Pharmaceutical compositions of lenvatinib

Patent metadata

Field	Value
Publication number	US-10583133-B2
Application number	US-201916289677-A
Country	US
Kind code	B2
Filing date	Mar 1, 2019
Priority date	Mar 12, 2018
Publication date	Mar 10, 2020
Grant date	Mar 10, 2020

Abstract

The present invention relates to a pharmaceutical composition comprising lenvatinib mesylate and a stabilizer in an amount of about 10% to about 20% based on the total weight of the composition, wherein the stabilizer is selected from the group consisting of calcium hydroxide and potassium hydroxide; and its process for preparation thereof.

First claim

The invention claimed is:

1. A pharmaceutical composition comprising lenvatinib mesylate and a stabilizer in an amount of about 10% to about 20% based on the total weight of the composition, wherein the stabilizer is selected from the group consisting of calcium hydroxide and potassium hydroxide.

2. A pharmaceutical composition according to claim 1 , wherein the composition further comprises
a) at least one diluent in an amount of about 30% to about 60% based on the total weight of the composition;
b) at least one binder in an amount of about 1% to about 5% based on the total weight of the composition;
c) at least one disintegrating agent in an amount of about 10% to about 30% based on the total weight of composition; and
d) lubricant in an amount of about 1% to about 5% based on the total weight of the composition.

3. A pharmaceutical composition according to claim 2 , wherein diluent is selected from group consisting microcrystalline cellulose, mannitol, or mixtures thereof.

4. A pharmaceutical composition comprising lenvatinib mesylate, calcium hydroxide and potassium hydroxide.

5. A pharmaceutical composition according to claim 4 , wherein the composition comprises calcium hydroxide in an amount of about 10% to about 15% based on the total weight of the composition.

6. A pharmaceutical composition accord claim 4 , wherein the composition comprises potassium hydroxide in an amount about 1% to about 5% based on the total weight of the composition.

7. A pharmaceutical composition according to claim 4 , wherein the composition further comprises
a) microcrystalline cellulose in an amount of about 15% to about 25% by weight;
b) mannitol in an amount of about 20% to about 35% by weight;
c) low-substituted hydroxypropyl cellulose in an amount of about 20% to about 30% by weight;
d) hydroxypropyl cellulose in an amount of about 1% to about 5% by weight; and
e) talc in an amount of about 1% to about 5% by weight.

8. A pharmaceutical composition comprising
a) lenvatinib mesylate in an amount of about 4% to about 15% by weight;
b) calcium hydroxide in an amount of about 10% to about 15% by weight;
c) potassium hydroxide in an amount of about 1% to about 5% by weight;
d) microcrystalline cellulose in an amount of about 15% to about 25% by weight;
e) mannitol in an amount of about 20% to about 35% by weight;
f) low-substituted hydroxypropyl cellulose in an amount of about 20% to about 30% by weight;
g) hydroxypropyl cellulose in an amount of about 1% to about 5% by weight; and
h) talc in an amount of about 1% to about 5% by weight.

9. A pharmaceutical composition according to claim 8 , wherein the composition comprises of about 40% low-substituted hydroxypropyl cellulose based on total weight of low-substituted hydroxypropylcellulose as intragranular, and about 60% low-substituted hydroxypropyl cellulose based on total weight of low-substituted hydroxypropyl cellulose with whole amount of talc as extragranular.

Assignees

• Shilpa Medicare Ltd

Inventors

• Math Nijaguni Revansiddayya Rudraswamy
• Reddy Sreenivas
• Peri Ravi Vamsi
• Toppaladoddi Krishnamurthy
• Pradeep Shivakumar

Classifications

• A61K31/47 Primary

  Quinolines; Isoquinolines · CPC title

• A61K47/02

  Inorganic compounds · CPC title

• A61K9/1611

  Inorganic compounds · CPC title

• 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

• A61K9/1623

  Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules · CPC title