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 ophthalmic pharmaceutical composition, comprising:
a pharmaceutical vehicle suitable for topical application to an eye of a human;
at least 0.001 w/v % but less than 0.01 w/v % travoprost as a therapeutic agent for lowering intraocular pressure;
greater than 0.0003 w/v % but less than 0.003 w/v % polymeric quaternary ammonium compound as a preservative; and
an effectively low amount of surfactant sufficient for providing a high degree of bioavailability of the travoprost, wherein:
i. the amount of surfactant is at least 0.01 w/v % but below 0.4 w/v % of the composition;
ii. the surfactant is entirely ethoxylated and hydrogenated castor oil;
iii. the composition is substantially free of benzalkonium chloride; and
iv. the pharmaceutical vehicle includes water.
2. A composition as in claim 1 wherein the concentration of the surfactant is at least 0.03 w/v % but less than 0.3 w/v %.
3. A composition as in claim 1 wherein the composition has a pH of 6.4 to 7.5.
4. A composition as in claim 1 wherein the surfactant is non-ionic.
5. A composition as in claim 1 wherein the composition has a pH of 6.4 to 7.2.
6. A composition as in claim 1 wherein the composition satisfies Ph. Eur. A, Ph. Eur. B or both.
7. A composition as in claim 1 wherein the composition is disposed in an eye dropper.
8. A composition as in claim 1 wherein concentration of the surfactant in the composition is less than 0.15 w/v %.
9. A composition as in claim 1 wherein the surfactant is entirely Polyoxyl 40 Hydrogenated castor Oil.
10. A composition as in claim 1 wherein the travoprost is in the composition at a concentration of less than 0.006 w/v %.
11. 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.
12. A composition as in claim 1 wherein the polymeric quaternary ammonium compound is polyquaternium-1.
13. A composition as in claim 2 wherein the composition has a pH of 6.4 to 7.5.
14. A composition as in claim 13 wherein the travoprost is in the composition at a concentration of less than 0.006 w/v %.
15. A composition as in claim 14 wherein the surfactant is entirely Polyoxyl 40 Hydrogenated castor Oil.
16. A composition as in claim 15 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.
17. A composition as in claim 16 wherein the composition is disposed in an eye dropper.
18. A composition as in claim 17 wherein concentration of the surfactant in the composition is less than 0.15 w/v %.
19. A composition as in claim 18 wherein the composition satisfies Ph. Eur. A, Ph. Eur. B or both.
20. A composition as in claim 19 wherein the composition has a pH of 6.4 to 7.2.
21. A composition as in claim 20 wherein the surfactant is non-ionic.