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Preparation method of poorly soluble medicine liposome

A technology for insoluble drugs and blank liposomes, applied in the field of pharmaceutical preparation technology, can solve problems such as difficult control, low encapsulation rate, complicated process, etc., and achieve the effect of realizing large-scale industrial production.

Active Publication Date: 2014-03-12
常州金远药业制造有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is: in the prior art, when the insoluble drug liposome is prepared by passive drug loading, the encapsulation efficiency is low, the process is complex and difficult to control

Method used

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  • Preparation method of poorly soluble medicine liposome
  • Preparation method of poorly soluble medicine liposome
  • Preparation method of poorly soluble medicine liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation Step A

[0051] Blank liposome prescription:

[0052]

[0053] Dissolve phospholipids and soybean oil in chloroform, place on a rotary evaporator, remove chloroform, and form a phospholipid film. Dissolve mannitol in water, add it to the phospholipid film, elute the phospholipid film, and control the average particle size below 150nm through a high-pressure homogenizer for later use.

[0054] The particle size chart of the blank liposome is attached figure 2 shown.

[0055] Preparation step B

[0056] Paclitaxel solution prescription:

[0057] Paclitaxel 0.4g

[0058] Ethanol 2g

[0059] Paclitaxel was dissolved in ethanol.

[0060] Preparation Step C

[0061] In step B, add the blank liposome solution prepared in step A (in step B, paclitaxel can be dissolved in ethanol, when the ethanol solution is mixed with water, paclitaxel is insoluble in water and precipitates, and its particles are very small, reaching micron size ), at room temperature,...

Embodiment 2

[0065] Preparation Step A

[0066] Blank liposome prescription:

[0067]

[0068] Heat and dissolve phospholipids, polyethylene glycol phosphatidylethanolamine, cholesterol and ethanol at 60°C, dissolve trehalose and histidine in water, adjust the pH to 6.5 with hydrochloric acid, heat to 65°C, inject the above ethanol solution, and stir for 30 minutes Finally, through a high-pressure homogenizer, the average particle size is controlled below 180nm for later use.

[0069] Preparation step B

[0070] Docetaxel solution prescription:

[0071] Docetaxel 0.6g

[0072] Ethanol 2g

[0073] Dissolve docetaxel in ethanol.

[0074] Preparation Step C

[0075] In step B, add the blank liposome solution prepared in step A (the principle of preparing the insoluble drug suspension or solution is as shown in Example 1), stir at 4°C and 100 rpm, the system turns from turbid to transparent After the buffer solution is replaced by cross tangential flow equipment (the residual amount ...

Embodiment 3

[0079] Preparation Step A

[0080] Blank liposome prescription:

[0081]

[0082] Dissolve phospholipids, phosphatidylglycerol, and cholesterol with methanol and methylene chloride to obtain an organic solution; dissolve sucrose and sodium succinate in water, adjust the pH to 5.5 with hydrochloric acid, and heat to 35°C. Slowly inject the above organic solution, stir for 30 minutes, recover the organic solvent in a vacuum, and then use a high-pressure homogenizer to control the average particle size below 100nm for later use.

[0083] Preparation step B

[0084] Amphotericin B Suspension Prescription:

[0085] Amphotericin B 1g

[0086] Sodium deoxycholate 0.1g

[0087] water 10g

[0088] Sodium deoxycholate was dissolved in water, amphotericin B was added, and ground by a colloid mill so that the average particle size of amphotericin B particles was below 5 μm.

[0089] Preparation Step C

[0090] In step B, add the blank liposome solution prepared in step A, stir a...

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Abstract

The invention belongs to the field of medicine preparation, and particularly relates to a preparation method of a poorly soluble medicine liposome. A blank liposome free of a medicine and a medicine suspension or a medicine solution are separately prepared, and then the blank liposome and the medicine are mixed under the conditions of a certain temperature and a certain rotating speed. According to the poorly soluble medicine liposome prepared by the method, the encapsulation efficiency is greater than or equal to 90%, and the mean grain size is smaller than or equal to 150nm. According to the preparation method, conventional process equipment is adopted, the product is stable in quality, the method is simple in technology, and low in cost, and the technical problem that the poorly soluble medicine liposome is difficultly industrialized is solved.

Description

technical field [0001] The method belongs to the technical field of pharmaceutical preparations, in particular to a method for preparing liposome preparations of insoluble drugs. Background technique [0002] Liposome is an artificial membrane. In the water, the hydrophilic head of the phospholipid molecule is inserted into the water, and the hydrophobic tail of the liposome extends to the air. After stirring, a spherical liposome of bilayer lipid molecules is formed, with a diameter ranging from 25 to 1000 nm. Liposomes can be used for genetically modified or prepared drugs, using the characteristics that liposomes can fuse with cell membranes to deliver drugs into cells Biological definition: when amphiphilic molecules such as phospholipids and sphingolipids are dispersed in the water phase, the hydrophobic The tails tend to clump together, avoiding the aqueous phase, while the hydrophilic heads are exposed to the aqueous phase, forming closed vesicles with a bilayer stru...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7048A61K31/337
Inventor 贺明朱瑶俊周钢贺欣
Owner 常州金远药业制造有限公司
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