Ophthalmic preparations
First Claim
Patent Images
1. An ophthalmic formulation comprising:
- (a) cyclosporine or a derivative thereof,(b) at least one solvent,(c) at least one oil,(d) at least one surfactant,(e) at least one preservative, and(f) water or buffer.
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Accused Products
Abstract
The present invention provides ophthalmic formulations containing cyclosporine, methods for preparing the formulation, and methods for using the formulation.
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Citations
34 Claims
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1. An ophthalmic formulation comprising:
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(a) cyclosporine or a derivative thereof, (b) at least one solvent, (c) at least one oil, (d) at least one surfactant, (e) at least one preservative, and (f) water or buffer. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 20, 21)
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19. An ophthalmic formulation comprising:
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(a) cyclosporine A, (b) ethanol, (c) medium chain triglycerides, (d) Polysorbate 80, (e) benzalkonium chloride, and (f) phosphate buffer.
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22. A method for preparing particles of cyclosporine or a derivative thereof, comprising:
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(a) forming an emulsion base by suspending cyclosporine or a derivative thereof in a mixture of oil, solvent, surfactant, preservative, and water or buffer to form an emulsion base, and (b) homogenizing the emulsion base to form particles of cyclosporine or a derivative thereof, droplets comprising solubilized cyclosporine or a derivative thereof, or a combination thereof. - View Dependent Claims (23, 24, 25, 26, 27)
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28. A method for preparing particles of cyclosporine or a derivative thereof, comprising:
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(a) dissolving cyclosporine or a derivative thereof in a mixture of (i) at least one oil, (ii) at least one solvent, and (iii) at least one surfactant to form an emulsion pre-mix, (b) adding at least one preservative, and water or buffer to the emulsion pre-mix, and (c) homogenizing or vigorously stirring the mixture of step (b), whereby cyclosporine A or a derivative thereof is precipitated into particles. - View Dependent Claims (29, 30, 31, 32, 33)
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34. A method for preparing particles of cyclosporine or a derivative thereof, comprising:
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(a) dissolving cyclosporine or a derivative thereof in ethanol to form a solution, (b) adding Polysorbate 80 and medium chain triglyceride to the solution of step (a), (c) adding benzalkonium chloride dissolved in water to the solution of (b), and (d) subjecting the solution of (c) to high-pressure homogenization to produce particles of cyclosporine or a derivative thereof.
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Specification