Vinpocetine polymer micelle preparation and preparation method thereof

A technology of vinpocetine and polymer glue, which is applied in the field of vinpocetine polymer micelles and its preparation, can solve the problems of low bioavailability and poor solubility in water, and achieve improved solubility, small particle size and uniform distribution Effect

Active Publication Date: 2012-01-25
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a novel vinpocetine polymer micelle preparation according to the problems such as low bioavailability and poor solubility in water of the vinpocetine preparation prepared according to the prior art

Method used

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  • Vinpocetine polymer micelle preparation and preparation method thereof
  • Vinpocetine polymer micelle preparation and preparation method thereof
  • Vinpocetine polymer micelle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of drug-loaded polymer micelles by film hydration method

[0032] Accurately weigh 20 mg of PEG-PLA, put it into a 50 mL dry round-bottom flask, add 0.8 mL of 5 mg / mL vinpocetine / acetonitrile solution, add 3 mL of acetonitrile to dissolve, and shake to make the polymer and drug Disperse evenly in organic solution. The water bath was heated to 60 °C, and the organic solvent was removed by rotary evaporation under reduced pressure for 45 min at a speed of 75 r / min. Incubate at 70°C for 5 min to melt the solid skeleton membrane and obtain a transparent gel-like sample. Add 5 mL of deionized water at the same temperature, stir at the same temperature at a constant speed of 1900 r / min for 2 h to hydrate, cool to room temperature, place in a -20°C refrigerator for quenching, and filter out unwrapped particles with a 0.22 μm microporous membrane Add the lyoprotectant PEG3350 (representing a weight-average molecular weight of 3350) to the micelle solutio...

Embodiment 2

[0033] Example 2 Preparation of drug-loaded polymer micelles by solvent diffusion method

[0034] Accurately weigh 20 mg of PEG-PLA and 4 mg of vinpocetine, dissolve them in 0.5 mL of acetonitrile solution, slowly add them dropwise to 5 mL of deionized water at a magnetic stirring speed of 600 r / min, and place in a fume hood Stir at the same speed for 4 h, remove the organic solvent, place in the refrigerator to cool, filter with a 0.22 μm microporous membrane to remove uncoated drugs, add a lyoprotectant to the filtered micellar solution, and then freeze-dry to prepare Obtain vinpocetine micellar freeze-dried powder. The drug-loaded micelles prepared by the above micelles preparation method have a drug loading of 6.43%.

Embodiment 3

[0035] Example 3 Preparation of drug-loaded polymer micelles by dialysis

[0036] Precisely weigh 40 mg of PEG-PLA and 20 mg of vinpocetine and dissolve them in 10 mL of N, N-dimethylformamide (DMF), incubate in a constant temperature water bath at 45 °C for 5 min, stir magnetically to mix . The solution was transferred to a dialysis bag with a molecular weight cut-off of 3500, dialyzed in 2 L of deionized water, and replaced with fresh deionized water at 2 h, 4 h, 6 h, 8 h, 12 h, and 24 h. After the dialysis was completed, the solution in the dialysis bag was taken out, centrifuged at 3000 r / min for 10 min, the supernatant was filtered through a 0.22 μm microporous membrane, the lyoprotectant F68 was added to the filtered micellar solution, and then freeze-dried The vinpocetine micellar freeze-dried powder was prepared. The drug-loaded micelles prepared by the above micelles preparation method have a drug loading of 2.58%.

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Abstract

The invention discloses a vinpocetine polymer micelle preparation and a preparation method thereof, and belongs to the technical field of medicinal preparation. The vinpocetine polymer micelle preparation is formed by embedding vinpocetine into polyethylene glycol polylactic acid, wherein a mass ratio of the vinpocetine to the polyethylene glycol polylactic acid is (1-12):20; and the weight-average molecular weight of the polyethylene glycol polylactic acid is between 7,000 and 45,000, the molecular weight of polyethylene glycol is between 2,000 and 15,000, and the molecular weight of polylactic acid is between 5,000 and 30,000. In the preparation method, the vinpocetine polymer micelle preparation is prepared by a membrane hydration method which is subjected to condition screening, and hydration temperature, hydration time, administration dose and the like are limited optimally, so in the obtained vinpocetine polymer micelle preparation product, the defects of poor oral administration absorption and low bioavailability of the vinpocetine are overcome.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a vinpocetine polymer micelle and a preparation method thereof. Background technique [0002] Vinpocetine (vinpocetine) is from Apocynaceae small vinca ( Vinca minor The derivative of the indole alkaloid vincamine (vincamine) extracted in L. is a cerebral circulation metabolism improving agent developed by Hungary Gedeon Richter Company in the 1970s. This drug is used as the drug of choice for improving cerebral circulation. Treatment of cerebral infarction, sequelae of cerebral hemorrhage and cerebral arteriosclerosis and other types of circulatory disorders and cerebrovascular diseases. [0003] However, the liver cells in the human body have a strong metabolic effect on vinpocetine, and there is a serious first-pass effect in the liver. The main metabolite of the drug is apovincine, which is excreted by the kidneys. Low; and Vinpocetine is widely distributed in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4375A61K47/34A61P9/10
Inventor 杨帆黄淑玲谢华廷李嘉慧李桃黄志军
Owner GUANGDONG PHARMA UNIV
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