IP Library Granted Patent US 8,632,809
Granted Patent B2
US 8,632,809 · App. 11/936,914 · Granted Jan 21, 2014

Water insoluble polymer matrix for drug delivery

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Quick Facts
Patent No.
US 8,632,809
App. No.
11/936,914
Granted
Jan 21, 2014
Kind
B2
Abstract

Disclosed is a pharmaceutical composition comprising (a) a bioerodible water insoluble polymer matrix comprising a polyester polymer, wherein the polymer matrix has a melting point of less than 60° C. and (b) an active agent dispersed within the polymer matrix, wherein the composition is formulated to controllably release the active agent for a pre -determined period of time to a target site. Also disclosed are methods of treating a disease or condition with the disclosed compositions.

Claims (25)

1. A pharmaceutical composition comprising:

(a) a bioerodible water insoluble polymer matrix comprising a polyester polymer, wherein the polymer matrix has a melting point of less than 60° C. and wherein the polyester polymer has an average molecular weight of 400 to 4000 and wherein the polyester polymer is at least 80 wt % of the composition; and

(b) an active agent dispersed within the polymer matrix;

wherein the active agent is an ophthalmic drug and wherein the viscosity of the composition is from 100 to 2000 cps at 55° C. and wherein the composition is formulated to controllably release the active agent within a vitreous of an eye for a pre-determined period of time and wherein the composition is a liquid or paste that can be injected through a needle no larger than 22 gauge into the vitreous without requiring a physical change of the composition.

2. The pharmaceutical composition of claim 1 , wherein the composition comprises a water miscible liquid incorporated in the matrix and wherein the concentration of the water miscible liquid is up to 50% (w/w).

3. The pharmaceutical composition of claim 2 , wherein the water miscible organic liquid is miscible within the polymer matrix.

4. The pharmaceutical composition of claim 1 , wherein the polymer matrix comprises a polymer selected from the group consisting of: poly(c-caprolactone)s; poly(ethylene glycol adipate)s; poly(propylene glycol adipate)s; poly(butylene glycol adipate)s; and blends and copolymers thereof.

5. The pharmaceutical composition of claim 4 , wherein the polymer matrix comprises a poly(ε-caprolactone) polymer.

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

wherein

R 1 , R 2 and R 3 are independently selected from the group consisting of alkyl and alkoxyl diols, triols and tetraols of 2 to 8 carbon atoms;

w, w 1 are independently an integer from 4 to 12;

W 2 , w 3 are independently an integer from 1 to 12;

W 4 , w 5 , w 6 , w 7 , w 8 , w 9 and w 10 are independently an integer from 0 to 12;

n is an integer from 4 to 9; and

m is an integer from 2 to 8.

7. The pharmaceutical composition of claim 6 , wherein R 1 , R 2 and R 3 are independently selected from the group consisting of butanediol, hexanediol, neopentyl glycol, diethylene glycol, trimethylol propane and pentaerythritol.

8. The pharmaceutical composition of claim 1 , wherein the polymer matrix comprises a polymer having the formula (C 6 H 10 O 2 ) x .(C 5 H 8 O 4 ) where x is such that the polymer has an average molecular weight of about 1000.

9. The pharmaceutical composition of claim 1 , wherein the ophthalmic drug has anti-infective or anti-allergic properties.

10. The pharmaceutical composition of claim 1 , wherein the ophthalmic drug is an ocular hypotensive drug selected from the group consisting of carbonic anhydrase inhibitors; beta-blockers; prostaglandins; bradykinin agonists; rho-kinase inhibitors; C-type natriuretic peptide receptor agonists, and guanylate cyclase activators.

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

12. The pharmaceutical composition of claim 1 , wherein the polyester polymer is at least 85 wt % of the composition.

13. The pharmaceutical composition of claim 6 , wherein the polyester polymer is at least 85 wt % of the composition.

14. The pharmaceutical composition of claim 1 wherein the ophthalmic drug is for treatment of age-related macular degeneration.

15. The pharmaceutical composition of claim 13 wherein the therapeutic agent is an ophthalmic drug for treatment of age-related macular degeneration.

Assignments (2)
MERGER Recorded Jul 21, 2008
From: ALCON MANUFACTURING, LTD.
To: ALCON RESEARCH, LTD.
Reel/Frame 021266/0729 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 12, 2007
From: ASGHARIAN, BAHRAM; CHOWHAN, MASOOD A.; WAX, MARTIN B.
To: ALCON MANUFACTURING, LTD.
Reel/Frame 020232/0082 →