Notoginsenoside sodium freezing-dried emulsion and preparation method thereof

A technology of sodium aescinate and freeze-dried emulsion, which is applied in anti-inflammatory agents, anti-toxic agents, pharmaceutical formulas, etc., can solve the problems of long-lasting biological effects and no literature reports, and facilitate industrial production and improve body resistance. Acceptability and the effect of ensuring safety

Inactive Publication Date: 2007-12-12
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The half-life of sodium aescinate is only 1.5 hours, but because it can promote the body to increase the secretion of ACTH and prostaglandin F2a, the biological effect lasts for a long time. After 16 hours of intravenous injection, it still has anti-exudation and detumescence effects
In order to alleviate the irritation of s...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Dissolve 200mg of sodium aescinate and 20g of β-cyclodextrin in 25ml of water, stir, and sonicate (please provide the conditions for sonication) to make the inner water phase; take 4g of soybean lecithin and dissolve it in 55ml of absolute ethanol to make the oil phase Add the inner water phase to the oil phase and stir magnetically at 20°C to obtain colostrum, take 0.5g of poloxamer and 2ml of glycerin and dissolve them in 150ml of water, add the colostrum and stir with a tissue grinder to make double milk, and decompress Ethanol was distilled off, and the double emulsion was homogenized repeatedly by a high-pressure homogenizer to obtain a finely dispersed emulsion; 20 g of mannitol was added to dissolve, and the water was removed by freeze-drying to obtain a dried sodium aescinate freeze-dried emulsion.

Embodiment 2

[0040]Dissolve 100 mg of sodium aescinate, 4 g of gelatin, and 8 g of gum arabic in 30 ml of water and stir to make an inner water phase; take 0.5 g of cephalin and dissolve it in 55 ml of absolute ethanol to make an oil phase; add the inner water phase to the oil phase Stir magnetically at 38°C to obtain colostrum, take 0.1g of poloxamer and 2ml of glycerin and dissolve it in 150ml of water, add colostrum and stir with a tissue masher to make double milk, distill under reduced pressure to remove ethanol, and then homogenize by high pressure The double emulsion was repeatedly creamed by a quality machine to obtain a finely dispersed emulsion; 25g of sucrose was added to dissolve it, and the water was removed by freeze-drying to obtain a dry freeze-dried emulsion of sodium aescinate.

Embodiment 3

[0042] Dissolve 100mg of sodium aescinate and 250g of β-cyclodextrin in 300ml of water, stir and ultrasonically dissolve to make an inner water phase; take 100g of phosphatidylethanolamine and dissolve it in 450ml of absolute ethanol to make an oil phase; add the inner water phase to Stir magnetically in the oil phase at 80°C to obtain colostrum, take 5g of poloxamer and 20ml of glycerin and dissolve it in 1000ml of water, add colostrum and stir with a tissue masher to make double milk, distill under reduced pressure to remove ethanol, and then pass through high-pressure The homogenizer was used to repeatedly milk evenly to obtain a finely dispersed emulsion; 200 g of mannitol was added to dissolve it, and the water was removed by freeze-drying to obtain a dry freeze-dried emulsion of sodium aescinate.

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Abstract

An escin sodium lyophilization dry emulsion for injection comprises therapeutically-effective amount of escin sodium and carrier material comprising phospholipid, emulsifying agent, water-soluble adjuvant and freeze-dried stabilizer. Its preparation method comprises preparing escin sodium into internal water phase, adding organic phase containing phospholipid, preparing into colostrum, adding outer water phase, preparing into emulsion of w/o/w, adding freeze-dry protective agent, and freeze-drying into solid.Berore application, water for injection is added as required for hydration, and oscillating, and emulsion is otbtained after recovery. The escin sodium lyophilization dry emulsion for injection has the advantages of reduced stimulatory function, increased toleration of clinical application and stability of medicament due to the protection of water-soluble stabilizer in adjuvant and phospholipid, thereby avoiding direct contact of lyophilization dry emulsion with wall of blood vessel.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a freeze-dried emulsion of sodium aescinate and a preparation method thereof. Background technique [0002] Sodium aescinate is a triterpenoid saponin containing ester bonds extracted from the dried mature seeds of the plant Aesculus aesculus. The main ingredients are sodium aescinate A and sodium aescinate B, which have the functions of reducing swelling, anti-exudation, anti-inflammation, improving blood circulation and increasing venous tension. Sodium aescinate can promote the body to increase the plasma concentration of ACTH and cortisone, can promote the secretion of PGF2α in the blood vessel wall, and can remove free radicals in the body, thereby anti-inflammation, anti-exudation, increase venous tension, and accelerate venous blood flow , Promote lymphatic return, improve blood circulation and microcirculation, and protect blood vessel walls. The h...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/107A61K47/44A61K47/40A61P29/00A61P39/06A61P7/10A61P7/04A61P9/10A61P13/12
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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