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Method for preparing sodium ibandronate crystal and hydrated crystal thereof

A technology of sodium ibandronate and crystals, applied in the field of crystal preparation of compounds, can solve the problems of unstable composition, unsuitable pharmaceutical composition, unfavorable large-scale industrial manufacturing, etc., and achieve simple and easy manufacturing method and convenient production Effect

Inactive Publication Date: 2008-02-06
CHONGQING SHENGHUAXI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its unstable composition, most of the crystalline states are obviously not suitable as pharmaceutical compositions, so it is not conducive to large-scale industrial production

Method used

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  • Method for preparing sodium ibandronate crystal and hydrated crystal thereof
  • Method for preparing sodium ibandronate crystal and hydrated crystal thereof
  • Method for preparing sodium ibandronate crystal and hydrated crystal thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Add 6g of sodium ibandronate to 40ml of water, stir and dissolve at room temperature, add 80ml of DMF dropwise, a white solid precipitates, continue to stir for 2 hours, cool to 0°C, filter with suction, and vacuum dry at 60-70°C for 3 hours to obtain Ibandronate Sodium phosphonate monohydrate crystalline state (I) 5g, X-ray powder diffraction pattern is shown in Figure 1. The dehydration peak shown by its TGA thermal analysis is 4.52%, and the bulk density is 0.75g / cm3.

Embodiment 2

[0026] Add 5g of ibandronic acid into 50ml of water, add 0.6g of solid sodium hydroxide under normal temperature stirring, stir to form a homogeneous solution, add 80ml of DMF at one time, a white solid precipitates out, continue to stir for 2 hours, cool to 0°C, filter with suction, and Vacuum-dried at 60-70°C for 3 hours to obtain 4.8 g of ibandronate sodium monohydrate crystalline state (I).

Embodiment 3

[0028] Sodium ibandronate 6g was added to 40ml of water, stirred and dissolved at room temperature, 80ml of dimethylacetamide was added dropwise, and a white solid was precipitated, continued to stir for 2 hours, cooled to 0°C, filtered with suction, and vacuum-dried at 60-70°C for 3 hours to obtain Sodium ibandronate monohydrate crystalline state (I) 5.2g.

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Abstract

The invention provides a preparation process for Ibandronate monosodium crystals and hydration crystals thereof. The Ibandronate monosodium compound in Formula (1) is dissolved in 2 to 30 times of water; at least one of azanyl amides, alkyl sulfoxides, glycol ethers and alicyclic ethers is added into the compound solution, is stirred under condition of room-temperature to precipitate crystals, then is cooled down to minus 5 to 15 DEG C and filtered, and is dried in vacuum between 30 and 75 DEG C. The process is simple and easy to operate; Ibandronate monosodium hydration crystals have good crystal stability and are suitable for industrial production and storage.

Description

technical field [0001] The invention relates to a crystal preparation method of a compound and a new crystalline product prepared by the method. Background technique [0002] The chemical formula of ibandronate sodium is C 9 h 22 NO 7 P 2 Na·H 2 O, the structure is shown in formula (1), and the chemical name is: (1-hydroxyl-3-(N-methyl-N-pentylamino)propylene) diphosphate monosodium salt. [0003] [0004] Sodium ibandronate is a third-generation nitrogen-containing diphosphate with an amino side chain substituted with an aliphatic hydrocarbon at the 3-position, and is in the form of a white powder. [0005] Ibandronate sodium is a drug developed by Hoffmann-La Roche for the treatment of bone metabolism disorders, such as hypercalcemia caused by malignant tumors, osteolysis, Paget-like disease, osteoporosis and metastatic bone disease. Medicinal compounds for diseases can be made into intravenous or oral pharmaceutical preparations for use. [0006] Disclosed in US...

Claims

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Application Information

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IPC IPC(8): C07F9/38
Inventor 姜维平
Owner CHONGQING SHENGHUAXI PHARMA CO LTD
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