Mucomimetic compositions and uses therefore

• US 20100086512A1
• Filed: 10/02/2008
• Published: 04/08/2010
• Est. Priority Date: 10/02/2008
• Status: Abandoned Application

• Current Assignee: Rolf Schaefer
• Original Assignee: Rolf Schaefer
• Inventors: Schaefer, Rolf
• Application Number:
  US12/285,350
• Publication Number:
  US 20100086512A1
• Time in Patent Office: Days
• US Class Current: 424/78.40
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents

Abstract

The present invention relates to mucomimetic and ophthalmic solutions comprising a cationic multimeric antimicrobial agent such as polyaminopropyl biguanide and a magnesium, calcium or magnesium/calcium complex of an anionic polymer such as hyaluronate, alginate, carboxymethyl cellulose, chondroitin sulfate or mixtures thereof. In specific embodiments, the solutions include additional components such as a surfactant, preferably polysorbate 20, a viscosity-modifying agent, preferably hydroxypropylmethyl cellulose, carboxymethyl cellulose or hydroxyethyl cellulose, a tonicity agent and a buffer. The solutions are biocompatible with and are highly comfortable when administered to mucous membranes, including those of the eye, as well as are effective disinfectants.

Claims

1. A mucomimetic solution comprising a cationic multimeric antimicrobial agent and a magnesium, calcium or magnesium/calcium complex of an anionic polymer.

2. The mucomimetic solution of claim 1 wherein the multimeric antimicrobial agent is polyaminopropyl biguanide or an acceptable salt thereof.

3. The mucomimetic solution of claim 1 wherein the anionic polymer is selected from the group consisting of hyaluronate, alginate, carboxymethyl cellulose, chondroitin sulfate and mixtures thereof.

4. The mucomimetic solution of claim 1 wherein the cationic multimeric antimicrobial agent is present in an amount ranging from about 0.001 to about 0.01% w/v.

5. The mucomimetic solution of claim 1 wherein the magnesium, calcium or magnesium/calcium complex of an anionic polymer is present in an amount ranging from about 0.01 to about 0.25% w/v.

6. The mucomimetic solution of claim 1 wherein the anionic polymer has a molecular weight of from about 70,000 to about 4 million Daltons.

7. The mucomimetic solution of claim 1 further including a viscosity-modifying agent selected from the group consisting of hydroxypropylmethyl cellulose, carboxymethyl cellulose and hydroxyethyl cellulose in an amount ranging from about 0.01 to about 0.2% w/v.

8. The mucomimetic solution of claim 1 further including a surfactant in an amount ranging from about 0.01 to about 1% w/v.

9. The mucomimetic solution of claim 1 further including polysorbate 20 in an amount ranging from about 0.01 to about 1% w/v.

10. The mucomimetic solution of claim 1 further including a buffer in an amount ranging from about 0.01 to about 0.25% w/v.

11. The mucomimetic solution of claim 1 further including a tonicity agent in an amount ranging from about 0.001 to about 1% w/v.

12. An ophthalmic solution comprising a cationic multimeric antimicrobial agent in an amount ranging from about 0.0001 to about 0.0005% w/v and a magnesium, calcium or magnesium/calcium complex of an anionic polymer in an amount ranging from about 0.01 to about 0.25% w/v.

13. The ophthalmic solution of claim 12 wherein the cationic multimeric antimicrobial agent is polyaminopropyl biguanide or an acceptable salt thereof.

14. The ophthalmic solution of claim 12 wherein the anionic polymer has a molecular weight of from about 70,000 to about 4 million Daltons.

15. The ophthalmic solution of claim 12 wherein the anionic polymer is selected from the group consisting of hyaluronate, alginate, carboxymethyl cellulose, chondroitin sulfate and mixtures thereof.

16. The ophthalmic solution of claim 12 further including a viscosity-modifying agent selected from the group consisting of hydroxypropylmethyl cellulose, carboxymethyl cellulose and hydroxyethyl cellulose in an amount ranging from about 0.01 to about 0.2% w/v.

17. The ophthalmic solution of claim 12 further including a surfactant in an amount ranging from about 0.01 to about 1% w/v.

18. The ophthalmic solution of claim 12 further including polysorbate 20 in an amount ranging from about 0.01 to about 1% w/v.

19. The ophthalmic solution of claim 12 further including a buffer in an amount ranging from about 0.01 to about 0.25% w/v.

20. The ophthalmic solution of claim 12 further including a tonicity agent in an amount ranging from about 0.001 to about 1% w/v.

21. An ophthalmic solution comprising polyaminopropyl biguanide in an amount ranging from about 0.0001 to about 0.0005% w/v, a magnesium, calcium or magnesium/calcium complex of an anionic polymer in an amount ranging from about 0.01 to about 0.25% w/v, a viscosity-modifying agent in an amount ranging from about 0.01 to about 0.2% w/v, polysorbate 20 in an amount ranging from about 0.01 to about 1% w/v and a tonicity agent in an amount ranging from about 0.001 to about 1% w/v.

22. The ophthalmic solution of claim 21 further including a buffer in an amount ranging from about 0.01 to about 0.25% w/v.

23. The ophthalmic solution of claim 21 wherein the anionic polymer has a molecular weight of from about 70,000 to about 4 million Daltons.

24. The ophthalmic solution of claim 21 wherein the anionic polymer is hyaluronate.

25. The ophthalmic solution of claim 21 wherein the viscosity-modifying agent is hydroxypropylmethyl cellulose and the tonicity agent is sodium chloride or a mixture of sodium chloride and potassium chloride.