# US 11,439,590 B2 · Pharmaceutical ophthalmic compositions for intraocular administration and methods for fabricating thereof

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- Number: US 11,439,590 B2
- Document ID: US11439590B2
- Status: Granted
- Kind: B2
- Application number: 17/084,514
- Filed: 2020-10-29
- Published: 2021-02-18
- Granted: 2022-09-13
- Earliest claimed: 2013-07-22
- Assignees: Novel Drug Solutions LLC; Pyp Car Northwest, Pa
- Applicants: Novel Drug Solutions LLC; Eye Care Northwest, Pa
- Inventors: Jeffrey T. Liegner; John Scott Karolchyk; Bernard Covalesky; Richard Dilzer; Kallan Peters
- Web page: https://patentgrep.com/patent/US11439590B2

## CPC

- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 38/12: Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)}
- A61K 38/14: Peptides containing saccharide radicals; Derivatives thereof {, e.g. bleomycin, phleomycin, muramylpeptides or vancomycin}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 47/38: Cellulose; Derivatives thereof
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Pharmaceutical ophthalmic compositions are described, the compositions consisting essentially of a therapeutically effective quantity of an anti-bacterial agent (such as moxifloxacin), a therapeutically effective quantity of an anti-inflammatory agent (such as prednisolone), a combination of at least two solubilizing and suspending agents (of which one is a non-ionic polyoxyethlene-polyoxypropylene block copolymer), and a carrier. Methods for fabricating the compositions and using them are also described.

## Claims

### Claim 1

A method for treating an ophthalmological disease, condition or pathology in a mammalian subject in need of such treatment comprising delivering to the subject by intraocular injection, an effective amount of a composition comprising:
(a) a therapeutically effective quantity of triamcinolone or a derivative thereof;
(b) a therapeutically effective quantity of moxifloxacin;
(c) a non-ionic poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) block copolymer having a molecular weight of the polyoxypropylene portion of about 4,000 Daltons and about a 70% polyoxyethylene content, with an overall molecular weight of between about 9,840 Daltons and about 14,600 Daltons, wherein the concentration of the non-ionic polyoxyethlene-polyoxypropylene block copolymer is between about 1 mass % and about 2 mass % of the pharmaceutical composition;
(d) about 1% of polysorbate 80; and
(e) a pharmaceutically acceptable carrier.

### Claim 2 (depends on 1)

The method of claim 1, wherein said composition further comprises a therapeutically effective quantity of a glycopeptide antibiotic selected from the group consisting of vancomycin, teicoplanin, telavancin, decaplanin, ramoplanin, gentamicin, tobramycin, amikacin, cefuroxime, polymyxin B sulfate, trimethoprim, and a combination thereof.

### Claim 3 (depends on 2)

The method of claim 2, wherein said antibiotic is vancomycin.

### Claim 4 (depends on 1)

The method of claim 1, wherein said pharmaceutically acceptable carrier is selected from the group consisting of sterile water, a sterile water solution of edetate calcium disodium, a sterile water solution of hydrochloric acid, and combinations thereof.

### Claim 5 (depends on 1)

The method of claim 1, wherein said intraocular injection comprises intravitreal injection.

### Claim 6 (depends on 1)

The method of claim 1, wherein said intraocular injection comprises intracameral injection.

### Claim 7 (depends on 5)

The method of claim 5, wherein the intravitreal injection is intraoperative.