Shaped ophthalmic inserts for treating dry eye syndrome

• US 4,343,787 A
• Filed: 12/28/1978
• Issued: 08/10/1982
• Est. Priority Date: 07/29/1975
• Status: Expired due to Term

• Current Assignee: Merck & Co., Inc.
• Original Assignee: Merck & Co., Inc.
• Inventors: Katz, Irving M.
• Primary Examiner(s): Robinson, Douglas W.
• Application Number:
  US05/973,975
• Time in Patent Office: 1,321 Days
• Field of Search: 424/78, 424/80, 424/180, 128/260
• US Class Current: 424/428
• CPC Class Codes: A61F 9/0017 implantable in, or in contact with, the eye, e.g. ocular inserts
• CPC Class Codes: A61K 31/715 Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• CPC Class Codes: A61K 31/74 Synthetic polymeric materials
• CPC Class Codes: A61K 31/765 Polymers containing oxygen
• CPC Class Codes: A61K 31/79 Polymers of vinyl pyrrolidone
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: Y10T 428/2982 Particulate matter [e.g., sphere, flake, etc.]

Abstract

Water soluble solid ophthalmic inserts for the treatment of dry eye in patients (human and animal), comprising a water soluble solid polymer of appropriate size.

Claims

1. A solid sterile ophthalmic insert comprising as the sole therapeutically active agent a water soluble solid polymer;

said insert having a dissolution time in lacrimal fluids of less than 24 hours and having a surface area of from about 5 to about 800 sq. mm., a length of from about 1-30 mm. and a width and height of from about 0.25 mm. to about 30 mm., said polymer being selected from the group consisting of a cellulose derivative, starch derivative, dextrose, polyalkylene glycol, polyvinylmethyl ether, polyethylene oxide, carboxyvinyl, and mixtures thereof.

2. The insert of claim 1 wherein the polymer is a cellulose derivative.

3. The insert of claim 2 wherein the polymer is a hydroxyloweralkyl cellulose, alkali carboxyloweralkyl cellulose, alkyl cellulose, and hydroxyloweralkyl-lower alkyl cellulose.

4. The insert of claim 3 wherein the polymer is hydroxypropyl cellulose.

5. The insert of claim 4 having a water content of between 1% and 40% by weight.

6. The insert of claim 1 wherein the surface area is from about 15-100 sq. mm. and the length is from about 5-20 mm. and the width and height is from about 1-5 mm.

7. The insert of claim 6 wherein the surface area is from about 5-50 sq. mm. and the length is from about 2-15 mm.

8. The insert of claim 5 wherein the water content is between 5% and 20% by weight.

9. A solid pathogen free ophthalmic insert comprising as the sole therapeutically active agent a water soluble solid polymer;

said insert having a dissolution time in lacrimal fluids of less than 24 hours and having a surface area of from about 5 to about 800 sq. mm., a length of from about 1-30 mm. and a width and height of from about 0.25 mm. to about 30 mm., said polymer being selected from the group consisting of a cellulose derivative, starch derivative, dextrose, polyalkylene glycol, polyvinylmethyl ether, polyethylene oxide, carboxyvinyl, and mixtures thereof.

10. The insert of claim 9 wherein the polymer is hydroxypropyl cellulose.

11. The insert of claim 9 having between 1-40% by weight of water.

12. The insert of claim 9 wherein the water content is between 5-20%.

13. The insert of claim 9 wherein the polymer is hydroxyloweralkyl cellulose, alkali carboxyloweralkyl cellulose, alkyl cellulose, and hydroxyloweralkyl-lower alkyl cellulose.

14. A solid sterile ophthalmic insert in the form of a rod comprising as the sole therapeutically active agent a water soluble solid polymer;

said insert having a dissolution time in lacrimal fluids of less than 24 hours and having a length of from about 2 to about 20 mm and a diameter of from about 0.5 to about 1.5 mm;

said polymer being selected from the group consisting of a cellulose derivative, starch derivative, dextrose, polyalkylene glycol, polyvinylmethyl ether, polyethylene oxide, carboxyvinyl, and mixtures thereof.

15. The insert of claim 14 wherein said polymer is hydroxypropyl cellulose.

16. The insert of claim 14 wherein said plasticizer is water.

17. The insert of claim 14 wherein the water content is between 5-20%.

18. A method of treating keratoconjunctivitis sicca comprising administering to the eye of a keratoconjunctivitis sicca patient a solid sterile ophthalmic insert consisting essentially of a water soluble solid polymer, as the sole therapeutically active agent having a surface area of from about 5 to about 800 sq. mm., a length of from about 1-30 mm. and a width and height of from about 0.25 mm. to about 30 mm., said polymer being selected from the group consisting of a cellulose derivative, natural gum, starch derivative, dextrose, polyalkylene glycol, polyvinylmethyl ether, polyethylene oxide, carboxyvinyl, xanthan gum and mixtures thereof.

19. The method of claim 18 wherein the polymer is a cellulose derivative, alginate or pectin compound.

20. The method of claim 18 wherein the polymer is a hydroxyloweralkyl cellulose, alkali carboxyloweralkyl cellulose, alkyl cellulose, and hydroxyloweralkyl-lower alkyl cellulose.

21. The method of claim 18 wherein said polymer is hydroxypropyl cellulose.

22. The method of claim 18 wherein the insert has a surface area of from about 15-100 sq. mm., the length is from about 5-20 mm. and the width and height is from about 1-5 mm.

23. The method of claim 18 wherein the surface area of said insert is from about 5-50 sq. mm. and the length is from about 2-15 mm.

24. The method of claim 18 wherein said insert is in the form a rod.

25. The method of claim 18 wherein said insert is from about 1% to 40% by weight water.

26. The method of claim 18 wherein the insert is from 5% to 20% by weight water.