Suspension formulations of nepafenac and other ophthalmic drugs for topical treatment of ophthalmic disorders

A surfactant, ophthalmic technology, applied in the directions of medical preparations containing active ingredients, organic active ingredients, drug combinations, etc., can solve the problem of undisclosed combination effects and other issues

Inactive Publication Date: 2008-05-07
ALCON INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although poloxamer and meloxapol surfactants (including those commercially available as Pluronic  and Pluronic  R surfactant) and propylene glycol are known to be used in ophthalmic compositions for topical administration, respectively, but they have not been used in combination with nepafenac, and their combined effect on corneal penetration of slightly water-soluble ophthalmic drugs is still unknown. unpublished

Method used

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  • Suspension formulations of nepafenac and other ophthalmic drugs for topical treatment of ophthalmic disorders
  • Suspension formulations of nepafenac and other ophthalmic drugs for topical treatment of ophthalmic disorders
  • Suspension formulations of nepafenac and other ophthalmic drugs for topical treatment of ophthalmic disorders

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Experimental program
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Effect test

Embodiment 1

[0031] The formulations shown below are representative compositions of the invention.

[0032] 1

Embodiment 2

[0034] The formulations shown below are representative compositions of the invention.

[0035] 2

[0036] Benzalkonium chloride

Embodiment 3

[0038] The formulations shown in Table 1 were prepared and evaluated in an ex vivo corneal penetration model. Corneal penetration results are also shown in Table 1. Formulations A-C were prepared by ball milling nepafenac in a slurry containing tyloxapol and / or polysorbate 80 for about 18 hours. Formulation AA is prepared by dissolving nepafenac in Pluronic  A mixture of P-104 and propylene glycol followed by the addition of the remaining ingredients is prepared. The rabbit model of ex vivo corneal infiltration is briefly described as follows:

[0039] Rabbits were sacrificed by first anesthetizing with ketamine (30 mg / Kg) and xylazine (6 mg / Kg), followed by injecting overdose of SLEEPAWAY(R) (sodium pentobarbital, 1 ml of 26% solution) into the marginal ear vein. The intact eye with eyelids and conjunctival sac is then removed and immediately stored in approximately 70 ml of fresh O 2 / CO 2 (95:5) in saturated BSS PLUS(R) lavage fluid. Within 1 hour, the enucleated rab...

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Abstract

Topical aqueous suspension compositions of sparingly soluble ophthalmic drugs are disclosed. The compositions comprise a combination of a poloxamer or meroxapol surfactant and a glycol tonicity-adjusting agent such as propylene glycol.

Description

Background of the invention [0001] The present invention relates to pharmaceutical compositions for the treatment of ophthalmic conditions. In particular, the present invention relates to suspension formulations for topical administration of nepafenac and other ophthalmic drugs. [0002] Nepafenac is also known as 2-amino-3-benzoylphenylacetamide. US Patent No. 5,475,034 discloses the topical application of nepafenac and other amide and ester derivatives of 3-benzoylphenylacetic acid to treat ophthalmic inflammation and pain. According to the '034 patent, compositions comprising 3-benzoylphenylacetic acid derivatives can be formulated into a variety of topically administrable ophthalmic compositions such as solutions, suspensions, gels or ointments. The composition optionally contains preservatives, such as benzalkonium chloride; and thickeners, such as carbomer, hydroxyethylcellulose or polyvinyl alcohol. However, the '034 patent does not disclose any formulations of nepaf...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/165A61K31/542A61K31/57
CPCA61K9/0048A61K31/165A61K31/57A61K31/542A61K9/10A61P27/02A61P27/06A61K9/08
Inventor G·R·欧文A·C·布鲁克斯G·格拉夫
Owner ALCON INC
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