Calcium heparin liposome preparation for injection

A technology of liposome preparation and heparin calcium, applied in the field of medicine, can solve the problem that no heparin calcium liposome preparation for injection is put on the market, the encapsulation rate of low molecular weight heparin nanoliposome is low, and no heparin calcium liposome is found. It can improve the bioavailability, good encapsulation efficiency and stability, and improve the quality of preparation products.

Inactive Publication Date: 2012-07-11
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low molecular weight heparin nano-liposome encapsulation efficiency obtained by the above method, it cannot reach the 80% standard stipulated in the "Chinese Pharmacopoeia"
[0008] Therefore, there is no bibliographical report on the heparin calcium liposome preparation for injection at present, and there is no heparin calcium liposome preparation for injection on the market.

Method used

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  • Calcium heparin liposome preparation for injection
  • Calcium heparin liposome preparation for injection
  • Calcium heparin liposome preparation for injection

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preparation example Construction

[0063] On the other hand, the present invention also provides a preparation method of heparin calcium liposome preparation for injection, which specifically includes the following preparation steps:

[0064] (1) Cholesterol, phosphatidylglycerol, lecithin and polyoxyethylene 40 hydrogenated castor oil are placed in a pear-shaped bottle, an organic solvent is added, heated and stirred to dissolve, and then the organic solvent is removed under reduced pressure on a rotary evaporator. A uniform and transparent phospholipid film is formed on the bottle wall;

[0065] (2) Under the protection of nitrogen, add the aqueous solution of heparin calcium and PVP into the bottle, stir to elute the phospholipid membrane and fully swell and hydrate. After the hydration is complete, do gradient homogenization at 100bar to 600bar for 4 to 6 times, 0.22μm Microporous membrane filtration to obtain heparin calcisomes;

[0066] (3) Under sterile conditions, dissolve trehalose and sorbitol in wat...

Embodiment 1

[0073] The preparation of embodiment 1 injection heparin calcium liposome preparation

[0074] The raw and auxiliary materials used and their weights are as follows (1000 bottles):

[0075]

[0076] Adopt preparation technology to prepare heparin calcium liposome preparation for injection:

[0077] (1) Put 90g of cholesterol, 150g of phosphatidylglycerol, 30g of lecithin and 20g of polyoxyethylene 40 hydrogenated castor oil in a pear-shaped bottle, add 10000ml of ethanol, heat and stir to dissolve it, and then remove it under reduced pressure on a rotary evaporator Organic solvent, forming a uniform and transparent phospholipid film on the bottle wall;

[0078] (2) Under the protection of nitrogen, add 100g heparin calcium and 30g PVP dissolved in 1200ml water for injection to the bottle, stir to elute the phospholipid film and fully swell and hydrate it. After the hydration is complete, do gradient homogenization at 100bar to 600bar 4 to 6 times, 0.22 μm microporous me...

Embodiment 2

[0080] The preparation of embodiment 2 injection heparin calcium liposome preparation

[0081] The raw and auxiliary materials used and their weights are as follows (1000 bottles):

[0082]

[0083] Adopt preparation technology to prepare heparin calcium liposome preparation for injection:

[0084] (1) Put 95g of cholesterol, 165g of phosphatidylglycerol, 35g of lecithin and 30g of polyoxyethylene 40 hydrogenated castor oil in a pear-shaped bottle, add 10000ml of ethanol, heat and stir to dissolve it, and then remove it under reduced pressure on a rotary evaporator Organic solvent, forming a uniform and transparent phospholipid film on the bottle wall;

[0085] (2) Under the protection of nitrogen, add 100g heparin calcium and 55g PVP dissolved in 1200ml water for injection to the bottle, stir to elute the phospholipid membrane and fully swell and hydrate it. After the hydration is complete, do gradient homogenization at 100bar to 600bar 4 to 6 times, 0.22 μm microporou...

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Abstract

The invention discloses a calcium heparin liposome preparation for injection and a preparation method thereof. The liposome injection is made from the following components in a specific weight ratio: calcium heparin, cholesterol, phosphatidyl glycerol, lecithin, polyoxyethylene (40) hydrogenated castor oil, trehalose, sorbitol and polyvinylpyrrolidone. The liposome injection has good stability; the liposomes are not liable to be dehydrated, fused, crystallized or broken during the freezing process; and the liposomes maintain good encapsulation efficiency and stability after long-term storage.The solubility of calcium heparin is increased, the quality of the product is improved, the toxic and adverse effects are reduced, the retention time of drugs in the systemic circulation is increased, the bioavailability of drugs is improved, and the efficacy is greatly improved. Besides, the preparation method is simple and suitable for industrial production.

Description

technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a heparin calcium liposome preparation for injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Calcium heparin, also known as low molecular weight heparin calcium, its chemical name: calcium dextran sulfate. Antithrombotic drugs include heparin, non-heparin antiplatelet aggregation drugs, enzymes and four other small subclasses. Heparin and enzymes are basically biochemical drugs. Among them, heparins occupy the largest market share, and among the heparins, heparin drugs dominate. Heparin calcium and low-molecular-weight heparin sodium occupy 20% and 7% of the entire antithrombotic drug market share, respectively. Although bioactive heparin has been discovered for more than 80 years, it is still one of the most important biochemical drugs because there is no product that can completely rep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/727A61K47/34A61P7/02
Inventor 陶灵刚赵雁鸿
Owner 灵康药业集团股份有限公司
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