PUNCTAL PLUG COMPRISING A WATER-INSOLUBLE POLYMERIC MATRIX

• US 20080114076A1
• Filed: 11/08/2007
• Published: 05/15/2008
• Est. Priority Date: 11/09/2006
• Status: Abandoned Application

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Manufacturing Limited (Alcon Incorporated)
• Inventors: Chowhan, Masood A., Asgharian, Bahram
• Application Number:
  US11/936,875
• Publication Number:
  US 20080114076A1
• Time in Patent Office: Days
• US Class Current: 514/772.3
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants
• CPC Class Codes: A61P 27/02 Ophthalmic agents

Abstract

Disclosed is a pharmaceutical composition comprising a water insoluble polymer matrix that comprises a bioerodable polyester polymer or a fatty acid based polyester polymer, or a mixture of both polymers, wherein the polymer matrix has a melting point of less than 60° C., and wherein the composition is liquid or paste at room temperature and is formulated to occlude a punctual channel in a subject and conforms to the shape of the canalicular or punctal channel.

Claims

1. A pharmaceutical composition comprising:

a water insoluble polymer matrix that comprises a polyester polymer or a fatty acid based polymer, or a mixture of both polymers, wherein the polymer matrix has a melting point of less than 60°

C., and

wherein the composition is liquid or paste at room temperature and is formulated to occlude a channel in a subject.

2. The pharmaceutical composition of claim 1, wherein the composition comprises up to 50% (w/w) of a water miscible organic liquid.

3. The pharmaceutical composition of claim 1, wherein the polymer matrix comprises a polyester polymer selected from the group consisting of:

poly(caprolactone)s;

poly(ethylene glycol adipate)s;

poly(propylene glycol adipate)s;

poly(butylene glycol adipate)s;

poly(hydroxybutarate)(s);

poly(hydroxyvalerate)(s); and

blends and copolymers thereof.

4. The pharmaceutical composition of claim 3, wherein the polymer matrix comprises a poly(ε

-caprolactone) polymer.

5. The pharmaceutical composition of claim 1, wherein the polymer matrix comprises a polyester polymer selected from the group consisting of:

6. The pharmaceutical composition of claim 5, wherein R₁, R₂ and R₃ are independently selected from the group consisting of butanediol, hexanediol, neopentyl glycol, diethylene glycol, trimethylol propane and pentaerythritol.

7. The pharmaceutical composition of claim 1, wherein the polymer matrix comprises a fatty acid based polymer having the following structure:

A-(B-A)_n-B-A,

wherein

A is an aliphatic hydroxycarboxylic acid ester from 6 to 60 carbon atoms;

B is a diacid dimer of unsaturated fatty acids from 8 to 40 carbon atoms; and

n is an integer from 0 to 3.

8. The pharmaceutical composition of claim 7, wherein A has the structure:

9. The pharmaceutical composition of claim 7, wherein B has the structure:

10. The pharmaceutical composition of claim 1, wherein the polymer matrix comprises a polyester polymer having an average molecular weight of 400 to 8000.

11. The pharmaceutical composition of claim 1, wherein the composition has a viscosity of 50 to 8000 cps at 55°

C.

12. The pharmaceutical composition of claim 1, wherein the polymer matrix or the composition is bioerodible.

13. The pharmaceutical composition of claim 1, wherein an active agent is dispersed within the polymer matrix.

14. A method of occluding a canalicular channel or punctal channel in a subject comprising administering the pharmaceutical composition of claim 1 into the channel.

15. The method of claim 14, wherein the pharmaceutical composition is not pre-heated prior to administering the composition into the channel.

16. The method of claim 14, wherein the pharmaceutical composition is injected into the channel with a needle.

17. A method of treating dry eye syndrome in a subject comprising administering the pharmaceutical composition of claim 1 into a canalicular or punctal channel of the subject, wherein the composition reduces drainage of tear fluid from the eye through the canalicular channel or punctal opening of the subject.

18. The method of claim 17, wherein the pharmaceutical composition conforms to the shape of the canalicular or punctal channel.

19. The method of claim 17, wherein the pharmaceutical composition is formulated into an injectable paste or liquid.

20. A kit comprising the pharmaceutical composition of claim 1 and a syringe.