Lapatinib particles and uses thereof

Patent metadata

Field	Value
Publication number	US-12029818-B2
Application number	US-202217812479-A
Country	US
Kind code	B2
Filing date	Jul 14, 2022
Priority date	Jul 23, 2020
Publication date	Jul 9, 2024
Grant date	Jul 9, 2024

Abstract

The disclosure provides particles of at least 95% by weight of lapatinib, or a pharmaceutically acceptable salt thereof, wherein the particles have a specific surface area (SSA) of at least 10 m2/g and have a mean particle size by volume distribution of between about 0.7 μm and about 8 μm.

First claim

We claim:

1. A composition, comprising particles comprising at least 95% by weight of lapatinib, or a pharmaceutically acceptable salt thereof, wherein the particles have a specific surface area (SSA) of at least 11 m 2 /g and have a mean particle size by volume distribution of between about 0.7 μm and about 8 μm.

2. The composition of claim 1 , wherein the particles have a SSA of at least 15 m 2 /g.

3. The composition of claim 1 , wherein the particles have a SSA of at least 18 m 2 /g.

4. The composition of claim 1 , wherein the particles have a SSA of between 12 m 2 /g and 50 m 2 /g.

5. The composition of claim 1 , wherein the particles have a mean particle size by volume distribution of between about 1 μm and about 8 μm.

6. The composition of claim 1 , wherein the particles comprise at least 98% of lapatinib, or a pharmaceutically acceptable salt thereof.

7. The composition of claim 1 , wherein the particles are uncoated and exclude polymer, protein, polyethoxylated castor oil and polyethylene glycol glycerides composed of mono-, di- and triglycerides and mono- and diesters of polyethylene glycol.

8. The composition of claim 1 , wherein the composition comprises a suspension further comprising a pharmaceutically acceptable liquid carrier.

9. The composition of claim 1 , further comprising one or more components selected from the group consisting of polysorbate, methylcellulose, polyvinylpyrrolidone, mannitol, and hydroxypropyl methylcellulose.

10. The composition of claim 1 , wherein the particles have a mean bulk density less than about 0.100 g/cm 3 , tapped or not tapped.

11. The composition of claim 1 , wherein the pharmaceutically acceptable salt of lapatinib comprises lapatinib ditosylate monohydrate.

12. The composition of claim 2 , wherein the particles have a mean bulk density between about 0.010 g/cm 3 and about 0.050 g/cm 3 , tapped or not tapped.

13. The composition of claim 12 , wherein the particles have a SSA of at least 18 m 2 /g.

14. The composition of claim 12 , wherein the particles have a SSA of between 15 m 2 /g and about 50 m 2 /g.

15. The composition of claim 14 , wherein the lapatinib or pharmaceutically acceptable salt thereof comprises lapatinib ditosylate monohydrate.

16. The composition of claim 14 , wherein the composition comprises a suspension further comprising a pharmaceutically acceptable liquid carrier.

17. The composition of claim 15 , wherein the composition comprises a suspension further comprising a pharmaceutically acceptable liquid carrier.

Assignees

• Crititech Inc

Inventors

• Sittenauer Jacob
• Farthing Joseph
• Williams Mark
• Baltezor Michael
• Dizerega Gere
• Abarca Aranza Barreda
• Clark Shelby

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

• A61K31/5365

  ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/4196

  1,2,4-Triazoles · CPC title

• A61K31/7068

  having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid · CPC title