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Pymeprazole crystal form E

A technology of pimeprazole crystal and crystal form, which is applied in the chemical field, can solve the problems of stability and druggability to be improved, and achieve the effect of stable crystal form properties and good reproducibility

Inactive Publication Date: 2012-10-17
天津市嘉凡生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, pimeprazole has multiple crystal forms, but its stability and druggability need to be improved

Method used

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  • Pymeprazole crystal form E

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0008] Embodiment 1 uses ethylene glycol to prepare the E crystal form of pimeprazole

[0009] Add the crude product of pimeprazole (100.0g) to ethylene glycol (4.0L), stir at room temperature (20~30°E) for 0.5 hours, and basically dissolve. Filtrate, slowly add n-heptane (6.0 L) to the filtrate, stir and crystallize for 0.5 hour, then add n-heptane (9.0 L), continue stirring and crystallizing for 0.5 hour. Filtrate, drain, and wash the obtained solid with n-heptane (7.5 L × 2 times), 60 min each time, filter, drain, and dry overnight at 60°E under vacuum (oil pump) to obtain a solid: 85.0 g.

[0010] Sutra figure 1 The XRPE data shown confirms the E crystalline form of pimeprazole.

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Abstract

The invention provides a pymeprazole crystal form E, the structure of which is as shown in the appended drawing 1. The beneficial effect of the present invention is that properties of the crystal form are stable.

Description

technical field [0001] The invention belongs to the field of chemistry, in particular to a crystal form E of pimeprazole. Background technique [0002] Drug crystal form research and drug solid-state research and development are of great significance in the pharmaceutical industry. Drug molecules usually have different solid forms, including salts, polycrystals, co-crystals, amorphous forms, hydrates and solvates; different crystal forms of the same drug molecule, in terms of crystal structure, stability, manufacturability and bioavailability There may be significant differences in properties such as degree, which directly affects the efficacy and developability of the drug. Therefore, any drug development requires comprehensive and systematic polymorph screening to find as many crystal forms as possible, and then use various solid-state methods to conduct in-depth research on these crystal forms to find the most suitable crystal form for development. [0003] In the prior...

Claims

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Application Information

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IPC IPC(8): C07D401/12
Inventor 王进
Owner 天津市嘉凡生物科技有限公司