Ophthalmic gel compositions of bimatoprost and timolol and associated methods
Inventors
Shah, Mandar V. • Subramanian, Veerappan • Subramanian, Ilango • Trehan, Aman
Assignees
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Publication Number
US-12064440-B2
Publication Date
2024-08-20
Expiration Date
Abstract
The present invention provides pharmaceutically acceptable and ophthalmologically suitable gel compositions comprising a therapeutically effective amount of a bimatoprost compound, a therapeutically effective amount of a timolol compound, and benzalkonium chloride. In certain embodiments, compositions provided by the invention further comprise a penetration enhancer component other than benzalkonium chloride. Further, the invention provides a process of preparing such compositions and methods of their use in treating ocular conditions, such as methods of reducing elevated intraocular pressure and/or treating glaucoma, such as open-angle glaucoma.
Core Innovation
The disclosure describes a pharmaceutically acceptable and ophthalmologically suitable gel composition that contains bimatoprost and timolol as the only active pharmaceutical ingredients. The gel includes benzalkonium chloride, a penetration enhancer component comprising one or more compounds selected from polyoxyethylene sorbitan fatty acid ester, tocopheryl polyethylene glycol succinate, polyoxyl hydrogenated castor oil, poly-arginine, and polyserine, and a viscosity enhancing component comprised of gellan gum, with defined concentration ranges and ratios.
The gel is characterized by a viscosity of less than about 75 cps after manufacture and while in storage at about 15°C to about 27°C, and by stability during storage at specified temperature and relative-humidity conditions for at least about one month. The timolol compound to viscosity enhancer component ratio is about 10:1 to about 1:10.
The composition is described as having gelling agents responsive to an ocular environment, with viscosity increasing upon exposure to the mammalian eye environment under conditions including temperature, ionic strength, and pH greater than about 6.2. The therapeutic context identified is treatment of elevated intraocular pressure and/or glaucoma, including open-angle glaucoma, by administration of the composition.
Claims Coverage
The provided claim material centers on one independent ophthalmic gel composition claim, with the core inventive features defined by bimatoprost and timolol as the only active pharmaceutical ingredients, benzalkonium chloride, a selected penetration enhancer component, gellan gum, and a viscosity limitation at defined storage temperatures. Dependent features further refine component selection, ratios, stability, viscosity behavior, and therapeutic use.
Bimatoprost and timolol only ophthalmic gel with defined accessory components
A pharmaceutically acceptable and ophthalmologically suitable gel comprising a bimatoprost compound, a timolol compound, benzalkonium chloride, a penetration enhancer component comprising one or more selected compounds, and a viscosity enhancing component, wherein bimatoprost compound and timolol compound are the only active pharmaceutical ingredients.
Penetration enhancer selection with defined composition ratios
A penetration enhancer component comprising one or more compounds selected from polyoxyethylene sorbitan fatty acid ester, tocopheryl polyethylene glycol succinate, polyoxyl hydrogenated castor oil, poly-arginine, and polyserine, with defined amount and ratios including a timolol-to-penetration enhancer ratio.
Gellan gum viscosity limitation and timolol-to-viscosity enhancer ratio
A viscosity enhancing component that is gellan gum, with timolol compound to viscosity enhancer component ratio of about 10:1 to about 1:10, and a gel viscosity of less than about 75 cps after manufacture and while in storage at about 15°C to about 27°C.
Condition-dependent viscosity increase in mammalian eye environment
A composition in which viscosity detectably or significantly increases when exposed to the mammalian eye environment under specified conditions relative to viscosity when stored at about 15°C to about 25°C (+/-2°C).
Stability during storage under defined temperature and relative-humidity conditions
A composition that remains stable during storage at specified temperature and relative-humidity conditions for at least about one month.
The claim scope focuses on a gellan gum-based ophthalmic gel with bimatoprost and timolol as the only active pharmaceutical ingredients, benzalkonium chloride, a selected penetration enhancer component, a defined timolol-to-gellan-gum ratio, and a viscosity limitation after manufacture and during storage. Dependent features further narrow viscosity behavior, stability, and therapeutic use.
Stated Advantages
Reductions in the frequency of ocular and periocular adverse effects/clinical findings versus reference bimatoprost/timolol formulations and comparator regimens are described.
The document describes comparative effectiveness for treating elevated intraocular pressure and glaucoma in the context of fixed-dose compositions.
Treats elevated intraocular pressure and/or glaucoma, including open-angle glaucoma.
Reduces ocular adverse events such as redness, burning, and itching versus reference products such as GANFORT®.
Documented Applications
Treating elevated intraocular pressure and/or glaucoma in a mammalian eye by administering an effective amount of the composition.
Lowering intraocular pressure and treating glaucoma and ocular hypertension.
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