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Preparation method and composite of low-molecular heparin nanopolymer

A low-molecular-weight heparin and nano-polymer technology, which is applied in the field of preparation methods of low-molecular-weight heparin nano-polymers and composites thereof, can solve the problems of unsatisfactory effect, unreasonable preparation process and preparation components, and is easy to achieve oral absorption dose. Control, long action time, small particle size range effect

Inactive Publication Date: 2012-09-05
诸敏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this technology solves the problem of heparin with a strong negative charge, the preparation process and formulation components are unreasonable. Although it can solve certain absorption and stability problems, the effect is not ideal.

Method used

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  • Preparation method and composite of low-molecular heparin nanopolymer
  • Preparation method and composite of low-molecular heparin nanopolymer
  • Preparation method and composite of low-molecular heparin nanopolymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: The following part of this example describes a preparation method of a low-molecular-weight heparin nanopolymer.

[0031] First, 2000 ml of 0.4M acetic acid and 2000 ml of 0.2M sodium acetate solution were mixed at a volume ratio of 1:1 to prepare 4000 ml of acetate buffer. After such configuration, the pH value of the acetate buffer is below 6.4.

[0032] Dissolve 2g of trimethyl chitosan in the previously configured acetate buffer to form a chitosan solution. Chitosan can form a hydrogel under acidic conditions (pH<6.4), which has the characteristics of mucous membrane adsorption, which can promote the absorption of drugs in the digestive tract and improve the bioavailability of drugs.

[0033] Dissolve 2 g of low-molecular-weight heparin sodium with an average molecular weight of less than 6000 Da in 40 ml of distilled water to prepare a low-molecular-weight heparin solution.

[0034] Under the stirring of a magnetic stirrer, the above-mentioned low-mole...

Embodiment 2

[0035] Example 2: The following part of this example describes a preparation method of a low-molecular-weight heparin nanopolymer.

[0036] First, 1000 ml of 0.4M acetic acid and 1000 ml of 0.2M sodium acetate solution were mixed at a volume ratio of 1:1 to prepare 2000 ml of acetate buffer. After such configuration, the pH value of the acetate buffer is below 6.4.

[0037] Dissolve 1 g of PEGylated chitosan in the previously prepared acetate buffer to form a chitosan solution. Chitosan can form a hydrogel under acidic conditions (pH<6.4), which has the characteristics of mucous membrane adsorption, which can promote the absorption of drugs in the digestive tract and improve the bioavailability of drugs.

[0038] Dissolve 6 g of tinzaparin sodium with an average molecular weight of 6000 Da in 120 ml of distilled water to prepare a low molecular weight heparin solution.

[0039] Under the stirring of a magnetic stirrer, the above-mentioned low-molecular-weight heparin solutio...

Embodiment 3

[0040]Example 3: The following part of this example describes a preparation method of a low-molecular-weight heparin nanopolymer.

[0041] First, 5000 ml of 0.4M acetic acid and 5000 ml of 0.2M sodium acetate solution were mixed at a volume ratio of 1:1 to prepare 10000 ml of acetate buffer. After such configuration, the pH value of the acetate buffer is below 6.4.

[0042] Dissolve 5g of trimethyl chitosan in the previously configured acetate buffer to form a chitosan solution. Chitosan can form a hydrogel under acidic conditions (pH<6.4), which has the characteristics of mucous membrane adsorption, which can promote the absorption of drugs in the digestive tract and improve the bioavailability of drugs.

[0043] Dissolve 1 g of enoxaparin with an average molecular weight of less than 6000 Da in 20 ml of distilled water to prepare a low molecular weight heparin solution.

[0044] Under the stirring of a magnetic stirrer, the above-mentioned low-molecular-weight heparin solu...

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Abstract

The invention relates to a preparation method and a composite of a low-molecular heparin nanopolymer. The preparation method is applied to large-scale production of oral low-molecular heparin. The preparation method of the low-molecular heparin nanopolymer comprises the following steps: mixing acetic acid and a sodium acetate solution to prepare an acetate buffer; dissolving chitosan into the acetate buffer to prepare a chitosan solution; dissolving the low-molecular heparin into distilled water to prepare a low-molecular heparin solution; and dripping the low-molecular heparin solution into the chitosan solution under the stirring of a magnetic stirrer to obtain the low-molecular heparin nanopolymer. The low-molecular heparin nanopolymer obtained by using the preparation method has the advantages of reasonable prescription design, good oral administration absorption, long acting time and high entrapment rate, and is suitable for large-scale production.

Description

technical field [0001] The invention relates to a preparation method of low-molecular-weight heparin nanometer polymer and its compound, which are applied to the large-scale production of oral low-molecular-weight heparin. Background technique [0002] Low molecular weight heparin is mainly used in clinical prevention and treatment of thromboembolic diseases, and it is economical, safe and effective. Research on low molecular weight heparin is very popular at home and abroad, and relevant experts have been looking for an ideal oral preparation of low molecular weight heparin to meet the needs of patients. [0003] Low-molecular-weight heparin cannot be absorbed orally and can only be administered by deep subcutaneous injection, which brings inconvenience to patients. There are many reasons that hinder its absorption. For example, low-molecular-weight heparin is water-soluble and macromolecular, and it is generally difficult to penetrate biomembranes. The biggest obstacle is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K31/727A61P7/02
Inventor 诸敏
Owner 诸敏
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