# US 11,077,103 B2 · Naloxegol oxalate and solid dispersion thereof

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- Number: US 11,077,103 B2
- Document ID: US11077103B2
- Status: Granted
- Kind: B2
- Application number: 16/462,856
- Filed: 2017-11-22
- Published: 2020-08-13
- Granted: 2021-08-03
- Earliest claimed: 2016-11-23
- Assignees: Aurobindo Pharma Ltd
- Applicants: Aurobindo Pharma Limited; Rama Shankar; Nimesh Chandra Misra; Siva Rama Kasibabu Velegula; Suresh Chapala; Sivakumaran Meenakshisunderam
- Inventors: Rama Shankar; Nimesh Chandra Misra; Siva Rama Kasibabu Velegula; Suresh Chapala; Sivakumaran Meenakshisunderam
- Web page: https://patentgrep.com/patent/US11077103B2

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 9/146: {with organic macromolecular compounds}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 31/765: Polymers containing oxygen
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- C07D 489/08: Oxygen atom
- C08G 65/33306: {acyclic}
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS

## Abstract

The present invention relates to solid dispersion of Naloxegol oxalate. Further, the present invention relates to an improved process for Naloxegol oxalate and intermediates thereof.

## Claims

### Claim 1

A solid dispersion of stable amorphous Naloxegol oxalate in a combination with Povidone K-30 in 1:1 w/w ratio and characterized by XRPD pattern of FIG. 1.

### Claim 2 (depends on 1)

The solid dispersion as claimed in claim 1, wherein the amorphous solid dispersion having purity of about 99.5% by HPLC and broad diffraction (halo) in XRPD.

### Claim 3

A process for the preparation solid dispersion of amorphous Naloxegol oxalate, which comprises:
a) providing a solution of Naloxegol oxalate in water;
b) adding Povidone K-30 in % w/w ratio 1:1; and
c) lyophilizing the step b) and isolating stable amorphous solid dispersion of Naloxegol oxalate.

### Claim 4 (depends on 3)

The process as claimed in claim 3, wherein the amorphous solid dispersion is characterized by XRPD pattern by FIG. 1.

### Claim 5 (depends on 3)

The process as claimed in claim 3, wherein the amorphous solid dispersion has impurity content of 0.04% of 3-O-MEM α-naloxegol, 0.05% PEG-5 naloxol, 0.06% oxidative dimer.