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Vinpocetine compound and drug composition thereof

A technology of vinpocetine and its composition, which is applied in the field of vinpocetine compounds, can solve the problems of poor storage stability of vinpocetine, achieve the effects of improving storage stability, less impurity content, and improving drug safety

Inactive Publication Date: 2015-03-04
北京康瑞达彤科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The storage stability of vinpocetine in the prior art is relatively poor, and its related substances will increase significantly in light and humid environments. In order to obtain a vinpocetine compound with better performance, the present invention is proposed

Method used

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  • Vinpocetine compound and drug composition thereof
  • Vinpocetine compound and drug composition thereof
  • Vinpocetine compound and drug composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Preparation of Vinpocetine Compounds

[0040] N,N-dimethylformamide and ethanol are formulated into a mixed solvent at a volume ratio of 2:1, and the raw material drug of vinpocetine is added to a mixed solvent of N,N-methylformamide and ethanol, and the mixed solvent The ratio of the volume of vinpocetine to the mass of vinpocetine is 4ml: 1g, heat up to 60°C, stir until completely dissolved, keep warm, adjust the pH of the solution to 5.5, add activated carbon for decolorization, the amount of activated carbon is 0.3% of the volume of the mixed solvent (g / ml), stirred for 30 minutes, filtered to obtain a clear solution, moved the clear solution into a reaction kettle, placed it in an oven at 100°C for 48 hours, and let it stand to cool down naturally. When the temperature dropped below 70°C, open the kettle and pour into the Add ice water to the solution, the volume ratio of the ice water to the mixed solvent is 15:1, filter to obtain a filter cake, wash the filter ca...

Embodiment 2

[0043] Preparation of Vinpocetine Compounds

[0044]N,N-dimethylformamide and ethanol are formulated into a mixed solvent at a volume ratio of 4:1, and the raw material drug of vinpocetine is added to a mixed solvent of N,N-methylformamide and ethanol, and the mixed solvent The ratio of the volume of Vinpocetine to the mass of Vinpocetine is 6ml: 1g, heat up to 70°C, stir until completely dissolved, keep warm, adjust the pH of the solution to 6.0, add activated carbon to decolorize, the amount of activated carbon is 0.3% of the volume of the mixed solvent (g / ml), stirred for 30 minutes, and filtered to obtain a clear solution. Move the clear solution into a reaction kettle, place it in an oven at 120°C for 12 hours, and let it cool down naturally. Add ice water to the solution, the volume ratio of the ice water to the mixed solvent is 5:1, filter to obtain a filter cake, wash the filter cake with ethanol at 5°C for 3 times, and then dry under reduced pressure for 2 hours to ob...

Embodiment 3

[0047] Preparation of Vinpocetine Sterile Powder Injection

[0048] Weigh 10 parts of vinpocetine and 5 parts of ascorbic acid prepared in Example 1 under sterile conditions, place them in a solid powder mixer and mix them evenly, and transfer the obtained raw materials to a sterile preparation workshop for precise metering and packaging. Each bottle contains Changchun Xitine 0.5g, stoppered and capped, the finished product is packaged for storage and sent for inspection.

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to vinpocetine compound. The vinpocetine compound is shown in an X-ray powder diffraction spectra I measured by a Cu-K alpha ray. A preparation method of the vinpocetine compound, and a drug composition containing the vinpocetine compound are also provided by the invention. The vinpocetine compound disclosed by the invention is long in storage time, less in impurity content, and good in storage stability; and the drug composition containing the vinpocetine compound is good in storage stability and high in safety performance.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a vinpocetine compound, a preparation method of the vinpocetine compound and a pharmaceutical composition thereof. Background technique [0002] Vinpocetin: English name Vinpocetinum; molecular formula C22H26N2O2; molecular weight 350.45; it is an alkaloid extracted from oleander plants, which is a derivative of vincamine (vlncamlne). Vinpocetine can inhibit phosphodiesterase activity, increase the role of c-GMP, the messenger of vascular smooth muscle relaxation, and selectively increase cerebral blood flow. In addition, it can also inhibit platelet aggregation, reduce human blood viscosity, enhance red blood cell deformability, and improve blood circulation. Fluidity and microcirculation, promote brain tissue uptake of glucose, increase brain oxygen consumption, improve brain metabolism, but have little effect on cardiovascular and blood pressure; good tolerance, s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D461/00A61K31/4375A61P7/02A61P9/00A61P25/28A61P25/14A61P25/00
Inventor 罗军徐丹周平
Owner 北京康瑞达彤科技有限公司
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