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Preparation method of enoxaparin sodium microspheres

A technology of enoxaparin sodium and microspheres, which is applied in the production of enoxaparin sodium microspheres and the field of preparation of enoxaparin sodium microspheres, which can solve the problem of affecting anticoagulation, unstable chemical properties of heparin, and restrictions on human epithelial or mucous membranes. Absorption and other problems, to achieve good biocompatibility, reduce microsphere perforation, high sample loading and encapsulation efficiency

Active Publication Date: 2019-01-08
江西浩然生物制药有限公司
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

However, the clinical application of this approach is limited, and the main obstacles to oral administration are: (1) the existence of heparinase in the human liver and intestinal microflora, which will degrade a large amount of heparin; (2) the acidic environment in the stomach causes heparin Chemical properties are unstable; (3) low molecular weight heparin sodium has the characteristics of hydrophilicity, negative charge and large molecular weight, which limits the absorption of human epithelial or mucous membranes, thus affecting its continuous anticoagulant effect

Method used

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Embodiment approach

[0020] The embodiment of the present invention is as follows: a preparation method of enoxaparin sodium microspheres, which uses PLGA (polyester obtained by condensation of lactic acid and glycolic acid) (50:50) as the carrier material, and enoxaparin sodium microspheres Its main steps are: add enoxaparin sodium aqueous solution to PLGA dichloromethane solution to form colostrum; add colostrum to PVA (polyvinyl alcohol) aqueous solution to form double emulsion; carry out vacuum drying at room temperature to obtain Enoxaparin Sodium Microspheres. The method is safe, non-toxic, stable and easy to operate. The enoxaparin sodium microspheres prepared by the invention have uniform particle size, high drug loading and encapsulation efficiency, and good biocompatibility, and are the first enoxaparin sodium nano-microspheres in China that can be administered orally and have a slow-release effect.

example 1

[0022] (1) Add 30g of PLGA (microsphere carrier material PLGA, which is a polylactic acid-glycolic acid copolymer) into 2L of dichloromethane at 0-10°C, and stir until fully dissolved;

[0023] (2) Take 100g of enoxaparin sodium and dissolve it in 400ml of ultrapure water;

[0024] (3) Add the solution obtained in (1) into the solution obtained in (2) dropwise at 0-10°C, stirring at 1000 rpm during the process, and keep stirring for 20 minutes after the process to form colostrum. This step is carried out in three-necked flask;

[0025] (4) Add 3kg of PVA (polyvinyl alcohol) into 30L of ultrapure water at 95°C, stir until the solution is clear, and cool to 0-10°C; this step is carried out in a reactor;

[0026] (5) Add colostrum into the solution obtained in (4) under the condition of 0-10°C, and stir at 1000 rpm during the process, and keep stirring for 30 minutes after the process ends;

[0027] (6) The rotating speed is adjusted to 125rpm, the reaction temperature is adjus...

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Abstract

The invention relates to a preparation method of enoxaparin sodium microspheres. According to the method, PLGA (polyester formed by performing condensation on lactic acid and glycolic acid (50:50)) asa carrier material, and micro-spheroidization is performed on enoxaparin sodium. The method comprises the following main steps: adding an enoxaparin sodium aqueous solution into a PLGA dichloromethane solution to form colostrum; adding the colostrum into a PVA (polyvinyl alcohol) aqueous solution to form multiple emulsion; performing vacuum drying at normal temperature to form the enoxaparin sodium microspheres. The method is safe and non-toxic, good in stability, and convenient to operate. The formed enoxaparin sodium microspheres are uniform in particle sizes, high in drug loading capacityand encapsulation efficiency and good in biocompatibility, and are the enoxaparin sodium microspheres, which can be taken orally and have a slow release effect, initiated domestically.

Description

technical field [0001] The invention belongs to the technical field of biopolymer material processing, and relates to a process for producing enoxaparin sodium microspheres, in particular to a preparation method of enoxaparin sodium microspheres. Background technique [0002] Enoxaparin sodium (Enoxaparin sodium) is a low molecular weight heparin, which is a mixture obtained by β-elimination degradation of high-quality heparin sodium. Compared with other low molecular weight heparins, enoxaparin sodium has lower average molecular weight (4500Da), longer half-life (4.5h), and higher bioavailability (nearly 100%). Enoxaparin sodium is usually used to prevent and treat deep venous thrombosis, pulmonary embolism and other diseases. It has many clinical indications, definite curative effect, less side effects, and is safe and convenient to use, so it has a large market demand. Because enoxaparin sodium will be degraded into inactive small fragments after oral administration, it ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34A61K31/727A61P7/02
CPCA61K9/5031A61K31/727A61P7/02
Inventor 万偲胡著阳魏超娟李国龙纪明妹
Owner 江西浩然生物制药有限公司
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