# US 10,307,432 B2 · Stabilized liquid fosaprepitant formulations

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- Number: US 10,307,432 B2
- Document ID: US10307432B2
- Status: Granted
- Kind: B2
- Application number: 15/886,247
- Filed: 2018-02-01
- Published: 2018-06-07
- Granted: 2019-06-04
- Earliest claimed: 2015-11-03
- Assignees: Cipla Limited
- Applicants: Cipla Limited
- Inventors: Geena Malhotra; Sarabjit Singh; Abhijit Jadhav
- Web page: https://patentgrep.com/patent/US10307432B2

## CPC

- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- 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 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- 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)

## Abstract

The present invention relates to stable pharmaceutical compositions of fosaprepitant or a salt thereof in the form of ready-to-use or ready-to-dilute compositions suitable for parenteral administration.

## Claims

### Claim 1

A liquid composition comprising:
fosaprepitant or a salt thereof, an aqueous albumin vehicle, and at least one stabilizer selected from fatty acid metal salts, antioxidants, and chelating agents,
wherein after storage at 2-8° C. for at least 1 month, aprepitant is present in an amount concentration of no more than 10%.

### Claim 2 (depends on 1)

The liquid composition according to claim 1, comprising a chelating agent selected from the group consisting of ethylenediaminetetraacetic acid, hydroxyethylethylenediaminetriacetic acid, diethylenetriaminepentaacetic acid, nitrilotriacetic acid, ethanol diglycine, 1,3-propylenediaminetetraacetic acid, or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 2)

The liquid composition according to claim 2, wherein the chelating agent comprises ethylenediaminetetraacetic acid or pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The liquid composition according to claim 1, wherein the aqueous albumin vehicle comprises a 25% aqueous albumin vehicle.

### Claim 5 (depends on 1)

The liquid composition according to claim 1, wherein the fosaprepitant is fosaprepitant dimeglumine.

### Claim 6 (depends on 1)

The liquid composition according to claim 1, further comprising an additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).

### Claim 7 (depends on 6)

The liquid composition according to claim 6, wherein the additional agent comprises a corticosteroid, a 5HT3 receptor antagonist, GABAB receptor agonist, or a combination thereof.

### Claim 8 (depends on 7)

The liquid composition according to claim 7, wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, or baclofen.

### Claim 9 (depends on 1)

A method of treating chemotherapy-induced nausea and vomiting (CINV), wherein the method comprises administering a liquid pharmaceutical composition according to claim 1.

### Claim 10 (depends on 9)

The method according to claim 9, comprising administering at least one additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).

### Claim 11 (depends on 10)

The method according to claim 10, wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, baclofen, or a combination thereof.

### Claim 12

A liquid composition comprising fosaprepitant or a salt thereof, a solubilizer comprising at least one alcohol, at least one glycol, or a combination thereof, wherein after storage at 2-8° C. for at least 1 month, aprepitant is present in an amount concentration of no more than 10%, wherein the composition is ready-to-use or ready-to-dilute.

### Claim 13 (depends on 12)

The liquid composition according to claim 12, wherein the alcohol comprises ethanol, octanol, glycofurol or a mixture thereof.

### Claim 14 (depends on 12)

The liquid composition according to claim 12, comprising a glycol comprising propylene glycol, glycerol, polyethylene glycol, or a mixture thereof.

### Claim 15 (depends on 12)

The liquid composition according to claim 12, comprising ethanol and propylene glycol.

### Claim 16 (depends on 12)

The liquid composition according to claim 12, further comprising an additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).

### Claim 17 (depends on 12)

The liquid composition according to claim 12, wherein the additional agent comprises a corticosteroid, a 5HT3 receptor antagonist, GABAB receptor agonist, or a combination thereof.

### Claim 18 (depends on 12)

The liquid composition according to claim 12, wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, or baclofen.

### Claim 19 (depends on 12)

A method of treating chemotherapy-induced nausea and vomiting (CINV), wherein the method comprises administering a liquid pharmaceutical composition according to claim 12.

### Claim 20 (depends on 19)

The method according to claim 19, comprising administering at least one additional agent for the treatment of chemotherapy-induced nausea and vomiting (CINV).

### Claim 21 (depends on 20)

The method according to claim 20, wherein the additional agent comprises dexamethasone, triamcinolone, flunisolide, budesonide, palonosetron, ondansetron, granisetron, tropisetron, decadron, zatisetron, baclofen, or a combination thereof.
