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Heparin complex as well as preparation method and application thereof

A complex and heparin technology, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, and emulsion delivery, etc., can solve the problems of the safety of heparin complexes and the unsatisfactory drug-carrying capacity of stable protein drugs.

Inactive Publication Date: 2010-07-07
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the safety, stability and drug-loading ability of the heparin complex prepared so far are still not ideal.

Method used

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  • Heparin complex as well as preparation method and application thereof

Examples

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preparation example Construction

[0030] The preparation method of the complex formed by grafting heparin onto the poloxamer utilizes the terminal hydroxyl group of the poloxamer and the active group of the carboxyl group or amino group in the heparin molecule. It can be a poloxamer or a poloxamer with a spacer molecule attached to the hydroxyl terminal carboxylation, and then react with the amino group of heparin; it can also be a poloxamer or a poloxamer with a spacer molecule attached to the hydroxyl terminal amino group and then react with the carboxyl group of heparin. Concrete reaction process is as follows:

[0031] a. Carboxylation of poloxamer or poloxamer with inter-arm molecules at the hydroxyl end, followed by reaction with the amino group of heparin

[0032] A certain amount of poloxamer or poloxamer, succinic anhydride, 4-dimethylaminopyridine, and triethylamine that are connected with spacer molecules are placed in dioxane, stirred and reacted overnight, and the resulting reactant The terminal...

Embodiment 1

[0041] Example 1. Synthesis of low molecular weight heparin-poloxamer and its anticoagulation experiment in vitro

[0042] 1-1. Synthesis of low molecular weight heparin-poloxamer-low molecular weight heparin

[0043] Weigh 12 g of Poloxamer 407 (relative molecular weight M=12000, where a=c=101, b=56), and add 2 mmol of succinic anhydride and 2 mmol of 4-dimethylaminopyridine to a round bottom flask and 0.55ml triethylamine, and dissolved in 200ml dioxane, stirred for 24h to obtain poloxamer with a carboxyl group at the end, using it as a reactant, using 1-ethyl-3,3-dimethylammonia Propylcarbodiimide (EDC) / N-hydroxyl diimide (NHS) method, add 10g of low molecular weight heparin sodium, and stir for 24 hours. The reaction product was dialyzed through a dialysis bag for 3 days, and the obtained product was freeze-dried to obtain a solid powder, that is, low molecular weight heparin-poloxamer-low molecular weight heparin.

[0044] 1-2. In vitro anticoagulation experiment of low...

Embodiment 2

[0049] Example 2. Preparation of low molecular weight heparin-poloxamer complex micelles

[0050] Take 50 mg of low molecular weight heparin-poloxamer-low molecular weight heparin prepared above, disperse in 20ml of distilled water, and ultrasonically treat at 37°C for 2 minutes to form a micellar suspension, then freeze-dry to make a solid freeze-dried product, According to the in vitro anticoagulant experiment in Example 1, the low molecular weight heparin-poloxamer complex micelles have anticoagulant effect and can be used alone or as a pharmaceutical adjuvant in thrombolytic preparations.

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Abstract

The invention relates to a heparin complex which has the following general formula: Y-X-Y or Y-g-X-g-y or X-Y or X-g-Y, wherein x is poloxamer, g is spacer-arm molecules, Y is heparin, and X, g, Y or X, Y are combined by covalent bonds. The invention also provides a preparation method of the heparin complex. The heparin complex can be applied as pharmaceutical excipients or conveying vectors.

Description

【Technical field】 [0001] The invention relates to a heparin compound and its preparation method and application, in particular to a covalently grafted heparin compound and its preparation method and application. 【Background technique】 [0002] Heparin is an anionic mucopolysaccharide with anticoagulant and antithrombotic activity【Kwon OH, NhoYC et al.Biocompatible surfaces by immobilization of heparin on diamond-likecarbon films deposited on various substrates.Surf.Interface Anal.2000,29 :386]. Low-molecular-weight heparin (LMWH) is a low-molecular-weight heparin fragment obtained by degradation of heparin or a low-molecular-weight heparin component obtained by a fractionation method. The relative molecular mass range is generally 3000-8000. disease. [0003] The complex formed by covalently grafting heparin onto the material has many advantages, such as achieving the purpose of immobilizing heparin and effectively preventing heparin from being taken away by the blood flow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K9/10A61K9/107A61K9/127
Inventor 赵应征田吉来李校堃鲁翠涛张翼高慧升周志彩唐琴琴靳卓徐艳艳
Owner WENZHOU MEDICAL UNIV
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