Sodium alginate sulfuric ester and preparation method and use thereof

A technology of sodium alginate and sulfuric acid ester, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, extracellular fluid diseases, etc., and can solve problems such as high prices and insufficient sources

Inactive Publication Date: 2004-11-03
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But very expensive due to insufficient sources

Method used

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  • Sodium alginate sulfuric ester and preparation method and use thereof
  • Sodium alginate sulfuric ester and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Add 10g of sodium alginate containing 80ml of formamide and 20ml of ClSO 3 In the sulfation reagent of H, stir at 60°C for 4 hours to obtain a brown-red solution, add an appropriate amount of deionized water, dialyze for 3 days, dissolve and shrink to dryness to obtain 15 g of sulfated sodium alginate. The sample S% is 13.21%, C%, H% are 21.05% and 1.93%, respectively. The degree of substitution of sulfate ester groups was calculated to be 1.41 / uronic acid unit (assuming that both sulfate and carboxyl groups form sodium salts). Infrared detection appears 1250cm -1 and 800cm -1 The vibration peak of the sulfate ester group. Permeation gel chromatography test has a retention time of 7.51 minutes, and the test conditions are: gel column TSKG3000-PW, mobile phase 0.1mol / L NaCl aqueous solution, flow rate 1.0mL / min, column temperature 30°C, and the refractive index detects the sample. The concentration of the sample is 0.4%, which is calibrated by the Pullulan standard s...

Embodiment 2

[0023] Add 10g sodium alginate containing 80ml formamide and 4mlClSO 3 In the sulfation reagent of H, stir at 40°C for 4 hours to obtain a brown-red solution, add an appropriate amount of deionized water, dialyze for 3 days, dissolve and shrink to dryness to obtain 12 g of sulfated sodium alginate. The sample S% is 5.69%, C%, H% are 30.78% and 3.03%, respectively. The degree of substitution of sulfate ester groups was calculated to be 0.41 / uronic acid unit (assuming that both sulfate and carboxyl groups form sodium salts). Infrared detection appears 1250cm -1 and 800cm -1 The vibration peak of the sulfate ester group. Permeation gel chromatography test has a retention time of 7.21 minutes, and the test conditions are: gel column TSKG3000-PW, mobile phase 0.1mol / L NaCl aqueous solution, flow rate 1.0mL / min, column temperature 30°C, and the refractive index detects the sample. The concentration of the sample is 0.4%, which is calibrated by the Pullulan standard sample provid...

Embodiment 3

[0025] Add 10g of sodium alginate containing 80ml of formamide and 30ml of ClSO 3 In the sulfation reagent of H, stir at 60°C for 4 hours to obtain a brown-red solution, add an appropriate amount of deionized water, dialyze for 3 days, dissolve and shrink to dryness to obtain 15 g of sulfated sodium alginate. The sample S% is 14.28%, C%, H% are 19.75% and 1.90%, respectively. The degree of substitution of sulfate ester groups was calculated to be 1.63 / uronic acid unit (assuming that both sulfate and carboxyl groups form sodium salts). Infrared detection appears 1250cm -1 and 800cm -1 The vibration peak of the sulfate ester group. Permeation gel chromatography test has a retention time of 7.71 minutes, and the test conditions are: gel column TSKG3000-PW, mobile phase 0.1mol / L NaCl aqueous solution, flow rate 1.0mL / min, column temperature 30°C, and the refractive index detects the sample. The concentration of the sample is 0.4%, which is calibrated by the Pullulan standard s...

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Abstract

The present invention discloses one kind of new compound sodium alginate sulfate and its preparation. The preparation process includes adding ad alginate into sulfatizing reagent, reaction at 40-70 deg.c to obtain reddish brown solution, dialysis and concentration to obtain sodium alginate sulfate. The in vitro blood coagulation with the obtained sodium alginate sulfate shows that it has very high anticoagulant activity and has APTT value reaching the level of haparin in the said concentration, so that sodium alginate sulfate may be used as anticoagulant in preparing blood coagulation resisting medicine.

Description

technical field [0001] The invention relates to a new compound-sodium alginate sulfate and its preparation method and application, which belongs to the field of chemical biology of renewable resources and also belongs to the field of organic chemistry. Background technique [0002] Heparin is an anticoagulant drug that has been used for over 50 years (Crafoord, C.; Jorpes E. 1941, JAMA 116:2831). It is a linear polysaccharide with a backbone mainly composed of disaccharide repeating units composed of α-D-glucosamine and α-L-iduronic acid, containing some sulfate and carboxyl groups (Paulo, A.S.M.; Mariana, S.P., 1999, TCM, 9(8), 227-232). But it is very expensive due to insufficient sources. Sodium alginate is a polysaccharide proposed from brown algae. It has a wide range of sources and is cheap. It is widely used in the preparation of microspheres, microcapsules and tablets in drug sustained-release systems. It has long-term sustained-release effects and can reduce certa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/734A61P7/02C08B37/04
Inventor 杜予民黄荣华杨建红
Owner WUHAN UNIV
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