Compositions Containing Ibrutinib

a technology of ibrutinib and ibrutinib, which is applied in the direction of drug compositions, inorganic non-active ingredients, granulation by pressing, etc., can solve the problems of interfering with the ability of cancer cells to grow, divide, repair, communicate with other cells, etc., and achieve the effect of facilitating the sprinkling of capsule contents

Inactive Publication Date: 2016-10-06
JANSSEN PHARMA NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0018]In a further aspect, the treatment methods herein involve use of a sprinkle capsule that is open to facilitate sprinkling of the capsule's contents into food or a beverage. In one embodiment, the beverage is water. In another embodiment,...

Problems solved by technology

Differences exist between the various types of targeted therapy but all interfere with...

Method used

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  • Compositions Containing Ibrutinib
  • Compositions Containing Ibrutinib
  • Compositions Containing Ibrutinib

Examples

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example 1

Solid Compositions Containing Ibrutinib

[0118]Solid compositions containing Ibrutinib were prepared for inclusion in a capsule as described in the following.

[0119]A. 140 mg Capsule

[0120]In this process, an intragranular blend was prepared by mixing MCC (151.49 mg; Avicel PH 101), SLS (9.40 mg; Kolliphor; fine), and CCS (13.10 mg; Ac-di-sol) in a vessel. This was then mixed with Ibrutinib (70 mg; micronized, Lonza, Nansha). The remaining Ibrutinib (70 mg) was then added and the composition mixed. Magnesium stearate (0.8 mg; Non-Bovine #5712) was then added to this mixture and the same blended to provide a pre-roller compaction blend. The pre-roller compaction blend was then roller compacted to form ribbons. The ribbons were then milled to provide a composition containing granules.

[0121]The granules were then blended with a second portion of SLS (4.6 mg; Kolliphor; fine) and CCS (9.9 mg; Ac-di-sol). To this blend was then added a second portion of magnesium stearate (0.8 mg; Non-Bovine...

example 2

Liquid Suspension Composition Containing Ibrutinib

[0125](i) 70 mg / mL Ibrutinib Liquid Suspension

[0126]A liquid composition containing 70 mg / mL of Ibrutinib was prepared. Specifically, water (300 mL) was mixed with a composition MCC of CCS (Avicel RC591; 6.5 g) for 30 minutes. This dispersion was then homogenized for 30 seconds using a SILVERSON® homogenizer L2R at the maximal speed (7500 rpm). HPMC (2910 5 mPas; 1.25 g) was mixed with water (120 mL) until homogeneous using a magnetic stirrer. Micronized Ibrutinib (35 g, Lonza Clinical) was then added to the HPMC solution and mixed for 120 minutes. The MCC / CCS dispersion was then mixed with the Ibrutinib mixture. Sucralose (0.5 g), sodium methyl parahydroxybenzoate (0.5725 g), and sodium ethyl parahydroxybenzoate (0.2875 g) were added to the mixture. After about 10 minutes stirring, citric acid monohydrate (0.7565 g), and disodium hydrogen phosphate anhydrous parenteral (0.69 g) were then added to this mixture. The mixture was stirre...

example 3

Large Scale Preparation of a Suspension Containing Ibrutinib Preparation of 4L Batch

[0131]Purified water (480 g) was added to a vessel and warmed to about 83° C. at a stirring rate of about 400 rpm for about 60 minutes. HPMC (10.002 g) was slowly added to the vessel and the mixture stirred at a rate of about 7600 rpm for about 4 minutes until the mixture was homogenized. To this vessel was added purified water (480 g) and then mixture was stirred for about 5 minutes at a rate of about 500 rpm at room temperature until the mixture was solubilized. Ibrutinib (278.6 g) was added to the mixture and it was stirred at 600 rpm for about 2 h until it was homogenous. The mixture was monitored using a microscope for agglomerates.

[0132]Purified water (2400 g) was then added to a second vessel. At a rate of about 500 rpm, MCC (51.74 g; Avicel) was added to the second vessel over a period of 3 minutes, followed by stirring at a rate of about 400 rpm for about 60 minutes. This mixture was then ho...

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Abstract

Discussed herein are pharmaceutical compositions containing Ibrutinib and processes for preparing them. The compositions may be utilized in the treatment of a variety of conditions including, without limitation, B-cell proliferative disorders such as non-Hodgkin lymphoma (diffuse large B cell lymphoma, follicular lymphoma, mantle cell lymphoma or burkitt lymphoma), Waldenstrom macroglobulinemia, plasma cell myeloma, chronic lymphocytic leukemia, lymphoma, or leukemia. These compositions are designed for oral ingestion. The compositions are contained within a capsule such as a standard or sprinkle or in a liquid formulation such as a suspension. In one embodiment, the pharmaceutical composition contains Ibrutinib, a salt, prodrug, or metabolite thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, and magnesium stearate. In another embodiment, the pharmaceutical composition contains Ibrutinib, a salt, prodrug, or metabolite thereof, microcrystalline cellulose, carboxymethylcellulose sodium, hydroxypropylmethylcellulose, citric acid monohydrate, disodium hydrogen phosphate, sucralose, sodium methyl parahydroxybenzoate, sodium ethyl parahydroxybenzoate, concentrated hydrochloric acid, sodium hydroxide, and water.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application No. 62 / 143,659, filed Apr. 6, 2015, the entirety of which is incorporated by reference.TECHNICAL FIELD[0002]This invention relates to compositions containing Ibrutinib and methods for using same.BACKGROUND[0003]Targeted therapy involves identifying specific differences between cancer cells and normal cells. These differences are used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects. Differences exist between the various types of targeted therapy but all interfere with the ability of the cancer cell to grow, divide, repair and / or communicate with other cells.[0004]Ibrutinib is an anticancer drug targeting B-cell malignancies. Ibrutinib blocks signals that stimulate malignant B cells to grow and divide uncontrollably. It was approved by the US FDA in November 2013 for the treatment of mantle cell l...

Claims

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Application Information

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IPC IPC(8): A61K31/519B01J2/10A61J3/07B01J2/22A61K9/48A61K9/00
CPCA61K31/519A61K9/4866A61K9/4858A61K9/0053A61K9/4833A23V2002/00B01J2/22B01J2/10A23L1/304A23L1/30A61J3/07A61K47/38A61K47/20A61P35/00A61P35/02A61K47/02A61K47/12A61K9/10A23L33/10A23L33/16A61P43/00
Inventor GUPTA, MANISH KUMARTAMBWEKAR, KAUSTUBHNAIR, BINURAJ KRISHNANGOLE, DILIP J.BERNINI, MARISTELLAINGHELBRECHT, SABINE
Owner JANSSEN PHARMA NV
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