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Crystal form of salt formed from vinpocetine and phosphoric acid, and preparation method

A kind of technology of vinpocetine and phosphoric acid, applied in the new crystal form of vinpocetine and phosphoric acid formed salt and preparation thereof, the salt crystal formed by vinpocetine and phosphoric acid and its preparation field

Inactive Publication Date: 2015-12-16
JIANGSU QINGJIANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far there are few relevant reports about the crystal form of the salt of Vinpocetine. In view of this, the technical problem to be solved in the present invention is to overcome the deficiencies in the prior art. The present invention is to provide a new salt form of Vinpocetine It has good solubility and stability, and the development of new salt forms has laid the foundation for the development and application of new dosage forms.

Method used

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  • Crystal form of salt formed from vinpocetine and phosphoric acid, and preparation method
  • Crystal form of salt formed from vinpocetine and phosphoric acid, and preparation method
  • Crystal form of salt formed from vinpocetine and phosphoric acid, and preparation method

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Experimental program
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Effect test

Embodiment 1

[0018] At room temperature, add vinpocetine (350mg, 1mmol) into a 100ml Erlenmeyer flask, add 80ml of a mixed solvent of methanol and water (4:1), stir with a magnet for 1 hour, the solution is clear, add 1mmol of phosphoric acid dropwise, After stirring for 20 minutes, it evaporated slowly and no solid appeared.

Embodiment 2

[0020] At room temperature, add vinpocetine (350mg, 1mmol) into a 100ml Erlenmeyer flask, add 80ml imported methanol, stir with a magnet for 1 hour, the solution is clear, add 1mmol of phosphoric acid dropwise, stir for 20 minutes, and place it in a desiccator Volatilize in medium to obtain a solid that is the new salt form

Embodiment 3

[0022] At room temperature, Vinpocetine (350mg, 1mmol) was added to a 100ml Erlenmeyer flask, 80ml of methanol was added, and trimethyl orthoformate was added, and after stirring with a magnet for 1 hour, the solution was clarified, and 1mmol of phosphoric acid was added dropwise, and placed in In a normal environment (non-dry environment), after stirring for 20 minutes, slowly volatilize to obtain a solid, that is, a new salt type.

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Abstract

The invention discloses a crystal form of a salt formed from vinpocetine and phosphoric acid, and a preparation method, and relates to the technical field of discovery and preparation of a crystal form of a pharmaceutical salt. The prepared salt formed from vinpocetine and phosphoric acid is detected through analytical methods, such as thermal gravimetric analysis (TGA), X-ray powder diffraction (P-XRD), X-ray single crystal diffraction (S-XRD), differential scanning calorimetry (DSC), and infrared spectroscopy (IR). Vinpocetine is a indissolvable medicine (the solubility of which is about 5 [mu]g / mL and pKa of which is 7.31), while it is proved through detection that the salt prepared from vinpocetine and phosphoric acid has excellent solubility and stability. Development of the novel salt form establishes foundation for development and application of new formulation.

Description

technical field [0001] The present invention relates to a salt crystal formed by vinpocetine and phosphoric acid and a preparation method thereof. Specifically, the present invention relates to a new crystal form of salt formed by vinpocetine and phosphoric acid and a preparation method thereof, belonging to the discovery and preparation technology of pharmaceutical crystal forms field. Background technique [0002] Vinpocetine was first developed by the Hungarian Gedeon Richter company and launched in 1978. Its pharmacological effects include: increasing cerebral blood flow; promoting the uptake and utilization of glucose and oxygen in the brain, increasing ATP, reducing the production of lactic acid during ischemia and hypoxia; preventing brain cell excitotoxic death (excessive stimulation caused by excitatory amino acids) body excitation); reduce brain hypoxic damage, protect neurons; enhance dopaminergic, serotonergic and noradrenergic nerve functions; prevent ischemic ...

Claims

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Application Information

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IPC IPC(8): C07D461/00
CPCC07D461/00C07B2200/13
Inventor 马玉恒
Owner JIANGSU QINGJIANG PHARMA
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