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A kind of vinpocetine tubular crystal and preparation method thereof

A vinpocetine and tubular technology, which is applied in the field of vinpocetine tubular crystals and its preparation, can solve the problems of cumbersome process, low bioavailability, and large particles, and achieve simple production process, good bioavailability, and high specific surface area Effect

Active Publication Date: 2017-03-01
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent aims at the disadvantages of vinpocetine, such as low purity, large particles, poor powder quality, poor product stability, long production cycle, etc., through a series of elution, concentration, cooling and purification of vinpocetine, and then drying, airflow ultra-fine grinding, freezing After drying, a special ultrafine freeze-dried preparation is prepared
The vinpocetine prepared by this patent has the advantages of good solubility and good biological activity. However, the scheme has successively undergone jet milling, dissolving with water for injection, low-temperature pre-cooling, low-temperature decompression drying and high-temperature drying. The process is cumbersome and the flow Complicated and expensive to produce
In addition, the pre-cooling process requires a temperature as low as -35°C, and the vacuum degree of the decompression drying process is about 0.08 MPa, both of which require a large amount of energy; jet milling, low-temperature pre-cooling and decompression processes require more equipment and consume more energy. , which not only increases the cost input but also does not conform to the economic intensive and resource-saving industrial development model, and is not suitable for mass industrial production
[0007] Publication number is that the Chinese patent of 102327208 discloses the preparation method of vinpocetine polymer micelle preparation, uses PEG-PLA (polyethylene glycol-polylactic acid) as carrier material burden vinpocetine to form polymer micelle, improves existing Problems such as low bioavailability and low dissolution rate of vinpocetine preparations in water
However, the disadvantages of this patent are also obvious. As one of the carriers, polyethylene glycol is mainly excreted and cleared through the kidneys. Although polyethylene glycol and polylactic acid are relatively less toxic to the human body, their metabolic process in the human body is still invisible. Increased the load on human organs (especially the kidneys)
At the same time, solvents such as dichloromethane, acetonitrile, and acetone are used in the patented process, which are solvents that need to be restricted in the drug preparation process, and the requirements for their residues are relatively strict, which increases the difficulty of technical utilization

Method used

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  • A kind of vinpocetine tubular crystal and preparation method thereof
  • A kind of vinpocetine tubular crystal and preparation method thereof
  • A kind of vinpocetine tubular crystal and preparation method thereof

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Experimental program
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Effect test

specific Embodiment approach

[0037] 1). Add vinpocetine to the solvent, start stirring at 100-800rpm, the optimum is 200rpm to raise the temperature to 40-95°C, the optimum is 50°C to dissolve it, and the obtained concentration ranges from 16mg / ml to 50mg / ml ml of vinpocetine solution, the optimum is 30mg / ml;

[0038] 2). Add water to the above solution at a certain speed, filter and wash at a constant temperature for 5-60 minutes, dry in a vacuum oven at 20-80°C for 2-8h, the optimum drying temperature is 40°C, and the optimum drying time is 4h. Obtain vinpocetine tubular crystals;

[0039] The solvent described in step 1) is the mixture of one or more in methanol, ethanol, propanol, isopropanol, ethyl acetate, the most optimal is methanol, ethanol, propanol, isopropanol, ethyl acetate single solvent;

[0040] The water in step 2) is a poor solvent, and the volume ratio of the poor solvent to the solvent used should be 0.5 to 5, preferably 2;

[0041] The adding rate of water in step 2) is 10ml / min-36...

Embodiment 1

[0044] 1) Add 160mg of crude vinpocetine to 10ml of absolute ethanol, start stirring at 100rpm, and heat up to 40°C to completely dissolve.

[0045] 2) Add 5ml of water (volume ratio: water / absolute ethanol = 0.5 / 1) to the dissolved solution at a rate of 10ml / min, white crystals are precipitated, grown at constant temperature for 5min, filtered, and vacuum-dried at 20°C for 4h. Obtain tubular crystal vinpocetine, its appearance is as attached figure 1 shown.

Embodiment 2

[0047] 1) Add 300mg of crude vinpocetine to 10ml of absolute ethanol, start stirring at 200rpm, and heat up to 50°C to completely dissolve.

[0048] 2) Add 20ml of water (volume ratio: water / absolute ethanol = 2 / 1) to the dissolved solution at a rate of 150ml / min, white crystals are precipitated, grown at constant temperature for 20min, filtered, and vacuum-dried at 40°C for 4h. Obtain tubular crystal vinpocetine, its appearance is consistent with embodiment 1, as attached figure 1 shown.

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Abstract

The invention relates to a vinpocetine tubular crystal and a preparation method thereof. The vinpocetine tubular crystal is prepared by the following steps: adding vinpocetine to a solvent, starting for stirring at a speed of 100-800rpm, increasing temperature to 40-95 DEG C so as to enable the vinpocetine to be dissolved to obtain a 16-50mg / ml vinpocetine solution; and adding water to the solution, filtering and washing after the temperature is kept constant for 5-60min, and drying for 2-8h in a vacuum drying box at 20-80 DEG C so as to obtain the vinpocetine tubular crystal. The vinpocetine product prepared by the invention is of a crystal structure which has closed or non-closed channels; the yield is 60-85%, bulk density is 0.25-0.4g / ml and the dissolution rate is increased by 20-40%; the tubular crystal, applied to the field of medicine, is capable of improving the problem of low dissolution rate of the vinpocetine in the water, promoting medicine absorption and enhancing the medicine efficiency and the bioavailability. The preparation method, which is capable of preparing the vinpocetine tubular crystal by a simple one-step dissolving process, is simple in production process and easy to implement industrial production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a vinpocetine tubular crystal and a preparation method thereof. The dissolution rate of the vinpocetine tubular crystal is increased by 20% to 40%, thereby promoting drug absorption and improving drug efficacy. The method adopts dissolution and crystallization, the dissolution process is rapid, the operation steps are simple, the solvent is green and environmentally friendly, no new impurities are introduced, and the product performance is significantly improved. Background technique [0002] Vinpocetine, an indole alkaloid, is a derivative of vincamine, the English name is Vinpocetine, and the chemical name is ethyl(13as,13bs)-13a-ethyl-2,3,5,6-13a,13 , sub-b hexahydro-1H-indole[3,2,1-de]pyridine[3,2,1-ij][1,5]-naphthalene-12-carboxylic acid, the molecular formula is C 22 h 26 N 2 o 2 , with a molecular weight of 350.45. Vinpocetine is a natural product extracted from the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D461/00
CPCC07B2200/13C07D461/00
Inventor 龚俊波王海洋杜艳妮刘玉敏王静康尹秋响张美景侯宝红
Owner TIANJIN UNIV