OCULAR INSERT

• US 3,630,200 A
• Filed: 06/09/1969
• Issued: 12/28/1971
• Est. Priority Date: 06/09/1969
• Status: Expired due to Term

• Current Assignee: Higuchi Takeru
• Original Assignee: Higuchi Takeru
• Inventors: HIGUCHI TAKERU
• Application Number:
  US04/831,481
• Time in Patent Office: 932 Days
• US Class Current: 424/427
• CPC Class Codes: A61F 9/0017 implantable in, or in contact with, the eye, e.g. ocular inserts
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants

Abstract

Drug dispensing ocular insert for insertion into the cul-de-sac of the conjunctiva between the sclera of the eyeball and the lid to dispense drug to the eye over a prolonged period of time is rendered more compatible with the eye and surrounding tissues by fabricating the insert of an inner core containing the drug and a soft hydrophilic outer layer.

Claims

1. In a drug dispensing ocular insert comprising a flexible body containing a drug and adapted for insertion into the cul-de-sac of the conjunctiva between the sclera of the eyeball and the lid to dispense said drug to the eye over a prolonged period of time, the improvement for rendering the ocular insert more compatible with the eye and the surrounding tissues comprising (1) an inner core comprised of a hydrophobic polymer, said inner core containing the drug and permeable to passage of the drug and (2) a soft flexible hydrophilic outer layer insoluble in tear liquid, compatible with the eye and surrounding tissue and permeable to passage of the drug.

2. The ocular insert of claim 1 wherein said inner core is porous to permit passage of gases and liquids therethrough.

3. The ocular insert of claim 1 wherein said inner core is a matrix of a hydrophobic polymer permeable to passage of the drug, to meter the passage of drug from the inner core to and through the hydrophilic outer layer.

4. The ocular insert of claim 3 wherein said hydrophilic outer layer is a hydrophilic hydrogel.

5. The ocular insert of claim 3 wherein said hydrophilic outer layer is a hydrophilic hydrogel of a polymer of an ester of acrylic acid or methacrylic acid.

6. The ocular insert of claim 1 wherein said inner core is comprised of a plurality of drug-containing particles.

7. The ocular insert of claim 1 wherein said inner core is a capsule of a hydrophobic polymer, having the drug in the interior chamber thereof, the walls of said capsule being permeable to passage of the drug, to meter the flow of drug from said interior chamber to and through the hydrophilic outer layer.

8. The ocular insert of claim 7 wherein said hydrophilic outer layer is a hydrophilic hydrogel.

9. The ocular insert of claim 7 wherein said hydrophilic outer layer is a hydrophilic hydrogel of a polymer of an ester of acrylic or methacrylic acid.

10. The ocular insert of claim 1 wherein said hydrophilic outer layer is comprised of a polymer selected from the group consisting of hydrophilic hydrogel of an ester of acrylic or methacrylic acid, modified collagen, cross linked hydrophilic polyether gel, cross linked polyvinyl alcohol, cross linked partially hydrolyzed polyvinyl acetate and cellulosic gel.

11. The ocular insert of claim 1 wherein said drug is an ophthalmic drug.

12. The ocular insert of claim 1 wherein said drug is a systematically active drug which will pass through the eye to the bloodstream and produce a pharmacologic response at a site remote from the eye.

13. The ocUlar insert of claim 1 wherein said drug is a systemically active drug which will pass through the tissue surrounding the eye to the bloodstream and produce a pharmacologic response at a site remote from the eye.

14. The ocular insert of claim 1 wherein from 1 microgram to 1 milligram of drug is incorporated in said tablet.

15. The ocular insert of claim 1 wherein same ranges from 4 to 20 millimeters in length, 1 to 12 millimeters in width, and 0.1 to 1 millimeter in thickness.

16. In a drug dispensing ocular insert comprising a flexible body containing a drug and adapted for insertion into the cul-de-sac of the conjunctiva between the sclera of the eyeball and the lid to dispense said drug to the eye over a prolonged period of time, the improvement for rendering the ocular insert more compatible with the eye and the surrounding tissues comprising (1) an inner core containing the drug and having an affinity therefor, and said inner core being comprised of material permeable to passage of the drug, which material is independently selected to provide the desired drug release rate, and (2) a soft flexible hydrophilic outer layer insoluble in tear liquid, said outer layer also being permeable to passage of the drug and being independently selected for its eye and tissue compatibility, but providing no significant barrier to flow or passage of the drug from the said inner core (1) to the eye and surrounding tissue, whereby there is no compromise in selection of material for the inner core (1) having the desired release rate for the drug therein by reason of the soft and flexible, eye and surrounding tissue compatible outer layer (2).

17. The ocular insert of claim 16 wherein said inner core is comprised of a polymer selected from the group consisting of plasticized or unplasticized polyvinyl chloride, plasticized nylon, unplasticized soft nylon, silicone rubber, polyethylene, hydrophilic hydrogel of an ester of acrylic or methacrylic acid, modified collagen, cross linked hydrophilic polyether gel, cross linked polyvinyl alcohol, cross linked partially hydrolyzed polyvinyl acetate, cellulosic gel, ion-exchange resin and plasticized polyethylene terephthalate.

18. The ocular insert of claim 17 wherein the drug is chloramphenicol and the polymeric material of the inner core is polyethylene terephthalate.

19. The ocular insert of claim 17 wherein the drug is promethazine trichloroacetate and the polymeric material of the inner core is polyvinyl chloride.

20. The ocular insert of claim 17 wherein the drug is chloramphenicol and the polymeric material of the inner core is polydimethylsiloxane rubber.

21. The ocular insert of claim 17 wherein the drug is a member selected from the group consisting of pilocarpine and pilocarpine perfluorobutyrate and the polymeric material of the inner core is polyvinyl chloride.

22. The ocular insert of claim 17 wherein the drug is dexamethasone and the polymeric material of the inner core is nylon-66.