# US 2019/0167801 A1 · Injectable, Non-Aqueous Suspension with High Concentration of Therapeutic Agent

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- Number: US 2019/0167801 A1
- Document ID: US20190167801A1
- Status: Published application
- Kind: A1
- Application number: 16/174,101
- Filed: 2018-10-29
- Published: 2019-06-06
- Earliest claimed: 2007-01-26
- Assignees: Durect Corporation
- Applicants: Durect Corporation
- Inventors: Paul R. Houston; Guohua Chen; Andrew Sheung-King Luk
- Web page: https://patentgrep.com/patent/US20190167801A1

## CPC

- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/10: Dispersions; Emulsions
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 38/385: {Serum albumin}
- A61K 38/47: acting on glycosyl compounds (3.2), e.g. cellulases, lactases
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- 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 47/34: 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 35/00: Antineoplastic agents
- C07K 16/244: {Interleukins [IL]}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/31: multispecific
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- C12Y 302/01017: Lysozyme (3.2.1.17)
- 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
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- C12Y: ENZYMES

## Abstract

An injectable, nonaqueous suspension including at least one therapeutic agent suspended in a single component vehicle. The single component vehicle is a single amphiphilic material, such as a polyethoxylated castor oil or derivative thereof, a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene stearate, a block copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide, a block copolymer of polypropylene oxide-polyethylene oxide-polypropylene oxide, a tetra-functional block copolymer of polyethylene oxide-polypropylene oxide, or a tetra-functional block copolymer of polypropylene oxide-polyethylene oxide. A dosage kit that includes the injectable, nonaqueous suspension and a method of administering the injectable, nonaqueous suspension are also disclosed.

## Claims

### Claim 1

An injectable, nonaqueous suspension comprising at least one therapeutic agent suspended in a single component vehicle having an amphiphilic material.

### Claim 2 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the single component vehicle comprises a polyethoxylated castor oil or derivative thereof, a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene stearate, a block copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide, a block copolymer of polypropylene oxide-polyethylene oxide-polypropylene oxide, a tetra-functional block copolymer of polyethylene oxide-polypropylene oxide, or a tetra-functional block copolymer of polypropylene oxide-polyethylene oxide.

### Claim 3 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the single component vehicle comprises a reaction product of castor oil with ethylene oxide in a molar ratio of 1 to 35 or a reaction product of castor oil with ethylene oxide in a molar ratio of 1 to 45.

### Claim 4 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the at least one therapeutic agent comprises a small molecule, protein, antibody, mimetibody, monoclonal antibody, antibody fragment, peptide, nucleotide, DNA fragment, RNA fragment, plasmid fragment, nucleotide fragment, or mixtures thereof.

### Claim 5 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the at least one therapeutic agent is present at a concentration that ranges from greater than or equal to approximately 50 mg/nil to approximately 500 mg/ml.

### Claim 6 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the at least one therapeutic agent comprises from approximately 5% by weight of a total weight of the injectable, nonaqueous suspension to approximately 50% by weight of the total weight of the injectable, nonaqueous suspension.

### Claim 7 (depends on 1)

The injectable, nonaqueous suspension of claim 1, further comprising at least one antioxidant.

### Claim 8 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the suspension has an injection force that is less than or equal to about 50 lbf.

### Claim 9 (depends on 1)

The injectable, nonaqueous suspension of claim 1, wherein the single component vehicle comprises a polyethoxylated castor oil or derivative thereof and the at least one therapeutic agent comprises a monoclonal antibody.

### Claim 10

A dosage kit comprising a syringe and an injectable, nonaqueous suspension, the injectable, nonaqueous suspension comprising at least one therapeutic agent suspended in a single component vehicle having an amphiphilic material.

### Claim 11 (depends on 10)

The dosage kit of claim 10, wherein the single component vehicle comprises a polyethoxylated castor oil or derivative thereof, a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene stearate, a block copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide, a block copolymer of polypropylene oxide-polyethylene oxide-polypropylene oxide, a tetra-functional block copolymer of polyethylene oxide-polypropylene oxide, or a tetra-functional block copolymer of polypropylene oxide-polyethylene oxide.

### Claim 12 (depends on 10)

The dosage kit of claim 10, wherein the at least one therapeutic agent comprises a small molecule, protein, antibody, mimetibody, monoclonal antibody, antibody fragment, peptide, nucleotide, DNA fragment, RNA fragment, plasmid fragment, nucleotide fragment, or mixtures thereof.

### Claim 13

A method of administering a therapeutic agent, comprising:
suspending at least one therapeutic agent in a single component amphiphilic vehicle to form an injectable, nonaqueous suspension; and
injecting the injectable, nonaqueous suspension into a patient in need thereof.

### Claim 14 (depends on 13)

The method of claim 13, wherein suspending at least one therapeutic agent in a single component vehicle comprises suspending the at least one therapeutic agent in a single component vehicle selected from the group consisting of a polyethoxylated castor oil or derivative thereof; a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene stearate, a block copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide, a block copolymer of polypropylene oxide-polyethylene oxide-polypropylene oxide, a tetra-functional block copolymer of polyethylene oxide-polypropylene oxide, and a tetra-functional block copolymer of polypropylene oxide-polyethylene oxide.

### Claim 15 (depends on 13)

The method of claim 13, wherein suspending at least one therapeutic agent in a single component vehicle comprises suspending the at least one therapeutic agent in a reaction product of castor oil with ethylene oxide in a molar ratio of 1 to 35 or in a reaction product of castor oil with ethylene oxide in a molar ratio of 1 to 45.

### Claim 16 (depends on 13)

The method of claim 13, wherein suspending at least one therapeutic agent in a single component vehicle comprises suspending a small molecule, protein, antibody, mimetibody, monoclonal antibody, antibody fragment, peptide, nucleotide, DNA fragment, RNA fragment, plasmid fragment, nucleotide fragment, or mixtures thereof in the single component vehicle.

### Claim 17 (depends on 13)

The method of claim 13, wherein the at least one therapeutic agent is present at a concentration that ranges from greater than or equal to approximately 50 mg/nil to approximately 500 mg/ml.

### Claim 18 (depends on 13)

The method of claim 13, wherein the at least one therapeutic agent comprises from approximately 5% by weight of a total weight of the injectable, nonaqueous suspension to approximately 50% by weight of the total weight of the injectable, nonaqueous suspension.

### Claim 19 (depends on 13)

The method of claim 13, further comprising adding at least one antioxidant to the injectable, nonaqueous suspension.

### Claim 20 (depends on 13)

The method of claim 13, wherein the single component amphiphilic vehicle comprises a polyethoxylated castor oil or derivative thereof and the at least one therapeutic agent comprises a monoclonal antibody.