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US 8,298,569 B2Granted
Ophthalmic emulsions containing an immunosuppressive agent
AssigneeNovagali Pharma SA
InventorsBetty Philips, Severine Bague, Laura Rabinovich-Guilatt, Gregory Lambert
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Abstract
Ophthalmic oil-in-water emulsions, which comprises colloid particles having an oily core surrounded by an interfacial film, the emulsion comprising an 10 immunosuppressive agent, an oil, preferably at least 50% of which being MCT, and tyloxapol. Use of such an emulsion for the manufacture of medicament for treatment of eye conditions, particularly of dry eye diseases.
Claims9
An ophthalmic oil-in-water emulsion, which comprises colloid particles having an oily core surrounded by an interfacial film, said emulsion comprising:
- 0.05 to 0.3% cyclosporine in weight to the total weight (w/w) of the emulsion,
- 0.5 to 4% w/w medium-chain triglycerides,
- 0.02% w/w benzalkonium chloride, and
- surfactants,
- wherein the surfactants consist of a mixture of tyloxapol and poloxamer,
- wherein the tyloxapol is present in an amount of 0.3% w/w and the poloxamer is present in an amount of 0.1% w/w, and
- wherein said emulsion is cationic,
- wherein said emulsion meets zeta potential stability under thermal stress conditions as determined by Test A:
- measuring zeta potential, in mV, of said emulsion at the time of preparation is Z0,
- sealing 5-10 ml of said emulsion in 10 ml Type I glass vials under nitrogen atmosphere without bubbling,
- storing said sealed vials at 80° C. for 7 days,
- measuring zeta potential, in mV, of said emulsion at 7 days, Z7days,
- determining the difference between Z7days−Z0, δA, the emulsion meeting the zeta potential stability under thermal stress conditions according to Test A for a δA less than the 10 mV standard error of zeta potential measurement,
- wherein said emulsion does not comprise phospholipids, and
- wherein said emulsion does not comprise substances capable of generating a negative charge.
12 more elements
Dependencies are inferred from the claim text.