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Crystalline form of maxacalcitol

A maxacalcitol, crystallization technology, applied in the direction of organic chemistry, organic chemistry methods, etc., can solve the problem of serum calcium and phosphate preventing the application of treatment

Inactive Publication Date: 2014-02-19
FORMOSA LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, 1α,25(OH) 2 D. 3 High potency in raising serum calcium and phosphate prevents its therapeutic use in most cases

Method used

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  • Crystalline form of maxacalcitol
  • Crystalline form of maxacalcitol
  • Crystalline form of maxacalcitol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation of Maxacalcitol Hydrate

[0038] Crude maxacalcitol (18.48 g) was dissolved in acetone (87 mL), followed by the addition of water (104.4 mL). The resulting solution was stirred at room temperature for about one hour, cooled to about 8°C, and then kept at room temperature for at least 4 hours. The formed crystals were filtered at room temperature and dried under vacuum overnight to give maxacalcitol hydrate (10.12 g).

Embodiment 2

[0040] Preparation of Maxacalcitol Hydrate

[0041] Crude maxacalcitol (1 g) was dissolved in a mixed solution of methyl formate (4 mL), followed by the addition of water (0.1 mL). The resulting solution was stirred and cooled to about 8°C and then kept at room temperature for at least 4 hours. The formed crystals were filtered at room temperature and dried under vacuum overnight to give maxacalcitol hydrate (0.4 g).

Embodiment 3

[0043] Preparation of Maxacalcitol Hydrate

[0044] Crude maxacalcitol (100 mg) was dissolved in acetonitrile (2 mL), followed by the addition of water (3.8 mL). The resulting solution was stirred and cooled to about 8°C and then kept at room temperature for at least 4 hours. The crystals formed were filtered at room temperature and dried under vacuum overnight to give maxacalcitol hydrate (35 mg).

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Abstract

The present invention relates to maxacalcitol hydrate, a new crystalline form of maxacalcitol, with superior technical properties e.g. in the manufacture of crystal suspension formulations, and with superior stability properties.

Description

technical field [0001] The present invention relates to maxacalcitol (maxacalcitol) hydrate, a new crystalline form of maxacalcitol, which has excellent technical properties (for example in the preparation of crystal suspension formulations) and has excellent stability. Background technique [0002] Vitamin D has long been known to play an important role in calcium and phosphate homeostasis through its actions on the intestines, kidneys, bones and parathyroid glands. These effects are mediated by the activated, hormonal form of 1α,25-dihydroxyvitamin D 3 [1α,25(OH) 2 D. 3 ] and vitamin D receptor (VDR) (Molecular Aspects of Medicine 2008, 29(6):433-52). VDR is a member of the steroid / thyroid hormone superfamily and contains a highly conserved N-terminal DNA-binding domain and a less conserved C-terminal ligand-binding domain. [0003] The central role of vitamin D3 in calcium metabolism, cell proliferation, and cell differentiation makes it an attractive candidate for ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C401/00
CPCC07C401/00C07B2200/13C07C2601/14C07C2602/24
Inventor 魏庆鹏黄沛蓁
Owner FORMOSA LAB