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Antithrombotic medicament for intravenous injection and preparation method and application thereof

A technology of antithrombotic drug and general formula, which is applied in the field of antithrombotic drug for intravenous injection and its preparation, can solve the problems of low purity and poor drug activity, achieve high purity, low degree of polymerization, and inhibit platelet aggregation and adhesion The effect of action

Active Publication Date: 2013-07-17
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The invention provides an antithrombotic drug for intravenous injection and its preparation method and application, which can solve the problems of low purity and poor drug activity in the prior art

Method used

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  • Antithrombotic medicament for intravenous injection and preparation method and application thereof
  • Antithrombotic medicament for intravenous injection and preparation method and application thereof
  • Antithrombotic medicament for intravenous injection and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: Preparation of oligomannuronic acid methyl sulfate sodium salt

[0042]The basic raw material used in this process is alginic acid (extracted from kelp produced in the north, M / G is 7:3), and the molecule of alginic acid is β-D-mannuronic acid linked by (1→4) ( A linear block compound formed by linking M) units with (1→4) linked α-L-pyranguronic acid (G) units, and MG mixed segments.

[0043] 1. Preparation of oligomannuronic acid

[0044] A. Hydrolysis: Take 100g of food-grade alginate produced in the north, prepare a uniform glue solution with a concentration of 2% (W / V) with water, stir and reflux for 10 hours in hydrochloric acid solution of 0.5mol / L, and then separate by centrifuge , take the sediment;

[0045] B. Classification: Dissolve the above precipitate in 0.8% Na 2 CO 3 In the aqueous solution, adjust the pH value to 2.85 with 0.5mol / L hydrochloric acid, separate the solution, and take the supernatant;

[0046] C. Secondary hydrolysis: Ad...

Embodiment 2

[0056] Embodiment 2: Preparation of oligomeric mannuronic acid propyl ester sulfate sodium salt

[0057] The difference between this example and Example 1 is that in the above-mentioned step 2 of the esterification, HCl-methanol is replaced by propylene oxide, and sodium hydroxide is used as a catalyst. Put 50g of oligomeric mannuronic acid into a three-necked reaction bottle, add 200mL of propylene oxide, stir, then add 0.3g of NaOH, stir for 6 hours, wash the reaction product with 95% ethanol three times, and dry under reduced pressure to obtain manna Propyl uronic acid ester. All the other steps are the same as in Example 1 to prepare oligomeric mannuronic acid propyl ester sulfate sodium salt.

Embodiment 3

[0058] Embodiment 3: Drug efficacy test of antithrombotic drug for intravenous injection

[0059] The main pharmacological activity experimental results of the oligomeric mannuronate propyl sulfate sodium salt obtained by applying the method of the present invention are as follows, and the following results are obtained through systematic experimental research according to the method stipulated by the state.

[0060] A, the anticoagulant efficacy result of the antithrombotic drug for intravenous injection of the present invention

[0061] Table 1 The effect of the new drug on the coagulation index of rabbits (X±S, n=6)

[0062]

[0063] * : vs normal saline * p** p*** p<0.001

[0064] #: vs 6.25mg / kg new drug #p<0.05##p<0.01###p<0.001

[0065] : All greater than 120 seconds

[0066] The results showed that the new drug could significantly prolong TT, CT, APTT, RT, and PT of rabbits. Tip: This drug has obvious anticoagulant effect.

[0067] B, the influence of antithr...

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Abstract

The invention provides an antithrombotic medicament for intravenous injection. The medicament is a modified acidic polysaccharide consisting of only one monosaccharide and has a structural general formula, wherein R is -CH3 or -CH2-CH(OH)-CH3; R' is -H or -SO3Na; each sugar ring has at least one R' which is -SO3Na; n is equal to 2 to 6; when R is -CH3, the compound represented by the structural general formula is an oligomannuronicacid methyl acetate sulfate sodium salt; and when R is -CH2-CH(OH)-CH3, the compound represented by the structural general formula is an oligomannuronicacid proply acetate sulfate sodium salt. The medicament for intravenous injection has obvious anticoagulation, wherein the anticoagulation titer is 17 to 23; rabbit collagen induced platelet aggregation and platelet adhesion are obviously inhibited; and local ischemic brain damage caused by formation of cerebral thrombosis is lessened by inhibiting the formation of cerebral thrombosis and ischemic brain tissues are obviously protected.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an antithrombotic drug for intravenous injection and its preparation method and application. Background technique [0002] The present invention relates to a novel mannuronic acid derivative. Patent No. ZL88109698.9 is an invention patent, which discloses a method for preparing mannuronic acid propyl ester sulfate. This approach demonstrates a general method for the preparation of such compounds. The compound produced by this method belongs to a series of heparin-like substances. During the preparation process, due to the different technical conditions in the important process links, such as the preparation, grading, esterification and sulfonation of mannuronic acid, a series of derivatives with different structures will be produced. Compounds with different structures also exhibit different biological activities. Therefore, the preparation method of the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H7/033
Inventor 管华诗于广利李桂玲江晓璐李春霞
Owner OCEAN UNIV OF CHINA
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