Cardiovascular pharmaceutical formulation preparation method and uses

A pharmaceutical preparation and cardiovascular technology, applied in the field of cardiovascular pharmaceutical preparation preparation, can solve the problems of long tablet disintegration time, inability to directly prepare water-soluble injections, strong hydrophobicity, etc.

Inactive Publication Date: 2008-05-07
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current market has only oral solid preparations, because acetaloflavone is insoluble in water, strong hydrophobicity, long disintegration time of tablets, poor absorption, etc. (Chinese patent CN1490000A), it is impossible to directly prepare water-soluble injections, so far there is no Oral preparations that enhance its water solubility and reduce absorption differences have not been reported in the literature to prepare easily soluble aceflavone injections, nor have prepared easily soluble aceflavone complexes or clathrates, and clarified their use.

Method used

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  • Cardiovascular pharmaceutical formulation preparation method and uses
  • Cardiovascular pharmaceutical formulation preparation method and uses
  • Cardiovascular pharmaceutical formulation preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Acetaloflavone Complex Injection:

[0039] Acetaloflavone (calculated as isorhamnetin 99.8%) 10g

[0040] Sodium hydroxide 2g

[0041] Sodium citrate amount

[0042] Citric acid amount

[0043] Sodium sulfite 0.1g

[0044] Add water for injection to 1000ml

[0045] In the preparation container, add 80% water for injection of the preparation amount. Saturate with nitrogen, add the prescribed amount of sodium hydroxide to dissolve, then stir the prescribed amount of aceflavone to dissolve, filter, add sodium sulfite to stir to dissolve, and then adjust the pH to 7.5-1 with citric acid and sodium citrate 1.0, add water for injection saturated with nitrogen to a sufficient amount,

[0046] The sample was kept at room temperature for 12 months. There was no significant change in content and related substances, and the clarity and stability were good, which met the quality requirements for injections in the Chinese Pharmacopoeia 2000 edition.

Embodiment 2

[0048] Acetaloflavone Complex Injection:

[0049] Acetaloflavone (calculated as isorhamnetin) 10g

[0050] Sodium carbonate 20g

[0051] Sodium citrate amount

[0052] Citric acid amount

[0053] Sodium sulfite 0.1g

[0054] Add water for injection to 2000ml

[0055] In the preparation container, add 80% water for injection of the preparation amount. Saturate with nitrogen, add sodium carbonate to dissolve, then heat and stir aceflavone to dissolve in it, filter, add sodium sulfite and stir to dissolve, then adjust the pH to 7.5-11.0 with citric acid and sodium citrate, add saturated nitrogen injection Water to a sufficient amount, filter with a vertical fusing glass funnel or a membrane filter, measure the content of the intermediate, potting under nitrogen flow, each anatomy potting 2 ~ 10ml, and sterilize with steam at 100°C for 15-30 minutes. .

Embodiment 3

[0057] Acetaloflavone Complex Sodium Chloride Infusion:

[0058] Acetaloflavone (calculated as isorhamnetin) 20mg, trisodium citrate dihydrate 10mg, nicotinamide 10mg, L-ornithine 1.8g, 3-hydroxypropyl β-cyclodextrin 10mg, malic acid amount, Calcium edetate sodium 2mg, appropriate amount of sodium chloride to adjust isotonicity

[0059] Add water for injection to 100ml.

[0060] In the preparation container, add fresh water for injection, nitrogen saturation, add the prescribed amount of sodium citrate trisodium dihydrate, nicotinamide, calcium sodium edetate, L-ornithine, 3-hydroxypropyl β- After the cyclodextrin is dissolved, add the prescribed amount of acetaloflavone, stir, filter, and add 0.1% (g / ml) activated carbon of the concentrated solution at the same time, mix well, heat and boil for about 15 minutes, filter while hot to decarbonize . Dilute the filtrate with nitrogen-saturated water for injection to the required amount, adjust the pH to 8.0-11.0 with malic acid...

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PUM

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Abstract

Disclosed is a preparation for treating cardiovascular and cerebrovascular diseases, its preparing process and use, wherein the preparation comprises hippophe flavone, pharmaceutically acceptable inorganic bases and organic bases, or water-soluble inclusion compound formed from hippophe flavone and cyclodextrin, or low-molecular-weight alcohols, polysorbate, polyethylene glycol and poloxamer. The use of the hippophe flavone compound and preparation is also disclosed.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a preparation method and application of cardiovascular drug preparations. Preparation method and application of cardiovascular drug preparation. Background technique [0002] Acetaloflavone is a flavonoid compound extracted, separated and refined from the natural plant Hippophae rhamnoides. Its main active ingredients are isorhamnetin, quercetin, isorhamnetin-3-glucoside and other flavonoid compounds. It can increase the blood flow of the myocardium and brain tissue of experimental animals, reduce the oxygen consumption of the myocardium, improve the ability to withstand hypoxia, and improve the arrhythmia and cell damage caused by heart and brain ischemia; reduce the content of serum cholesterol and low-density lipoprotein; dilate Blood vessels, lower blood pressure; inhibit platelet aggregation, reduce blood viscosity. The current market has only oral solid preparations, be...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K31/7048A61K9/08A61K9/14A61K9/19A61P9/12A61P9/10A61P9/04A61P13/12A61P3/10
Inventor 刘力
Owner 刘力
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