Fulvestrant formulations and methods of their use

Patent metadata

Field	Value
Publication number	US-12370199-B2
Application number	US-202117379534-A
Country	US
Kind code	B2
Filing date	Jul 19, 2021
Priority date	May 6, 2016
Publication date	Jul 29, 2025
Grant date	Jul 29, 2025

Abstract

The disclosure is directed to fulvestrant formulations including suspensions of fulvestrant particles suitable for injection. The formulations can comprise fulvestrant particles having an LD Dv(10) less than about 3 microns, for example, between about 1 micron to about 3 microns, an LD Dv(50) less than about 35 microns, for example, between about 2 microns and about 35 microns, and an LD Dv(90) less than about 120 microns, for example, between about 4 microns and about 120 microns. The formulations can comprise fulvestrant particles having a CE Dv(90) less than about 200 microns, for example, between about 10 microns and about 200 microns, a CE Dv(50) less than about 60 microns, for example, between about 5 microns and about 60 microns, and a CE Dv(10) less than about 25 microns, for example, between about 1 microns and about 25 microns.

First claim

What is claimed is:

1. A method of forming an aqueous fulvestrant suspension comprising:
mixing an aqueous medium and at least one stabilizer to form a suspension vehicle, the at least one stabilizer comprising:
a surfactant and
a polyvinylpyrrolidone, polyethylene glycol with an average molecular weight of about 3350 g/mol, a carboxymethylcellulose sodium, a non-electrolyte, or a combination thereof;

adding an amount of fulvestrant to the suspension vehicle; and
dispersing the fulvestrant in the suspension vehicle to form an aqueous fulvestrant suspension;
wherein the aqueous fulvestrant suspension comprises fulvestrant particles having one or more of:
a laser diffraction determined (LD) Dv(10) from about 1 micron to about 3 microns;
an LD Dv(50) from about 2 microns to about 35 microns; and
an LD Dv(90) from about 4 microns to about 120 microns;

and having one or more of:
a microscopy image capture determined (CE) Dv(90) from about 10 microns and about 200 microns;
a CE Dv(50) from about 5 microns to about 60 microns; and
CE Dv(10) from about 1 microns to about 25 microns.

2. The method of claim 1 , further comprising high pressure homogenizing the aqueous fulvestrant suspension.

3. The method of claim 2 , wherein the high pressure homogenization is performed at a pressure of about 15,000 psi to about 45,000 psi.

4. The method of claim 2 , further comprising adding an electrolyte to the homogenized aqueous fulvestrant suspension and mixing the electrolyte into the suspension.

5. The method of claim 2 , further comprising adding another non-electrolyte to the homogenized aqueous fulvestrant suspension and mixing the other non-electrolyte into the suspension.

Assignees

• Eagle Pharmaceuticals Inc

Inventors

• Chen Feng-Jing
• Krill Steven L
• Shmeis Rama Abu

Classifications

• A61K47/26

  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 · CPC title

• A61K9/14

  Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)} · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K9/10 Primary

  Dispersions; Emulsions · CPC title