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Last Updated: April 18, 2024

Claims for Patent: 8,754,123


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Summary for Patent: 8,754,123
Title:Pharmaceutical compositions having desirable bioavailability
Abstract: The present invention is directed to the provision of pharmaceutical compositions. The compositions include a therapeutic agent and a relatively low amount of surfactant for providing higher bioavailability of the therapeutic agent. The compositions are particularly desirable as ophthalmic compositions in which the therapeutic agent is a prostaglandin such as travoprost and the surfactant is a vegetable oil such as castor oil.
Inventor(s): Kabra; Bhagwati P. (Euless, TX)
Assignee: Alcon Research, Ltd. (Fort Worth, TX)
Application Number:13/442,475
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,754,123
Patent Claims: 1. An aqueous ophthalmic pharmaceutical solution composition suitable for topical application to an eye of a human, comprising: a prostaglandin suitable for lowering intraocular pressure of the eye, the prostaglandin being in the composition at a concentration that is at least 0.001 w/v % but less than 0.01 w/v %; a surfactant in the composition at a concentration that is at least 0.03 w/v % but less than 0.3 w/v %, wherein: i. the surfactant is entirely ethoxylated and/or hydrogenated vegetable oil and the ethoxylated and/or hydrogenated castor oil is the only surfactant in the composition; and ii. the composition is free of benzalkonium chloride; and a polymeric quaternary ammonium compound in the composition at a concentration that is greater than 0.0003 w/v % but less than 0.003 w/v %; and water.

2. A composition as in claim 1 wherein concentration of the surfactant in the composition is less than 0.15 w/v %.

3. A composition as in claim 1 wherein the prostaglandin is travoprost.

4. A composition as in claim 1 wherein the prostaglandin and the surfactant are non-ionic.

5. A composition as in claim 1 wherein the surfactant is entirely ethoxylated or hydrogenated vegetable oil.

6. A composition as in claim 1 wherein the surfactant is entirely castor oil.

7. A composition as in claim 1 wherein the surfactant is entirely Polyoxyl 40 Hydrogenated castor Oil.

8. A composition as in claim 1 wherein the composition satisfies Ph. Eur. A, Ph. Eur. B or both.

9. A composition as in claim 1 wherein the composition is substantially free of any chloride containing agents.

10. A composition as in claim 1 wherein the prostaglandin is in the composition at a concentration of less than 0.006 w/v %.

11. A composition as in claim 1 wherein the composition is disposed in an eye dropper.

12. A composition as in claim 4 wherein the surfactant is entirely ethoxylated and/or hydrogenated vegetable oil.

13. A composition as in claim 12 wherein the surfactant is entirely castor oil.

14. A composition as in claim 13 wherein the prostaglandin is in the composition at a concentration of less than 0.006 w/v %.

15. A composition as in claim 14 wherein the composition satisfies Ph. Eur. A, Ph. Eur. B or both.

16. A composition as in claim 14 wherein the prostaglandin is travoprost.

17. A composition as in claim 16 wherein the surfactant is entirely Polyoxyl 40 Hydrogenated castor Oil.

18. A composition as in claim 17 wherein the composition is disposed in an eye dropper.

19. A composition as in claim 18 wherein concentration of the surfactant in the composition is less than 0.15 w/v %.

20. A composition as in claim 18 wherein concentration of the polymeric quaternary ammonium compound in the composition is greater than 0.0007 w/v % but less than 0.0015 w/v % of the pharmaceutical composition.

21. A composition as in claim 1 wherein concentration of the polymeric quaternary ammonium compound in the composition is greater than 0.0007 w/v % but less than 0.0015 w/v % of the pharmaceutical composition.

22. A composition as in claim 1 wherein the polymeric quaternary ammonium compound is polyquaternium-1.

23. A composition as in claim 20 wherein the polymeric quaternary ammonium compound is polyquaternium-1.

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