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Rasagiline orally disintegrating compositions

A technology of rasagiline mesylate and its composition, which is applied in the field of rasagiline orally disintegrating composition, which can solve the problems of high friability, increased cost, and high cost

Inactive Publication Date: 2014-01-08
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, EP0814789 relies on freeze-drying of the MAO-B inhibitor formulation which is an expensive process and results in high friability of the product, also increasing costs due to packaging requiring expensive special blister packs

Method used

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  • Rasagiline orally disintegrating compositions
  • Rasagiline orally disintegrating compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Formulation A was prepared using the following steps using the excipients in Table 1:

[0112] 1. Mix xylitol, aerosil 0.3mg / tablet, rasagiline mesylate, starch NF, Ac-Di-Sol, flavoring agent 1.34mg / tablet, and sodium saccharin 0.5mg / tablet for 5 minutes .

[0113] 2. Add Purified Water USP to the mixture from Step 1 and mix for 60 seconds.

[0114] 3. Dry the granules (outlet temperature: 44°C).

[0115] 4. Sieve the granules through a 0.6 mesh sieve.

[0116] 5. The granules are then mixed with 0.3 mg / tablet of aerosil, Pharmaburst TM , 0.5 mg / tablet of sodium saccharin, and 1 mg / tablet of cherry flavor were mixed for 15 minutes.

[0117] 6. The mixture from step 5 was then blended with stearic acid and talc for 5 minutes.

[0118] 7. Compress the tablet to a hardness of 5 kPa.

Embodiment 2

[0120] Formulation B was prepared using the following steps using the excipients in Table 1:

[0121] 1. Mix xylitol, aerosil 0.3mg / tablet, rasagiline mesylate, starch NF, Ac-Di-Sol, flavoring agent 1.34mg / tablet, and sodium saccharin 0.5mg / tablet for 5 minutes .

[0122] 2. Add Purified Water USP to the mixture from Step 1 and mix for 60 seconds.

[0123] 3. Dry the granules (outlet temperature: 44°C).

[0124] 4. Sieve the granules through a 0.6 mesh sieve.

[0125] 5. The granules are then mixed with 0.3 mg / tablet of aerosil, Pharmaburst TM , 0.5 mg / tablet of sodium saccharin, and 1 mg / tablet of cherry flavor were mixed for 15 minutes.

[0126] 6. The mixture from step 5 was then blended with stearic acid and talc for 5 minutes.

[0127] 7. Compress the tablet to a hardness of 6 kPa.

Embodiment 3

[0129] Formulation C was prepared using the following steps using the excipients in Table 1:

[0130] 1. Mix 77.276mg / tablet of xylitol, 0.3mg / tablet of aerosil, rasagiline mesylate, starch NF, Ac-Di-Sol, 1.34mg / tablet of flavoring agent, and 0.5mg / tablet of The sodium saccharin was mixed for 5 minutes.

[0131] 2. Add Purified Water USP to the mixture from Step 1 and mix for 60 seconds.

[0132] 3. Dry the granules (outlet temperature: 44°C).

[0133] 4. Sieve the granules through a 0.6 mesh sieve.

[0134] 5. The granules were then mixed with 0.3 mg / tablet of aerosil, sodium bicarbonate, 150 mg / tablet of xylitol, 0.5 mg / tablet of sodium saccharin, and 1 mg / tablet of cherry flavor for 15 minutes.

[0135] 6. The mixture from step 5 was then blended with stearic acid and talc for 5 minutes.

[0136] 7. Compress the tablet to a hardness of 4 kPa.

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Abstract

This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, a mixture of a disintegrant, a flow agent and particles having a non-filamentous microstructure of at least two sugar alcohols, a supplemental sugar alcohol, a supplemental flow agent, and a supplemental disintegrant. This invention further provides a method of treating a subject afflicted with Parkinson's disease comprising administering to the subject a therapeutically effective amount of the solid pharmaceutical composition, thereby treating the subject. Finally, this invention provides a process of making such solid pharmaceutical compositions.

Description

[0001] This application is the international application number PCT / US2005 / 041882, the international application date is November 17, 2005, and the date of entering the Chinese national phase is July 10, 2007. A divisional application for a disintegrating composition". [0002] This application claims the benefit of US Provisional Application No. 60 / 630,918, filed November 24, 2004, the contents of which are hereby incorporated by reference. [0003] Throughout this application, various publications are referenced throughout by reference. The contents of these publications in their entirety are hereby incorporated by reference into this application in order to more fully describe the state of the art known to those skilled in the art herein as of the date the invention was described and patented . Background of the invention [0004] 美国专利号5,532,415,5,387,612,5,453,446,5,457,133,5,599,991,5,744,500,5,891,923,5,668,181,5,576,353,5,519,061,5,786,390,6,316,504和6,630,514,和PCT国际公布...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K9/16A61K9/48A61K9/28A61K31/135A61K47/26A61P25/16
CPCA61K31/4166A61K9/2059A61K31/135A61K9/2054A61K9/0056A61K9/2018A61P25/16
Inventor 舒拉米特·帕塔斯尼克丹尼尔勒·利希特阿德里安·吉尔贝特
Owner TEVA PHARMA IND LTD
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