# US 10,441,543 B2 · Processes for making cyclic lipid implants for intraocular use

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- Number: US 10,441,543 B2
- Document ID: US10441543B2
- Status: Granted
- Kind: B2
- Application number: 14/876,436
- Filed: 2015-10-06
- Published: 2016-01-28
- Granted: 2019-10-15
- Earliest claimed: 2006-12-19
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Lon T. Spada; James N. Chang; Michelle H. Luu
- Web page: https://patentgrep.com/patent/US10441543B2

## CPC

- A61K 9/146: {with organic macromolecular compounds}
- A61K 9/0051: {Ocular inserts or implants}
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/557: Eicosanoids, e.g. leukotrienes {or prostaglandins}
- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- 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)
- A61P 27/00: Drugs for disorders of the senses
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 27/10: for accommodation disorders, e.g. myopia
- A61P 27/12: for cataracts
- A61P 31/10: Antimycotics
- A61P 31/12: Antivirals
- A61K 9/141: {Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers ((co) spray-dried products A61K9/16, (co) lyophilised products A61K9/19; the carrier being chemically bound to the active ingredient A61K47/50)}
- 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

Biocompatible implants comprising a cyclic lipid therapeutic agent are made using a low temperature melt extrusion process. The implants are suitable for intraocular use to treat an ocular condition.

## Claims

### Claim 1

A solid intraocular implant comprising a cyclic lipid therapeutic agent, a polymer and a low melting cosolvent,
wherein the solubility parameters of the cyclic lipid therapeutic agent, the polymer and the low melting cosolvent are all within about 10 MPa1/2 of each other;
wherein the low melting cosolvent has a melt temperature of between about 50° C. and about 80° C.;
wherein the cyclic lipid therapeutic agent is selected from the group consisting of bimatoprost, latanoprost, travoprost, unoprostone, prostaglandin E1, prostaglandin E2, and mixtures thereof;
wherein the polymer is a biodegradable polymer selected from the group consisting of polylactic acid, polyglycolic acid, and polylactide-co-glycolide; and
wherein the low melting cosolvent is selected from the group consisting of decafluorobutane, poly(hexamethylene adipamide), and polyethylene glycol 3350;
wherein the cyclic lipid agent comprises 20% by weight of the intraocular implant,
wherein the potency of the cyclic lipid therapeutic agent released from the implant is at least about 50% of its maximum potency; and
wherein no polymorphs of the therapeutic agent are present in the implant.

### Claim 2 (depends on 1)

The intraocular implant of claim 1, wherein the cyclic lipid therapeutic agent is bimatoprost.

### Claim 3 (depends on 1)

The intraocular implant of claim 1, wherein the cyclic lipid therapeutic agent is latanoprost.

### Claim 4 (depends on 1)

The intraocular implant of claim 1, wherein the cyclic lipid agent is travoprost.

### Claim 5 (depends on 2)

The intraocular implant of claim 2, wherein the low melting cosolvent is polyethylene glycol 3350.

### Claim 6 (depends on 1)

The intraocular implant of claim 1, wherein the implant is monolithic.