US 10,702,477 B2 · Afatinib-containing formulation

Abstract

The present invention refers to a process for preparing granules or particles comprising afatinib dimaleate, comprising the steps of providing afatinib dimaleate and at least one pharmaceutically acceptable excipient, and preparing granules or particles involving the use of at least one solvent selected from organic solvent and water, wherein all pharmaceutically acceptable excipients used in the process for preparing granules or particles have neutral or acidic properties, and wherein afatinib dimaleate has a solubility of at least 5 mg/ml in said at least one solvent. The present invention further refers to granules or particles comprising afatinib dimaleate that are prepared according to this process. Additionally, the present invention refers to a process for preparing a pharmaceutical composition comprising afatinib dimaleate, as well as to an adsorbate comprising afatinib dimaleate. Finally, the present invention refers to a pharmaceutical composition comprising afatinib dimaleate for use in a method of treating certain diseases.

Claims16

Dependent claims

Process for preparing amorphous granules or particles comprising afatinib dimaleate, wherein the process comprises:

(a) providing afatinib dimaleate and at least one pharmaceutically acceptable excipient;
and
(b) preparing amorphous granules or particles by use of afatinib dimaleate and at least one pharmaceutically acceptable excipient as provided in step (a), and at least one solvent selected from organic solvents and water;
wherein all pharmaceutically acceptable excipients which are used in the process for preparing granules or particles have neutral or acidic properties,
wherein the excipient is determined to have neutral properties if the pH of a solution/suspension of the excipient in water when measured by pH meter has a pH of 6 to 8, and
wherein the excipient is determined to have acidic properties if the pH of the solution/suspension of the excipient in water has a pH of less than 6, and
wherein said afatinib dimaleate as provided in step (a) has a solubility of at least 5 mg/ml in said at least one solvent of step (b).

4 more elements

Dependencies are inferred from the claim text.

Afatinib-containing formulation

Life of this patent

Afatinib-containing formulation

Life of this patent

Abstract

Claims16