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Claims for Patent: 5,461,081

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Claims for Patent: 5,461,081

Title: Topical ophthalmic pharmaceutical vehicles
Abstract:Universal ophthalmic pharmaceutical vehicles which increase in viscosity upon instillation in the eye are disclosed. Ophthalmic compositions of the universal vehicle and a pharmaceutically active drug are also disclosed. In one embodiment, the vehicle gels upon instillation in the eye. In another embodiment, suspension vehicles having superior physical stability are provided.
Inventor(s): Ali; Yusuf (Forth Worth, TX), Reed; Kenneth W. (Lawrenceville, GA)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX)
Application Number:08/178,941
Patent Claims: 1. A topical ophthalmic vehicle comprising: a negatively charged, water soluble polymer selected from the group consisting of carboxy vinyl polymers, sodium carboxy methylcellulose, pectin, gelatin (Type B), sodium hyaluronate, acacia, calcium carboxy methylcellulose, sodium alginate and polystyrene sulfonic acid; and a positively charged electrolyte selected from the group consisting of Na.sup.+, K.sup.+, Mn.sup.++, Ca.sup.++, Mg.sup.++, Fe.sup.++, Fe.sup.+++, Al.sup.+++, Li.sup.+, Zn.sup.++, Be.sup.++, lysine.smallcircle.HCl, arginine.smallcircle.HCl and histadine.smallcircle.HCl; and wherein the concentrations of the polymer and the electrolyte are such that the vehicle is administrable as a drop and increases in viscosity upon instillation in the eye as a result of the migration of the positively charged electrolyte out of the vehicle.

2. The vehicle of claim 1 wherein the polymer concentration is from about 0.1 to about 10 wt. %.

3. The vehicle of claim 2 wherein the polymer concentration is from about 0.1 to about 3 wt %.

4. The vehicle of claim 1 wherein the electrolyte concentration is from about 0.01 to about 1 wt %.

5. The vehicle of claim 1 wherein the polymer is a carboxy vinyl polymer.

6. The vehicle of claim 5 wherein the polymer is Carbopol.RTM. carboxy vinyl polymer.

7. The vehicle of claim 1 wherein the electrolyte is selected from the group consisting of Na.sup.+, Ca.sup.++, and Al.sup.+++.

8. The vehicle of claim 1 wherein the increase in viscosity upon instillation transforms the vehicle into a gel.

9. A pharmaceutical suspension composition which remains at least about 95% flocculated after standing for six months which comprises: a pharmaceutically active, water-insoluble drug and a suspension vehicle, wherein the suspension vehicle comprises a negatively charged, water soluble polymer selected from the group consisting of carboxy vinyl polymers, sodium carboxy methylcellulose, pectin, gelatin (Type B), sodium hyaluronate, acacia, calcium carboxy methylcellulose, sodium alginate and polystyrene sulfonic acid; and a positively charged electrolyte selected from the group consisting of Na.sup.+, K.sup.+, Mn.sup.++, Ca.sup.++, Mg.sup.++, Fe.sup.++, Fe.sup.+++, Al.sup.+++, Li.sup.+, Zn.sup.++, Be.sup.++, lysine.smallcircle.HCl, arginine.smallcircle.HCl and histadine.smallcircle.HCl; and wherein the concentrations of the polymer and the electrolyte are such that the vehicle is administrable as a drop and increases in viscosity upon instillation in the eye as a result of the migration of the positively charged electrolyte out of the vehicle.

10. The suspension composition of claim 9 wherein the polymer is Carbopol.RTM. and the electrolyte is selected from the group consisting of Na.sup.+, Ca.sup.++, and Al.sup.+++, and wherein the amount of Carbopol.RTM. is from about 0.1 to about 3 wt % and the amount of electrolyte is from about 0.01 to about 1 wt %.

11. A topical ophthalmic vehicle administrable as a drop which increases in viscosity upon instillation in the eye comprising:

a water soluble Carbopol.RTM. carboxy vinyl polymer and an electrolyte selected from the group consisting of Na.sup.+, Ca.sup.++, and Al.sup.+++, wherein the amount of Carbopol.RTM. is from about 0.1 to about 3 wt % and the amount of electrolyte is from about 0.01 to about 1 wt %.

12. A topical ophthalmic vehicle administrable as a drop which increases in viscosity upon instillation in the eye comprising:

a positively charged, water soluble polymer selected from the group consisting of gelatin (Type A) and polyvinyl amine; and a negatively charged electrolyte selected from the group consisting of PO.sub.4.sup.-3, HPO.sub.4.sup.-2, H.sub.2 PO.sub.4.sup.-, I.sup.-, Cl.sup.-, F.sup.-, SO.sub.4.sup.-2, HCO.sub.3.

13. The vehicle of claim 12 wherein the polymer concentration is from about 0.1 to about 10 wt. %.

14. The vehicle of claim 13 wherein the polymer concentration is from about 0.1 to about 3 wt %.

15. The vehicle of claim 12 wherein the electrolyte concentration is from about 0.01 to about 1 wt %.

16. The vehicle of claim 12 wherein the increase in viscosity upon instillation transforms the vehicle into a gel.

17. A method delivering a drug to the eye which comprises:

topically administering a composition comprising a charged, water soluble polymer and an oppositely charged electrolyte at concentrations such that the composition is administrable as a drop and gels upon instillation as a result of the migration of the electrolyte out of the composition.

18. The method of claim 17 wherein the polymer is carboxy vinyl polymer and the electrolyte is selected from the group consisting of Na.sup.+, CA.sup.++, and Al.sup.+++.

19. The method of claim 18 wherein the polymer is Carbopol.RTM. carboxy vinyl polymer.
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