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Details for Patent: 5,520,920

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Details for Patent: 5,520,920

Title: Use of certain anionic surfactants to enhance antimicrobial effectiveness of ophthalmic compositions
Abstract:Certain anionic surfactants are used to enhance antimicrobial effectiveness in comfortable, sustained release ophthalmic compositions containing polyelectrolytes, such as carboxyvinyl polymers, polystyrene sulfonic acid polymers and cationic exchange resins, as well as at least one active ingredient.
Inventor(s): Castillo; Ernesto J. (Arlington, TX), Ali; Yusuf (Fort Worth, TX)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX)
Filing Date:Aug 13, 1993
Application Number:08/106,459
Claims:1. A method of improving or enhancing the antimicrobial efficacy of an ophthalmic composition comprising a cationic antimicrobial, an anionic polyelectrolyte and an active ingredient, said method comprising adding to said composition an antimicrobial-enhancing amount of an anionic surfactant selected from the group consisting of:

a) a compound of formula: ##STR4## wherein: R.sup.1 =C.sub.4 -C.sub.27 saturated or unsaturated hydrocarbon; M=H or a pharmaceutically acceptable salt; and

n=1, 2 or 3; and

b) a compound of formula: ##STR5## wherein: R.sup.2 =C.sub.4 -C.sub.27 saturated or unsaturated hydrocarbon; M=H or a pharmaceutically acceptable salt; and

n=1, 2 or 3.

2. The method of claim 1, wherein the final composition concentration of said anionic surfactant is between about 0.005 and about 5.0 wt %.

3. The method of claim 2, wherein said anionic surfactant comprises a compound of formula I.

4. The method of claim 3, wherein the final composition concentration of said anionic surfactant is between about 0.005 and about 0.5 wt %.

5. The method of claim 4, wherein the final composition concentration of said anionic surfactant is between about 0.01 and about 0.2 wt %.

6. The method of claim 5, wherein the final composition concentration of said anionic surfactant is between about 0.03 and about 0.12 wt %.

7. The method of claim 2, wherein said anionic surfactant comprises a compound of formula II.

8. The method of claim 7, wherein the final composition concentration of said anionic surfactant is between about 0.1 and about 5.0 wt %.

9. The method of claim 8, wherein the final composition concentration of said surfactant is between about 0.1 and about 2.0 wt %.

10. The method of claim 9, wherein the final composition concentration of said surfactant is about 0.5 wt %.

11. The method of claim I wherein said surfactant is selected from the group consisting of lauroyl sarcosine, oleoyl sarcosine, myrstoyl sarcosine, cocoyl sarcosine, stearoyl sarcosine, pelargodoyl sarcosine and sodium capryl lactylate.

12. The method of claim 1, wherein said cationic antimicrobial comprises benzalkonium chloride.

13. The method of claim 1, wherein said anionic polyelectrolyte is selected from the group consisting of: carboxyvinyl polymers, polystyrene sulfonic acid polymers and finely divided cationic exchange resins.

14. The method of claim 13, wherein said anionic polyelectrolyte comprises a carboxyvinyl polymer.

15. The method of claim 13, wherein said anionic polyelectrolyte comprises a polystyrene sulfonic acid polymer of formula: ##STR6## wherein: R=H or CH.sub.3 ; and X=an integer such that the molecular weight of the polystyrene sulfonic acid polymer may vary from about 10,000 to 1.6 million.

16. The method of claim 13, wherein said anionic polyelectrolyte comprises a finely divided cationic exchange resin.
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