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Vinpocetine composition and preparation method thereof

A technology of vinpocetine and injection, applied in the field of pharmaceutical preparations, can solve problems such as toxic side effects and physical damage, and achieve the effects of changing the color of the solution, reducing dosage, and improving irritation

Active Publication Date: 2013-07-31
HENAN RUNHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, benzyl alcohol, propylene glycol and other vascular stimulating regulators have certain toxic and side effects, which are prone to gluteal muscle contracture and cause varying degrees of damage to the patient's body.

Method used

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  • Vinpocetine composition and preparation method thereof
  • Vinpocetine composition and preparation method thereof
  • Vinpocetine composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The vinpocetine composition of the present embodiment consists of:

[0032] Vinpocetine 10g Ascorbic acid 0.3g

[0033] Sodium Metabisulfite 2g Tartaric Acid 6g

[0034] Sorbitol 160g

[0035] Make injection 2000ml altogether.

[0036] The preparation method is as follows:

[0037] (1) Take 80% of the amount of water for injection to filter and deoxygenate, heat to 40°C, add ascorbic acid, tartaric acid and sodium metabisulfite, stir to dissolve completely;

[0038] (2) Add Vinpocetine, stir, and dissolve completely;

[0039] (3) Add sorbitol, stir and dissolve, make up water for injection, and use 0.3% activated carbon to stir and adsorb;

[0040] (4) Sterilize for 15 minutes at a temperature of 121°C, and fill with nitrogen.

Embodiment 2

[0042] The vinpocetine composition of the present embodiment consists of:

[0043] Vinpocetine 12g Ascorbic acid 0.1g

[0044] Sodium Metabisulfite 2g Tartaric Acid 8g

[0045] Sorbitol 160g

[0046] Make injection 2000ml altogether.

[0047] The preparation method is as follows:

[0048] (1) 80% of the amount of water for injection is filtered to remove oxygen, heated to 45 ° C, added ascorbic acid, tartaric acid and sodium metabisulfite, stirred to dissolve completely;

[0049] (2) Add Vinpocetine, stir, and dissolve completely;

[0050] (3) Add sorbitol, stir and dissolve, make up water for injection, and use 0.3% activated carbon to stir and adsorb;

[0051] (4) Sterilize at 121°C for 15 minutes and fill with nitrogen.

Embodiment 3

[0053] The vinpocetine composition of the present embodiment consists of:

[0054] Vinpocetine 20g Ascorbic acid 0.45g

[0055] Sodium Metabisulfite 2g Tartaric Acid 15g

[0056] Sorbitol 160g was made into 2000ml of injection.

[0057] The preparation method is as follows:

[0058] (1) 80% of the amount of water for injection is filtered to remove oxygen, heated to 50 ° C, added ascorbic acid, tartaric acid and sodium metabisulfite, stirred to dissolve completely;

[0059] (2) Add Vinpocetine, stir, and dissolve completely;

[0060] (3) Add sorbitol, stir and dissolve, make up water for injection, and use 0.3% activated carbon to stir and adsorb;

[0061] (4) Sterilize at 121°C for 15 minutes and fill with nitrogen.

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Abstract

The invention relates to a vinpocetine composition and a preparation method thereof. The vinpocetine composition comprises 10 to 20 parts of vinpocetine, 0.1 to 0.45 parts of ascorbic acid, 1 to 5 parts of one or more antioxidants, 6 to 15 parts of one or more cosolvents, 120 to 180 parts of one or more physical stabilizers and 2000 parts of water. Compared with the prior art, the preparation method realizes that under the same conditions, vinpocetine degradation products of the vinpocetine composition are not increased obviously and ascorbic acid degradation products are reduced greatly and a solution color is improved obviously. The preparation method avoids a vascular stimulation conditioning agent frequently used in an injection. Through adjusting a pH value, ion intensity and a use amount of a physical stabilizer according to a result of analysis of vinpocetine stimulation production reasons, and especially using the principle that a large amount of sorbitol can wrap vinpocetine thereby avoiding stimulation production, the preparation method produces the vinpocetine composition which does not contain a vascular stimulant and does not produce stimulation on human blood vessels.

Description

technical field [0001] The invention relates to a vinpocetine composition and a preparation method of the composition, belonging to the field of pharmaceutical preparations. Background technique [0002] Vinpocetine, whose chemical name is ethyl(13as,13bs)-13a-ethyl-2,3,5,6-13a,13bhexahydro-1H-indole[3,2,1-de]pyridine[ 3,2,1-ij][1,5]naphthalene-12-carboxylic acid. Its chemical structural formula: [0003] [0004] Molecular formula: C 22 h 26 N 2 o 2 [0005] Molecular weight: 350.46 [0006] Vinpocetine is an indole alkaloid. A large number of scientific studies have confirmed that it can selectively improve the blood circulation of the brain, promote the energy metabolism of the brain, regulate the function of the neurotransmitter system, and protect the brain from deficiency in many aspects. The damage caused by blood hypoxia is especially suitable for the treatment of cardiovascular and cerebrovascular diseases, and it also has a significant effect on brain di...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61K47/22A61P9/00A61P9/10
Inventor 吴素林张炜靳勇
Owner HENAN RUNHONG PHARMA
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