Method for preparing medicine encapsulating liposome

A technology for encapsulating drugs and liposomes, which is applied in the field of preparation of drug-encapsulating liposomes, can solve problems such as the preparation technology of microparticle carriers that have not been seen, and achieve the goals of improving bioavailability, improving release behavior, and increasing encapsulation efficiency Effect

Active Publication Date: 2014-09-10
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, solid dispersion technology is mostly applied to solid oral preparations, and there is no report on its application to the preparation technology of particulate carriers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: Diclofenac sodium liposome

[0027] The first embodiment of the present invention adopts the water-soluble drug diclofenac sodium as the target drug, and the amphiphilic macromolecular material selects povidone (PVP), adopts the melting method to prepare the diclofenac sodium-polyvidone solid dispersion, and the liposome forms The membrane material is selected from hydrogenated soybean lecithin, cholesterol, Tween 80 and cetyl alcohol, and the liposome encapsulating diclofenac sodium is prepared by freeze-drying method.

[0028] Experimental group: 30mg of povidone (PVP) was melted in a water bath at 65°C, and 8mg of diclofenac sodium was added to disperse evenly, and transferred to an ice bath at 0°C for quenching treatment to prepare a solid dispersion of diclofenac sodium-povidone. Dissolve 20mg of hydrogenated soybean lecithin, 6mg of cholesterol, 2mg of Tween 80 and 2mg of cetyl alcohol in 20ml of tert-butanol, dissolve in a water bath at 65°C, add di...

Embodiment 2

[0034] Embodiment 2: Paclitaxel liposome

[0035] The second embodiment of the present invention adopts fat-soluble drug paclitaxel as target drug, amphiphilic polymer material polyethylene glycol (PEG 2000), adopts solvent-melt method to prepare paclitaxel-polyethylene glycol solid dispersion, lipid Dipalmitoylphosphatidylcholine (DPPC), distearoylphosphatidylethanolamine (DSPE-PEG2000) grafted with polyethylene glycol 2000 (DSPE-PEG2000) and Tween 80 were selected as the film-forming materials, and the paclitaxel-loaded lipid was prepared by injection method. plastid.

[0036]Experimental group: add 30mg of polyethylene glycol (PEG 2000) into 0.5ml of absolute ethanol, melt in a water bath at 65°C, add 5mg of paclitaxel to disperse evenly, transfer to 0°C for quenching in an ice bath, and make paclitaxel-polyethylene glycol Alcoholic solid dispersion. 5mg of dipalmitoylphosphatidylcholine (DPPC), 1mg of polyethylene glycol 2000 grafted distearoylphosphatidylethanolamine (D...

Embodiment 3

[0041] Embodiment 3: Irinotecan hydrochloride liposome

[0042] The third embodiment of the present invention adopts irinotecan hydrochloride as the target drug, the amphiphilic polymer material selects poloxamer (Poloxamer 188), and adopts the melting method to prepare irinotecan hydrochloride-poloxamer solid dispersion, The liposome film-forming material is selected from hydrogenated egg yolk phospholipid, cholesterol, Tween 80 and glycerin, and the nano liposome loaded with irinotecan hydrochloride is prepared by a high-pressure milk homogenization method.

[0043] Experimental group: 55 mg of poloxamer (Poloxamer 188) was melted in a water bath at 65°C, and 5 mg of irinotecan hydrochloride was added to disperse evenly to obtain a solid dispersion of irinotecan hydrochloride-poloxamer. Add 20mg of hydrogenated egg yolk phospholipids, 6mg of cholesterol, 2mg of Tween 80, and 6mg of glycerin into 10ml of 80°C water, add irinotecan hydrochloride-poloxamer solid dispersion, emu...

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Abstract

The invention relates to a method for preparing a medicine encapsulating liposome, which comprises: preparing medicine solid dispersion; and uniformly dispersing the medicine solid dispersion and a liposome film-forming material in an organic solvent to prepare the medicine encapsulating liposome. When the method is used, a medicine can be uniformly encapsulated in the liposome, the medicine encapsulating rate is improved, and sudden release of the medicine encapsulating liposome is reduced. The liposome is suitable for encapsulating various medicines and can be used in a wide formulation range.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to a preparation method of drug-encapsulated liposomes. 【Background technique】 [0002] Liposomes are monolayer or multilayer microcapsules composed of ordered lipid bilayers. Liposome belongs to the colloidal system, has a cell-like structure, has a strong affinity with the cell membrane, and can increase the ability of the encapsulated drug to penetrate the cell membrane. Liposomes have good biocompatibility, can realize targeted delivery of drugs in vivo, and have many advantages such as prolonging drug action time, increasing drug stability in vivo and in vitro, reducing drug toxicity, and enhancing pharmacological effects. [0003] There are many methods for preparing liposomes, such as film dispersion method, reverse phase evaporation method, freeze-drying method, injection method, ultrasonic dispersion method, etc. At present, lipo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/32A61K47/34A61K47/24A61K47/28A61K47/10
Inventor 鲁翠涛赵应征
Owner ZHEJIANG HISUN PHARMA CO LTD
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