0.1 g0.1 g0.1 gbromobenzoyl)phenyl-acetateBoric acid1.5 g1.5 g1.5 g1.5 gBenzalkonium chloride0.005 g 0.005 g 0.005 g 0.005 g Polysorbate 800.15 g ———Polyoxyl 40 stearate—0.15 g ——Tyloxapol——0.15 g 0.02 g Sterile purified waterq.s.q.s.q.s.q.sTotal volume 100 mL 100 mL 100 mL 100 mLpH7.07.07.07.0Remaining rate51.3 63.7 73.8 89.6 (%) at 60° C.after 4 weeks

[0148] The remaining rate (%) in the above Table 1 indicates values obtained by correcting moisture vaporization from the container. As is apparent from the Table 1, stability test was carried out under the conditions of pH 7.0 at 60° C. for 4 weeks, and sodium 2-amino-3...

experimental example 2

Stability Test of Sodium 2-amino-3-(4-bromobenzoyl)phenylacetate

[0150] Five eye drops of sodium 2-amino-3-(4-bromobenzoyl)phenylacetate comprising the components as shown in Table 2 were prepared, filled respectively into a polypropylene container and preserved at 60.degree. C. for 4 weeks, and then the content of 2-amino-3-(4-bromobenzoyl)phenylacetic acid and the pH in each eye drop were measured.

TABLE 2ComponentsA-04A-05A-06A-07A-08Sodium 2-amino-3-(4-0.1 g0.1 g0.1 g0.1 g0.1 gbromobenzoyl)phenylacetateBoric acid1.1 g1.1 g1.1 g1.1 g1.1 gBorax1.1 g1.1 g1.1 g1.1 g1.1 gBenzalkonium chloride0.005 g 0.005 g 0.005 g 0.005 g 0.005 g Polysorbate 80—————Tyloxapol0.02 g 0.05 g 0.03 g ——Polyoxyl 40 stearate———0.02 g 0.05 g Polyvinylpyrrolidone (K-30)2.0 g2.0 g2.0 g2.0 g1.0 gSodium edetate0.02 g 0.02 g 0.02 g 0.02 g 0.02 g Sodium hydroxideq.s.q.s.q.s.q.s.q.s.Sterile purified waterq.s.q.s.q.s.q.s.q.s.Total volume 100 mL 100 mL 100 mL 100 mL 100 mLpH8.178.168.158.198.1960° C.,Remaining rate ...

experimental example 3

Preservative Effect Test of Aqueous Liquid Preparation Containing Sodium 2-amino-3-(4-bromobenzoyl)phenylacetate

[0152] Preservative effect test of compositions A-04, A-05 and A-07 of Experimental Example 2 was carried out against Staphylococcus aureus (hereinafter referred to as S. aureus), Escherichia Coli (hereinafter referred to as E. coli), Pseudomonas aeruginosa (hereinafter referred to as P. aeruginosa), Candida albicans (hereinafter referred to as C. albicans) and Aspergillus niger (hereinafter referred to as A. niger).

[0153] The results are shown in Tables 3-1, 3-2 and 3-3.

[0154] Table 3-1

TABLE 3-1Cell count (CFU / mL)6 hours24 hours7 days14 days21 days28 daysInoculumafterafterafterafterafterafterA-04countinoculationinoculationinoculationinoculationinoculationinoculationS. aureus2.1 × 1063.0 × 10100000E. coli6.5 × 106000000P. aeruginosa5.8 × 106000000C. albicans3.2 × 105——0000A. niger1.8 × 105——0000

[0155] Table 3-2

TABLE 3-2Cell count (CFU / mL)6 hours24 hours7 days14 days21...

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Abstract

The present invention discloses a stability enhanced aqueous liquid preparation 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. The present invention further discloses new bromfenac ophthalmic compositions which can potentially treat a broader patient population, and have greater stability properties, and may require a lower concentration or less doses of bromfenac then previously known bromfenac compositions. The present invention further comprises a method for treating inflammation and / or pain of the eye in a patient which method comprises topical application to the eye of a patient in need thereof of a therapeutically effective amount of a topical ophthalmic composition comprising bromfenac at a concentration of about 0.05% w / v to about 0.24% w / v.

Description

CROSS-REFERENCES TO RELATED APPLICATIONS [0001] This application is a continuation-in-part of U.S. patent application Ser. No. 10 / 525,006 filed Jan. 16, 2004, which claims priority to Japanese Patent Application No. 12427 / 2003 filed on Jan. 21, 2003 in Japan. This application also claims the benefit of priority from U.S. Provisional Patent Application 60 / 803,621, and 60 / 803,618 both filed May 31, 2006. All four of the listed applications are hereby incorporated in their entirety as if fully set forth.BACKGROUND OF THE INVENTION [0002] The present invention relates to an aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof. More particularly, the present invention relates to an aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or a pharmacologically acceptable salt thereof or a hydrate thereof and an alkyl aryl polyether alcohol type polymer or a polyethyle...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/195A61P27/02A61K9/00A61K31/196A61K47/14A61P29/00
CPCA61K9/0043A61K9/0048A61K31/196A61K47/14A61K47/186A61K47/10A61K47/32A61K47/183A61K47/02A61K47/34A61P27/02A61P27/16A61P29/00A61K9/08
Inventor SAWA, SHIROUFUJITA, SHUHEIGRILLONE, LISA R.
Owner SENJU PHARMA CO LTD
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