Ophthalmic composition

• US 9,770,447 B2
• Filed: 07/12/2016
• Issued: 09/26/2017
• Est. Priority Date: 06/24/2014
• Status: Active Grant

• Current Assignee: Sydnexis, Inc.
• Original Assignee: Sydnexis, Inc.
• Inventors: Ostrow, Gregory I., Widder, Kenneth J., Baker, David S.
• Primary Examiner(s): FAY, ZOHREH A
• Application Number:
  US15/208,537
• Publication Number:
  US 20160339007A1
• Time in Patent Office: 441 Days
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Provided herein is an ophthalmic composition. In some embodiments, the ophthalmic composition includes a low concentration of an ophthalmic agent for treatment of an ophthalmic disorder or condition; and an ophthalmically acceptable carrier, wherein the ophthalmic agent is distributed with substantial uniformity throughout the ophthalmically acceptable carrier. Further disclosed herein include an ophthalmic composition including a low concentration of an ophthalmic agent and deuterated water. Also disclosed herein are methods of arresting or preventing myopia development by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.

Claims

1. An ophthalmic composition, comprising one and no more than one ophthalmic agent, and deuterated water, at a pD of from about 4.2 to about 7.9, wherein the ophthalmic agent consists of atropine, atropine sulfate, or a combination thereof, at a concentration of from about 0.001 wt % to about 0.03 wt %.

2. The ophthalmic composition of claim 1, wherein the ophthalmic composition has a pD of one of:

less than about 7.3, less than about 7.2, less than about 7.1, less than about 7, less than about 6.8, less than about 6.5, less than about 6.4, less than about 6.3, less than about 6.2, less than about 6.1, less than about 6, less than about 5.9, less than about 5.8, less than about 5.2, or less than about 4.8 after extended period of time under storage condition.

3. The ophthalmic composition of claim 1, wherein the muscarinic antagonist is present in the composition at a concentration of one of:

from about 0.001 wt % to about 0.025 wt %, from about 0.001 wt % to about 0.02 wt %, from about 0.001 wt % to about 0.01 wt %, from about 0.001 wt % to about 0.008 wt %, or from about 0.001 wt % to about 0.005 wt %.

4. The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises an osmolarity adjusting agent.

5. The ophthalmic composition of claim 4, wherein the osmolarity adjusting agent is sodium chloride.

6. The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises a preservative.

7. The ophthalmic composition of claim 6, wherein the preservative is selected from benzalkonium chloride, cetrimonium, sodium perborate, stabilized oxychloro complex, SofZia, polyquaternium-1, chlorobutanol, edetate disodium, polyhexamethylene biguanide, or combinations thereof.

8. The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises a buffer agent.

9. The ophthalmic composition of claim 8, wherein the buffer agent is selected from borates, borate-polyol complexes, phosphate buffering agents, citrate buffering agents, acetate buffering agents, carbonate buffering agents, organic buffering agents, amino acid buffering agents, or combinations thereof.

10. The ophthalmic composition of claim 1, wherein the ophthalmic composition further comprises a pD adjusting agent.

11. The ophthalmic composition of claim 10, wherein the pD adjusting agent comprises deuterated hydrochloric acid, deuterated sodium hydroxide, deuterated acetic acid, or deuterated citric acid.

12. The ophthalmic composition of claim 1, wherein the ophthalmic composition comprises one of:

less than 5% of H₂O, less than 4% of H₂O, less than 3% of H₂O, less than 2% of H₂O, less than 1% of H₂O, less than 0.5% of H₂O, less than 0.1% of H₂O, or 0% of H₂O.

13. The ophthalmic composition of claim 1, wherein the ophthalmic composition is not formulated as an injectable formulation.

14. An ophthalmic solution, comprising one and no more than one ophthalmic agent, and deuterated water, at a pD of from about 4.2 to about 7.9, wherein the ophthalmic agent consists of atropine, atropine sulfate, or a combination thereof, at a concentration of from about 0.001 wt % to about 0.03 wt %.

15. The ophthalmic solution of claim 14, wherein the ophthalmic solution has a pD of one of:

less than about 7.3, less than about 7.2, less than about 7.1, less than about 7, less than about 6.8, less than about 6.5, less than about 6.4, less than about 6.3, less than about 6.2, less than about 6.1, less than about 6, less than about 5.9, less than about 5.8, less than about 5.2, or less than about 4.8 after extended period of time under storage condition.

16. The ophthalmic solution of claim 14, wherein the ophthalmic solution comprises one of:

less than 5% of H₂O, less than 4% of H₂O, less than 3% of H₂O, less than 2% of H₂O, less than 1% of H₂O, less than 0.5% of H₂O, less than 0.1% of H₂O, or 0% of H₂O.

17. A method of arresting myopia progression, comprising administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition comprising one and no more than one ophthalmic agent, and deuterated water, at a pD of from about 4.2 to about 7.9, wherein the ophthalmic agent consists of atropine, atropine sulfate, or a combination thereof, at a concentration of from about 0.001 wt % to about 0.03 wt %.

18. The method of claim 17, wherein the ophthalmic composition is stored at between about 2°

C. to about 10°

C. prior to first use.

19. The method of claim 17, wherein the ophthalmic composition is stored at between about 16°

C. to about 26°

C. after first use.