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Claims for Patent: 5,540,918

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Claims for Patent: 5,540,918

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. (Ft. Worth, TX)
Application Number:08/472,446
Patent Claims: 1. An ophthalmic composition having enhanced or improved antimicrobial efficacy, said composition comprising a cationic antimicrobial, an anionic polyelectrolyte, a therapeutically-effective amount of an active ingredient, and an anionic surfactant, wherein said artionic surfactant is present in an amount effective to enhance the cationic antimicrobial's effectiveness and is 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 composition of claim 1, wherein the final composition concentration of said anionic surfactant is between about 0.005 and about 5.0 wt %.

3. The composition of claim 1, wherein said anionic surfactant comprises a compound of formula I.

4. The composition of claim 3, wherein the final composition concentration of said anionic surfactant is between about 0.01 and 0.5 wt %.

5. The composition of claim 1, wherein said anionic surfactant comprises a compound of formula II.

6. The composition of claim 5, wherein the final composition concentration of said anionic surfactant is between about 0.1 and 5.0 wt %.

7. The composition of claim 1, wherein said anionic surfactant is selected from the group consisting of lauroyl sarcosine, oleoyl sarcosine, myrstoyl sarcosine, cocoyl sarcosine, stearoyl sarcosine, pelargodoyl sarcosine and sodium capryl lactylate.

8. The composition of claim 1, wherein the active ingredient comprises a beta-blocker.

9. The composition of claim 8, wherein the beta-blocker is selected from the group consisting of betaxolol and timolol.

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