Aqueous antimicrobial ophthalmic solutions

• US 4,525,346 A
• Filed: 09/29/1983
• Issued: 06/25/1985
• Est. Priority Date: 09/28/1981
• Status: Expired due to Term

• Current Assignee: Alcon Manufacturing Limited (Alcon Incorporated)
• Original Assignee: Alcon Laboratories Incorporated (Alcon Incorporated)
• Inventors: Stark, Raymond L.
• Primary Examiner(s): Robinson, Douglas W.
• Application Number:
  US06/537,331
• Time in Patent Office: 635 Days
• Field of Search: 424/78, 424/329, 424/80, 564/295
• US Class Current: 424/78.04
• CPC Class Codes: A61K 31/785 Polymers containing nitrogen
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61L 12/145 Polymeric quaternary ammonium compounds

Abstract

This invention relates to ophthalmic compositions which comprise quaternary ammonium salt having the formula ##STR1## wherein X=a pharmaceutically acceptable anion, such compositions providing aqueous disinfecting solutions for contact lenses as well as a preserved ocular compositions including contact lens treating solutions comfort drop solutions, preserved saline solutions, ointments and other ocular medicaments.

Claims

1. An aqueous ophthalmic contact lens solution comprising:

from about 0.00001 to about 3.0 percent by weight/volume of a quaternary ammonium compound having a number average molecular weight in the range of about 2,000 to about 30,000, said compound having the formula ##STR3## wherein X=a pharmaceutically acceptable anion;

an effective amount of NaCl to provide isotonicity to said solution; and

an effective amount of buffer to provide said solution with an ophthalmically acceptable pH.

2. An aqueous ophthalmic solution as recited in claim 1 wherein said solution further comprises a wetting agent.

3. An aqueous ophthalmic solution as recited in claim 2 wherein said solution further comprises a chelating agent and a surfactant.

4. The ophthalmic solution as recited in claims 1, 2 or 3 wherein the quaternary ammonium compound has a molecular weight in the range of from about 3,000 to about 14,000.

5. An ophthalmic solution as recited in claim 1 wherein said solution is a preserved saline solution.

6. An ophthalmic solution as recited in claim 1 wherein said solution is a preserved disinfecting solution for a soft contact lens.

7. An ophthalmic solution as recited in claim 2 wherein said solution is a preserved comfort drop solution.

8. An ophthalmic solution as recited in claim 3 wherein said solution is a cleaning solution.

9. An aqueous ophthalmic solution as recited in claim 1 wherein X=Cl^-.

10. An aqueous ophthalmic soft contact lens solution as recited in claim 1 wherein said contact lens is a soft contact lens.

11. An aqueous ophthalmic soft contact lens solution as recited in claim 1 or 10 wherein said anion is Cl^-.

12. The aqueous ophthalmic soft contact lens solution as recited in claim 1 wherein said quaternary ammonium compound has a molecular weight sufficiently large to substantially preclude adsorption, absorption or physical binding onto a soft contact lens.

13. An aqueous ophthalmic soft contact lens solution as recited in claim 12 wherein said solution further comprises a wetting agent.

14. An aqueous ophthalmic soft contact lens solution as recited in claim 12 wherein said anion is Cl^-.

15. An aqueous ophthalmic soft contact lens solution as recited in claim 13 wherein said solution further comprises a chelating agent and a surfactant.

16. An ophthalmic soft contact lens solution as recited in claims 12, 13, 14 or 15, wherein the quaternary ammonium compound has a molecular weight in the range of from about 3,000 to about 14,000.

17. An isotonic contact lens disinfecting solution comprising from about 0.001 to about 0.01 percent by weight/volume of a quaternary ammonium compound having a number average molecular weight in the range of about 2,000 to about 30,000, said quaternary ammonium compound having the formula ##STR4## wherein X=a pharmaceutically acceptable anion;

an effective amount of NaCl to provide isotonicity to said solution;

an effective amount of a buffer to provide said solution with an ophthalmically acceptable pH.

18. A contact lens disinfecting solution as recited in claim 17 wherein said quaternary ammonium compound has a molecular weight in the range of from about 3,000 to about 14,000.

19. An isotonic contact lens disinfecting solution as recited in claims 17 or 18 wherein said solution further includes ethylenediaminetetracetic acid or salts thereof and a wetting agent selected from the group consisting of polyvinyl alcohol, polyvinyl pyrrolidone, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, polyvidone and mixtures thereof.

20. An isotonic contact lens disinfecting solution as recited in claim 18 wherein X=Cl^-.

21. A method of imparting antimicrobial activity to an aqueous ophthalmic contact lens solution comprising:

adding to said solution from about 0.00001% to about 3.0% by weight/volume of a quaternary ammonium salt as an antimicrobial agent having a molecular weight in the range of about 3,000 to about 14,000, said quaternary ammonium salt having the formula ##STR5## wherein X=a pharmaceutically acceptable anion.

22. A method as recited in claim 21 wherein said antimicrobial agent preserves said solution and wherein said ammonium salt comprises from about 0.0001% to about 0.005% by weight/volume of said solution.

23. A method as recited in claim 21 wherein said antimicrobial agent comprises from about 0.001% to about 0.01% by weight/volume of said solution and wherein said solution disinfects a contact lens.

24. A method as recited in claims 21, 22 or 23 wherein the pharmaceutically acceptable anion is Cl^-.

25. A method as recited in claims 21, 22 or 23 wherein the pharmaceutically acceptable anion is Br^-.