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Novel polymorphs and pseudopolymorphs of risedronate sodium

A technology of risedronate sodium and risedronic acid, which is applied in the field of risedronate sodium pharmaceutical compositions, and can solve the problems of unpublished X-ray results

Inactive Publication Date: 2007-08-29
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The monohydrate and sesquihydrate were further characterized by single crystal X-ray crystallography and thermogravimetric analysis, but the X-ray results were not published

Method used

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  • Novel polymorphs and pseudopolymorphs of risedronate sodium
  • Novel polymorphs and pseudopolymorphs of risedronate sodium
  • Novel polymorphs and pseudopolymorphs of risedronate sodium

Examples

Experimental program
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Effect test

Embodiment 1

[0237] At reflux temperature, a solution of sodium hydroxide (1.18 g, 1 equivalent) in water / ethanol mixture (32% v / v) (18.5 ml) was added dropwise to risedronic acid (8.35 g) in water / ethanol Suspension in ethanol mixture (32% v / v) (105ml). The reaction mixture was heated to reflux for 18 hours. The reaction mixture was cooled to room temperature. Cool further using an ice bath. The precipitate was filtered off, washed with ethanol (2×10 ml) and dried in a vacuum oven at 50° C. for 24 hours to obtain 8.77 g (91%) of risedronate sodium Form B.

Embodiment 2

[0239] At reflux temperature, an aqueous solution (100 ml) of sodium hydroxide (1.47 g, 1 equiv.) was added in one portion to a suspension of risedronic acid (10.0 g) in ethanol (100 ml). The reaction mixture was heated to reflux for an additional 18 hours. The reaction mixture was then cooled to room temperature. Cool further using an ice bath. The precipitate was filtered off, washed with ethanol (1×15 ml), and dried in a vacuum oven at 50° C. for 27 hours to obtain 9.35 g of risedronate sodium Form B.

Embodiment 3

[0241] A solution of sodium hydroxide (1.18 g, 1 equivalent) in a water / ethanol mixture (60% v / v) (126 ml) was added in one portion to dry solid risedronic acid (8.35 g) at room temperature. The reaction mixture was then heated to reflux for 18 hours. The reaction mixture was then cooled to room temperature. Cool further using an ice bath. The precipitate was filtered off, washed with ethanol (1×10 ml) and dried in a vacuum oven at 50° C. for 24 hours to obtain 8.04 g (84%) of risedronate sodium Form B (LOD by TGA = 6.22%).

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Abstract

The invention provides novel polymorphs and pseudopolymorphs of risefronate sodium and risedronate disodium, preparing method thereof, composition containing same, and use thereof for preparing medicaments for treating osteoporosis.

Description

[0001] This application is an international filing date of January 6, 2003 (the international application number is PCT / US03 / 00345), and the national phase application number is 03813091.2 entitled "New polymorphs and pseudopolymorphs of risedronate sodium A divisional application of the patent application for "crystal form". [0002] Cross References to Related Applications [0003] This application claims the benefit of the following provisional applications: 60 / 372,465, filed April 11, 2002, 60 / 404,174, filed August 16, 2002, and 60 / 405,668, filed August 22, 2002 . field of invention [0004] The present invention relates to new polymorphs and pseudopolymorphs of risedronate sodium and processes for their preparation. The present invention also relates to pharmaceutical compositions containing risedronate sodium in various polymorphic or pseudopolymorphic forms. Background of the invention [0005] Osteoporosis is a disease characterized by the gradual demineralization...

Claims

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Application Information

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IPC IPC(8): C07F9/58A61K31/675A61K9/14A61K9/20A61K9/48A61P19/10
CPCC07F9/582C07F9/58A61P19/10A61K9/14
Inventor J·阿龙希梅R·里斯茨-里龙E·科瓦勒维斯基-伊斯海R·里多-哈达斯
Owner TEVA PHARMA IND LTD
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