Use of certain anionic surfactants to enhance antimicrobial effectiveness of ophthalmic compositions

• US 5,520,920 A
• Filed: 08/13/1993
• Issued: 05/28/1996
• Est. Priority Date: 08/28/1992
• Status: Expired due to Term

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Laboratories Incorporated (Alcon Incorporated)
• Inventors: Castillo, Ernesto J., Ali, Yusuf
• Primary Examiner(s): AZPURU, CARLOS A
• Application Number:
  US08/106,459
• Time in Patent Office: 1,019 Days
• Field of Search: 424/427, 424/428, 424/78.04, 424/405, 514/912, 514/975
• US Class Current: 424/405
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/183 Amino acids, e.g. glycine, EDTA or aspartame
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 31/04 Antibacterial agents

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.

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;

R¹ =C₄ -C₂₇ 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;

R² =C₄ -C₂₇ 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 %.

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 CH₃ ; 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.

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.