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;
an amount of a prostaglandin suitable for treating glaucoma;
a polymeric quaternary ammonium compound for preserving the composition; and
a surfactant wherein the surfactant is ethoxylated and/or hydrogenated vegetable oil at a concentration in the composition of at least 0.01 w/v % but less than 0.4 w/v %, wherein:
i. the ethoxylated and/or hydrogenated vegetable oil surfactant is entirely or substantially entirely the only surfactant in the composition;
ii. the pharmaceutical vehicle includes water; and
iii. the composition is free of any benzalkonium chloride.
2. A composition as in claim 1 wherein the prostaglandin is the only therapeutic agent.
3. A composition as in claim 1 wherein the prostaglandin, the surfactant or both are non-ionic.
4. A composition as in claim 2 wherein the prostaglandin is travoprost.
5. A composition as in claim 1 wherein the ethoxylated and/or hydrogenated vegetable oil surfactant is entirely castor oil.
6. A composition as in claim 1 wherein the ethoxylated and/or hydrogenated vegetable oil surfactant is entirely Polyoxyl 40 Hydrogenated castor Oil.
7. A composition as in claim 1 wherein the surfactant is between 0.001 and 0.3 w/v % of the composition.
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 other chlorine containing preservation agents.
10. A composition as in claim 1 wherein the prostaglandin is less than 0.01 w/v % of the composition.
11. A composition as in claim 1 wherein the prostaglandin is less than 0.006 w/v % of the composition.
12. A composition as in claim 1 wherein the prostaglandin is non-ionic and/or relatively insoluble in aqueous solution.
13. A composition as in claim 1 wherein the surfactant and the prostaglandin are non-ionic.
14. An ophthalmic pharmaceutical composition, comprising:
a pharmaceutical vehicle suitable for topical application to an eye of a human;
an amount of therapeutic agent suitable for treating glaucoma wherein the therapeutic agent is a prostaglandin;
a polymeric quaternary ammonium compound for preserving the composition; and
a surfactant, the surfactant being ethoxylated and/or hydrogenated vegetable oil at a concentration in the composition of at least 0.01 w/v % but less than 0.3 w/v %, wherein:
i. the ethoxylated and/or hydrogenated vegetable oil surfactant is entirely or substantially entirely the only surfactant in the composition;
ii. the prostaglandin is travoprost;
iii. the pharmaceutical vehicle includes water; and
iv. the composition is free of any benzalkonium chloride.
15. A composition as in claim 14 wherein the composition is disposed within an eye dropper.
16. A composition as in claim 6 wherein the concentration of the surfactant is between 0.001 and 0.15 w/v %.
17. A composition as in claim 14 wherein the concentration of the surfactant is between 0.001 and 0.15 w/v %.
18. A composition as in claim 1 wherein the prostaglandin is travoprost.
19. A composition as in claim 18 wherein the ethoxylated and/or hydrogenated vegetable oil surfactant is entirely Polyoxyl 40 Hydrogenated castor Oil.
20. A composition as in claim 1 wherein the polymeric quaternary ammonium compound is polyquaternium 1.