Crystal form of salt formed by vinpocetine and D-tartaric acid and preparation method of crystal form

A technology of vinpocetine and tartaric acid, applied in the direction of organic chemistry, organic chemistry, etc.

Active Publication Date: 2016-11-16
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

Method used

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  • Crystal form of salt formed by vinpocetine and D-tartaric acid and preparation method of crystal form
  • Crystal form of salt formed by vinpocetine and D-tartaric acid and preparation method of crystal form
  • Crystal form of salt formed by vinpocetine and D-tartaric acid and preparation method of crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Add vinpocetine (350mg, 1mmol) and D-tartaric acid (150mg, 1mmol) into a 50ml Erlenmeyer flask at 0°C, add 20ml of methanol, and add in batches. When the solution is slightly turbid, stop adding and stir. After 1 hour, it was directly heated to 40 °C, a large amount of solids were precipitated, filtered and dried to obtain the product.

Embodiment 2

[0019] Add vinpocetine (350mg, 1mmol) and D-tartaric acid (150mg, 1mmol) into a 50ml Erlenmeyer flask at 10°C, add 20ml of methanol, and add in batches. When the solution is slightly turbid, stop adding and stir. After 1 hour, it was directly heated to 40 °C, a large amount of solids were precipitated, filtered and dried to obtain the product.

Embodiment 3

[0020] Embodiment 3: solid preparation (vinpocetine tablet) stability test data:

[0021] During the long-term six-month stability stakeout period, the new salt crystal has good stability and no new impurities appear. At the same time, the purity of the raw material can be further improved, and the solubility is also greatly improved.

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Abstract

The invention relates to a crystal form of salt formed by vinpocetine and D-tartaric acid and a preparation method of the crystal form and belongs to the technical field of the discovering and preparation of the crystal form of medicine salt. The salt prepared by the method is detected as the salt formed by the vinpocetine and the D-tartaric acid through analyzing 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). The vinpocetine is an insoluble drug (the solubility is about 5 microgram/mL and pKa=7.31), tests show that the salt formed by the vinpocetine and the D-tartaric acid is good in solubility and stability in the preparing process of solid preparations, and the development of new salt crystals lays a foundation for the development and application of the new dosage form of the salt. The spatial structure of the salt formed by the vinpocetine and D-tartaric acid is as shown in picture 1.

Description

technical field [0001] The present invention relates to a salt crystal formed by vinpocetine and D-tartaric acid and a preparation method thereof. Specifically, the present invention relates to a new crystal form of a salt formed by vinpocetine and D-tartaric acid and a preparation method thereof, belonging to pharmaceutical crystal forms The field of discovery and preparation technology. 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 ischemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D461/00
CPCC07B2200/13C07D461/00
Inventor 马玉恒
Owner JIANGSU QINGJIANG PHARMA
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