# US 2021/0275501 A1 · Ocular formulations for drug-delivery and protection of the anterior segment of the eye

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- Number: US 2021/0275501 A1
- Document ID: US20210275501A1
- Status: Published application
- Kind: A1
- Application number: 17/068,954
- Filed: 2020-10-13
- Published: 2021-09-09
- Earliest claimed: 2014-09-17
- Assignees: PanOptica, Inc.
- Applicants: PanOptica, Inc.
- Inventors: David P. BINGAMAN; Paul G. CHANEY; Martin B. WAX
- Web page: https://patentgrep.com/patent/US20210275501A1

## CPC

- A61K 31/425: Thiazoles
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/10: Dispersions; Emulsions
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/427: not condensed and containing further heterocyclic rings
- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- 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
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present application relates to topical formulations comprising Compound-I or its free base, and a second active agent selected from nicotinic acid, nicotinamide, and vitamin K, and a combination thereof, for treating ocular neovascularization. The present application also relates to pharmaceutical compositions comprising particles of Compound-I or its free base, and suspension formulations comprising the particle compositions of Compound-I or its free base.

## Claims

### Claim 1

A topical, ocular, suspension formulation, comprising:
a. particles of a first active agent of Formula II:
or a pharmaceutically acceptable salt thereof; and
b. one or more pharmaceutically acceptable excipients selected from hydroxy propyl methyl cellulose (HPMC), carboxylmethyl cellulose and salts thereof, and hydroxyl ethyl cellulose (HEC);
wherein the first active agent or the pharmaceutically acceptable salt thereof is present in about 0.1% to about 2.0% (w/v), and the particles have a mean diameter of between 100 nm and 100 μm.

### Claim 2 (depends on 1)

The formulation of claim 1, wherein the first active agent is Compound-I:

### Claim 3 (depends on 1)

The formulation of claim 1, further comprising a second active agent, or a pharmaceutically acceptable salt thereof, wherein the second active agent is nicotinic acid, nicotinamide, or vitamin K, or a combination thereof.

### Claim 4 (depends on 1)

The formulation of claim 1, wherein the particles have a mean diameter of between 30 μm and 60 μm.

### Claim 5 (depends on 1)

The formulation of claim 1, wherein the particles have a mean diameter of between 1 μm and 5 μm.

### Claim 6 (depends on 1)

The formulation of claim 1, wherein the particles have a mean diameter of about 3 μm, about 30 μm, about 35 μm, or about 50 μm.

### Claim 7 (depends on 1)

The formulation of claim 1, comprising about 0.1% to about 1.0% (w/v) of the compound of Formula II or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 1)

The formulation of claim 1, comprising about 0.2% to about 1.0% (w/v) of the compound of Formula II or a pharmaceutically acceptable salt thereof.

### Claim 9 (depends on 1)

The formulation of claim 1, comprising about 0.2%, about 0.3%, about 0.4%, about 0.5%, about 0.6%, about 0.7%, about 0.8%, about 0.9%, or about 1.0% (w/v) of the compound of Formula II or a pharmaceutically acceptable salt thereof.

### Claim 10 (depends on 3)

The formulation of claim 3, wherein the second active agent is present in an amount of less than 10 μM.

### Claim 11 (depends on 3)

The formulation of claim 3, wherein the second active agent is present in an amount of about 1 μM, about 2 μM, about 3 μM, about 4 μM, or about 5 μM.

### Claim 12 (depends on 3)

The formulation of claim 3, wherein the second active agent is present in an amount of about 1 μM.

### Claim 13 (depends on 1)

The formulation of claim 1, further comprising one or more excipients selected from a non-ionic liquid polymer and a hydrophilic non-ionic surfactant.

### Claim 14 (depends on 13)

The formulation of claim 13, wherein the non-ionic liquid polymer is of the alkyl aryl polyether alcohol type.

### Claim 15 (depends on 13)

The formulation of claim 13, wherein the hydrophilic non-ionic surfactant is poloxamer.

### Claim 16 (depends on 1)

The formulation of claim 1, further comprising one or more excipients are selected from Polysorbate (Tween) 80, Poloxamer (Pluronic) F-127, Poloxamer 407, Povidone (PVP K-29/32 or K-30), and Tyloxapol, and a combination thereof.

### Claim 17 (depends on 1)

The formulation of claim 1, further comprising a stabilizer for the second active agent.

### Claim 18 (depends on 1)

The formulation of claim 1, wherein the formulation has a pH of about 6.

### Claim 19 (depends on 1)

The formulation of claim 1, wherein the one or more pharmaceutically acceptable excipients are selected from one or more of hydroxyl propyl methyl cellulose (HPMC) and carboxylmethyl cellulose and salts thereof.

### Claim 20 (depends on 1)

The formulation of claim 1, wherein the one or more pharmaceutically acceptable excipients are selected from one or more of hydroxyl propyl methyl cellulose (HPMC) and hydroxyl ethyl cellulose (HEC).