Claims for Patent: 10,314,780

Summary for Patent: 10,314,780

Title:	Drippable opthalmic bimatoprost gel
Abstract:	The invention refers to a drippable ophthalmic gel, said gel having composition comprising bimatoprost in an amount of 0.003 to 0.03% by weight, polyacrylate in an amount of >0.2% by weight, povidone (PVP), dextrane, polyethylene glycols (PEG), carboxymethyl cellulose (CMC) or poly(vinyl alcohol) (PVA) in an amount of 0.2 to 10% by weight, an isotonizing agent in an amount to produce an osmolality of 200 to 400 mosml/kg, a salt for adjusting the viscosity in an amount of 0.05 to 0.4% by weight, a base in an amount to adjust the pH to 6 to 8 and excipients normally used in ophthalmic gels, having a viscosity in the range of 200 to 2000 mPa·s.
Inventor(s):	Heinz Polzer, Pierre-Paul Elena, Jürgen SENGE
Assignee:	MEDPROJECT PHARMA-ENTWICKLUNGS- und VERTRIEBSGESELLSCHAFT MBH , Laboratoires Thea SAS
Application Number:	US15/580,770
Patent Claims:	1. A drippable ophthalmic gel, said gel comprising 1) bimatoprost in an amount of 0.003 to 0.03% by weight, 2a) polyacrylate in an amount of >0.2% by weight, 2b) povidone, dextrane, polyethylene glycol, carboxymethyl cellulose or poly(vinyl-alcohol) in an amount of 0.2 to 10.0% by weight, 3) an isotonizing agent in an amount to produce an osmolality of 200 to 400 mosml/kg, 4) a salt for adjusting the viscosity in an amount of 0.05 to 0.4% by weight, 5) a base in an amount to adjust the pH to 6 to 8, 6) excipients normally used in ophthalmic gels, and 7) water, and having a viscosity in the range of 200 to 2000 mPa ·s, measured with a Brookfield RVDV-II Viscometer at 25° C. 2. The drippable ophthalmic gel according to claim 1 characterized in that the amount of polyacrylate is in the range of >0.2% to 3.0% by weight. 3. The drippable ophthalmic gel according to claim 1, characterized in that the amount of povidone is in the range of >0.8% to 10% by weight. 4. The gel according to claim 1, characterized in that the amount of bimatoprost is less than 0.01% by weight. 5. The gel according to claim 1, characterized by comprising sorbitol, mannitol or glycerol as an isotonizing agent in an amount of 1.2 to 5.5% by weight. 6. The gel according to claim 1, characterized by comprising a base in an amount of 0.1 to 0.8% by weight. 7. The gel according to claim 1, characterized in that the base is trometamol. 8. The gel according to claim 1, characterized by containing as the polyacrylate such types having a molecular weight between 1,000,000 and 4,000,000. 9. The gel according to claim 1, characterized by comprising no preservative. 10. The gel according to claim 1, characterized by comprising benzalkonium chloride as a preservative. 11. The gel according to claim 10, characterized in that the amount of benzalkonium chloride is in the range of 0.005 to 0.02% by weight. 12. A single-dose container containing the drippable ophthalmic gel according to claim 1, wherein the drippable ophthalmic gel is preservative-free. 13. A multidose plastic container containing the drippable ophthalmic gel according to claim 1, wherein the drippable ophthalmic gel contains a preservative. 14. A method of making the drippable ophthalmic gel according to claim 1, comprising the following steps: A) dissolving 2b) in 7) and heating while mixing; B) dissolving 5) in 7), C) dissolving 1), 3), 4), and 6) in 7) and then disperse 2a) therein, D) combining C) with A) to form a mixture, then adding B) to the mixture, and then adding 7) thereto. 15. A method of treating a subject suffering from elevated intraocular pressure, comprising administering the drippable ophthalmic gel of claim 1 to said subject, thereby reducing elevated intraocular pressure in said subject. 16. The drippable ophthalmic gel of claim 1, wherein the drippable ophthalmic gel comprises the isotonizing agent in an amount to produce an osmolality of 270 to 330 mosmol/kg. 17. The drippable ophthalmic gel of claim 1, wherein the base is in an amount to adjust the pH to 7.3. 18. The drippable ophthalmic gel of claim 1, wherein the amount of polyacrylate is in the range of >0.2% to 0.7% by weight. 19. The drippable ophthalmic gel of claim 1, wherein the amount of povidone is in the range of >2.5% to 10% by weight. 20. The drippable ophthalmic gel of claim 1, wherein the amount of bimatoprost is less than 0.0045% by weight.