Solid and crystalline ibandronate sodium and processes for preparation thereof

A technology of sodium ibandronate and crystal form, applied in the field of solid state chemistry of sodium ibandronate, can solve the problems of restricting oral active ingredients and the like

Inactive Publication Date: 2007-08-22
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The rate at which an active ingredient dissolves in a patient's gastric fluid may be of therapeutic interest because it limits the upper limit of the rate at which an orally administered active ingredient can reach the patient's bloodstream

Method used

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  • Solid and crystalline ibandronate sodium and processes for preparation thereof
  • Solid and crystalline ibandronate sodium and processes for preparation thereof
  • Solid and crystalline ibandronate sodium and processes for preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0187] Sodium ibandronate (3 g) was dissolved in dimethylsulfoxide (DMSO) (20 mL) at 125°C. To the resulting solution was added dropwise 2-butanol (40 mL) to give a white precipitate. The slurry was stirred at 125°C for 3 hours, then cooled to room temperature and stirred for 16 hours. The precipitate was separated by vacuum filtration, washed with 2-butanol (2×5 ml), and dried in a vacuum oven at 50° C. for 24 hours to obtain 3 g of sodium ibandronate in crystal form C. Form C ibandronate sodium was analyzed by TGA as described above, and the weight loss was about 15% to about 16%.

Embodiment 2

[0189] Sodium ibandronate (3 g) was dissolved in DMSO (20 mL) at 120°C. To the resulting solution was added dropwise 1-butanol (40 mL) to give a white precipitate. The slurry was stirred at 120°C for 3 hours, then cooled to room temperature and stirred for 16 hours. The precipitate was isolated by vacuum filtration, washed with 1-butanol (2×5 ml), and dried in a vacuum oven at 50° C. for 24 hours to obtain 3 g of sodium ibandronate in crystal form C.

[0190] Sodium Ibandronate Form D

Embodiment 3

[0192] Sodium ibandronate (3 g) was dissolved in water (6 mL) at reflux temperature. To the resulting solution was added dropwise acetone (50 mL) at reflux temperature to obtain a white precipitate. The slurry was stirred at reflux temperature for 4.5 hours, then cooled to room temperature. The precipitate was separated by vacuum filtration, washed with acetone (3×13 ml), and dried in a vacuum oven at 50° C. for 22 hours to obtain 3.3 g of ibandronate sodium ibandronate in crystal form D. D-type ibandronate sodium was analyzed by TGA, and the weight loss was about 25%.

[0193] Sodium Ibandronate Form E

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Abstract

The present invention relates to solid amorphous and crystalline forms of ibandronate sodium.

Description

[0001] This application claims the benefit of US Provisional Patent Application No. 60 / 604,026, filed August 23, 2004 and Provisional Application No. 60 / 690,867, filed June 16, 2005. technical field [0002] The present invention relates to the solid state chemistry of ibandronate sodium. Background technique [0003] The experimental formula for ibandronate sodium is C 9 h 22 NO 7 P 2 Na·H 2 O. The chemical name of ibandronate sodium is (1-hydroxy-3-(N-methyl-N-pentylamino)propylene) bisphosphonic acid monosodium salt. The chemical structure of ibandronate sodium is as follows: [0004] The chemical structure of ibandronic acid (IBD-Ac) is as follows: [0005] Sodium ibandronate is a third-generation nitrogen-containing bisphosphonate characterized by aliphatic tertiary amine side chains. Ibandronate sodium is a white powder. [0006] US Patent No. 4,972,814 discloses bisphosphonic acid derivatives, methods for their preparation and pharmaceutical compositions ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/663A61P19/10C07F9/38
CPCC07F9/3873A61P19/08A61P19/10A61P3/00A61P35/00A61K31/663
Inventor R·利夫什茨-利伦T·拜尔J·阿伦希姆
Owner TEVA PHARMA IND LTD
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