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Stable solid fingolimod dosage forms

A solid, lozenge technology, applied in the field of conjugates or complexes, novel fingolimod salts

Inactive Publication Date: 2018-01-02
HANDA PHARM LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] So far, there is no fingolimod or pharmaceutically acceptable salts, conjugates or complexes thereof that are specifically designed to provide fingolimod or its pharmaceutically acceptable salts, conjugates or complexes that dissolve rapidly in the patient's mouth, are stable on storage, are easy to manufacture and exhibit low friability. dosage form technology

Method used

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  • Stable solid fingolimod dosage forms
  • Stable solid fingolimod dosage forms
  • Stable solid fingolimod dosage forms

Examples

Experimental program
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Effect test

example 1

[0161] Fingolimod tablets that disintegrate quickly can be manufactured by dissolving fingolimod in an aqueous solution of lactitol. The solution was sprayed on mannitol and then dried. The resulting product is sieved and blended with other excipients before being compressed into lozenges. These lozenges should have the following composition:

[0162] Fingolimod HCl

0.56mg*

Lactitol

20mg

Mannitol

177.44mg

Magnesium stearate

2mg

[0163] *Equivalent to 0.5mg Fingolimod

[0164] These lozenges are placed in a humidity chamber and exposed to 85% relative humidity at 25°C to 30°C for about 6 hours. After humidification, the tablets are dried for about 6 hours at about 40°C to 45°C and 30% relative humidity.

example 2

[0166] Fingolimod tablets can be manufactured by dissolving fingolimod in an aqueous solution of lactitol and mannitol. The solution is spray dried to produce a solid powder. The resulting product is blended with lubricant and compressed into lozenges. These lozenges should have the following composition:

[0167] Fingolimod HCl

0.56mg*

Lactitol

20mg

Mannitol

177.44mg

Magnesium stearate

2mg

[0168] *Equivalent to 0.5mg Fingolimod

[0169] These lozenges are placed in a humidity chamber and exposed to 85% relative humidity at 25°C to 30°C for about 6 hours. After humidification, the tablets are dried for about 6 hours at about 40°C to 45°C and 30% relative humidity.

[0170] The moisturized and dried lozenges should exhibit a hardness greater than 2.5 kilolbs, a brittleness of less than 2%, and should disintegrate in less than 60 seconds when placed in a USP disintegration device.

example 3

[0172] Fast disintegrating fingolimod lozenges can be produced by freeze-drying an aqueous solution of gelatin, lactitol and mannitol. The solution is transferred to a heat-formed bubble holder and freeze-dried to form a lozenge. These lozenges should have the following composition:

[0173] Fingolimod HCl

[0174] These bubble trays were freeze-dried at a shelf temperature of -45°C. The resulting product was then thermally dried for four hours at a shelf temperature of 50°C to 55°C.

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Abstract

The present invention relates to a solid pharmaceutical dosage forms and methods for preparing the solid pharmaceutical dosage form that contains fingolimod or its pharmaceutically acceptable salts, conjugates or complexes thereof. The solid pharmaceutical dosage forms may rapidly disintegrates in a patient's oral cavity.

Description

[0001] This application claims the rights of U.S. Provisional Patent Application No. 62 / 105,603 filed on January 20, 2015 and U.S. Provisional Patent Application No. 62 / 216,100 filed on September 9, 2015. Technical field [0002] The present invention relates to a pharmaceutical dosage form and a method for manufacturing a pharmaceutical dosage form (such as hydrochloride) containing fingolimod and its pharmaceutically acceptable salts, conjugates or complexes. The pharmaceutical dosage form of the present invention should be stable during storage. The embodiments of the present invention should disintegrate or dissolve quickly in the oral cavity of the patient. The present invention also relates to novel fingolimod salts, conjugates or complexes that can be incorporated into pharmaceutical dosage forms. Background technique [0003] For reasons of stability, economy, simplicity and convenience of administration, the pharmaceutically active agent is usually formulated into a soli...

Claims

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Application Information

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IPC IPC(8): A61K31/137A61K47/26A61K47/00A61K9/20A61P25/00A61P37/02
CPCA61K31/137A61K9/0056A61K9/2013A61K9/2018A61K9/2027A61K9/205A61P25/00A61P37/02A61P37/06A61K9/006A61K9/2004A61K31/138
Inventor 刘芳宇
Owner HANDA PHARM LLC