Pharmaceutical compositions having desirable bioavailability
View Patent ↗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.
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.