Dabigatran etexilate liposome

A dabigatran etexilate and liposome technology, applied in the field of dabigatran etexilate liposome and solid preparations, can solve the problem that the drug effect can only be maintained for several days

Active Publication Date: 2014-01-29
江苏阿尔法集团盛基药业(宿迁)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, dabigatran currently on the market is a capsule, which needs to be taken twice a day and needs to be packaged in a special packaging material containing a desiccant. After taking it out, its efficacy can only last for a few days.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The preparation of embodiment 1 dabigatran etexilate liposome

[0018] Dissolve 1000g of lecithin and 100g of cholesterol in 2000ml of organic solvent (acetone: dichloromethane = 1:1), place on a rotary thin film evaporator to remove the organic solvent under reduced pressure to obtain a phospholipid film. Add the solution 1000ml that is dissolved in 100g dabigatran etexilate, mix well. Ultrasound at 70°C for 60 minutes. The solution was spray-dried to obtain dabigatran etexilate liposomes.

[0019] Get above-mentioned 100g dabigatran etexilate liposome, pulverize and cross 80 mesh sieves. Add 200g of starch, 10g of croscarmellose sodium, mix well, add 50ml of 30% ethanol solution containing 2g of povidone K30 to make soft material, pass through a 20 mesh sieve to granulate, dry at 60 degrees, add stearic acid Magnesium 8g, mixed evenly, and pressed into tablets.

Embodiment 2

[0020] The preparation of embodiment 2 dabigatran etexilate liposomes

[0021] Dissolve 500g of lecithin and 10g of cholesterol in 1500ml of organic solvent (acetone: dichloromethane = 1:1), place on a rotary thin film evaporator to remove the organic solvent under reduced pressure to obtain a phospholipid film. Add the solution 600ml that is dissolved in 10g dabigatran etexilate, mix well. Ultrasound at 70°C for 60 minutes. The solution was spray-dried to obtain dabigatran etexilate liposomes.

[0022] Get above-mentioned 100g dabigatran etexilate liposome, pulverize and cross 80 mesh sieves. Add 300g of microcrystalline cellulose and 10g of croscarmellose sodium, mix well, add 80ml of 2% hypromellose in 20% ethanol solution to make soft material, pass through a 20-mesh sieve to granulate, and dry at 60 degrees. Sieve through a 20-mesh sieve, add 4g of talcum powder, mix evenly, fill capsules, and get ready.

Embodiment 3

[0023] The preparation of embodiment 3 dabigatran etexilate liposomes

[0024] Dissolve 300g of lecithin and 50g of cholesterol in 1000ml of organic solvent (acetone: dichloromethane = 1:1), place on a rotary thin film evaporator to remove the organic solvent under reduced pressure to obtain a phospholipid film. Add the solution 600ml that is dissolved in 10g dabigatran etexilate, mix well. Ultrasound at 70°C for 60 minutes. The solution was spray-dried to obtain dabigatran etexilate liposomes.

[0025] Get above-mentioned 100g dabigatran etexilate liposome, pulverize and cross 80 mesh sieves. Add 100g of powdered cellulose, 10g of low-substituted hydroxypropyl cellulose, mix well, add 50ml of 30% ethanol solution containing 2g of starch to make soft material, pass through a 20-mesh sieve to granulate, dry at 60 degrees, add 2g of magnesium stearate , mix evenly, and press into tablets.

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PUM

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Abstract

The invention provides dabigatran etexilate liposome. The dabigatran etexilate liposome is characterized by consisting of at least one phospholipid and a lipophilic compound. The dabigatran etexilate liposome preferably comprises the following components in parts by weight: 1 part of dabigatran etexilate, 10 to 50 parts of lecithin and 1 to 10 parts of cholesterol. The invention also provides a dabigatran etexilate liposome solid preparation. The dabigatran etexilate liposome solid preparation is prepared from the following components in parts by weight: 1 part of dabigatran etexilate liposome, 1 to 3 parts of a filling agent, 0 to 0.2 part of a disintegrating agent, 0.02 to 0.1 part of an adhesive and 0 to 0.08 part of a lubricating agent. The solid preparation can also comprise 0 to 10 parts of a corrigent and 0 to 0.15 part of a flavoring agent. According to the technical scheme of the invention and the advantages of the liposome, the medicine adsorption and utilization ratio of dabigatran etexilate is increased, the half-life period of the medicine is prolonged, and the administration dosage or the administration frequency can be effectively reduced.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a liposome of dabigatran etexilate and a solid preparation prepared by using the liposome. Background technique [0002] Dabigatran etexilate was first approved by the US Food and Drug Administration (FDA) in 2010 for the prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation. Currently, this indication has been approved in more than 60 countries around the world. Unlike vitamin K antagonists that act on different coagulation factors, dabigatran etexilate can provide effective, predictable and stable anticoagulant effect, and at the same time, there are fewer drug interactions, no drug food interactions, and no routine treatment Coagulation monitoring or dose adjustment. Dabigatran etexilate is the first antithrombin compound marketed by oral administration route, and its efficacy is comparable to that of enoxaparin and warfarin. Compare...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4439A61K47/24A61P7/02
Inventor 蔡进尹晓龙吉民徐春涛张领
Owner 江苏阿尔法集团盛基药业(宿迁)有限公司
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