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Method and apparatus for preparing novel liposome

A technology of liposomes and proliposomes, which is applied in the field of preparation of liposome preparations and devices for preparing liposomes, and can solve problems such as inability to apply

Active Publication Date: 2012-11-14
BC WORLD PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this technique has a big problem because high boiling point solvents such as dimethylacetamide (DMA), dimethylformamide (DMF), dimethyl sulfoxide (DMSO) cannot be applied in the process because Use of heated air to remove organic solvents during spray drying

Method used

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  • Method and apparatus for preparing novel liposome
  • Method and apparatus for preparing novel liposome
  • Method and apparatus for preparing novel liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1a~1f

[0053] Example 1a~1f and 2a~2d: Preparation of amphotericin B liposomes

[0054] Dissolve 84 mg of distearoylphosphatidylcholine (DSPC) in 1 ml of a 1:1 mixed solvent of chloroform and methanol at 65°C. 200 mg of ascorbic acid (VIt-C) was completely dissolved in 2 ml of N,N-dimethylacetamide (DMA) by ultrasound for 10 minutes. 50 mg of amphotericin B was dissolved in the DMA-Vit C solution at 65°C, and the DSPC solution was added to the resulting solution. At 65°C, 213 mg of hydrogenated soybean phosphatidylcholine and 52 mg of cholesterol were dissolved in 1 ml of a 1:1 mixed solvent of chloroform and methanol. The solution of hydrogenated soybean phosphatidylcholine and cholesterol was mixed with the amphotericin B-DSPG solution.

[0055] The amphotericin B-lipid solution and 900 mg of lactose were contained in the reaction vessel 1, and then sealed. The temperature of the reaction vessel was maintained at 45°C, 55°C and 65°C. By operating the pump 4, supercritical carbon dio...

Embodiment 1

[0057] Example 1 relates to the characteristics of liposome solution according to the temperature and pressure of the reaction vessel during the supercritical process. In Examples 1a to 1f, the particle size and the drug content according to the temperature and pressure of the reaction vessel are recorded in Table 1. Example 2 relates to: when the proliposome particles prepared at a reaction temperature of 45°C and a pressure of 200 bar are hydrated by adding an aqueous solution (including water) in the supercritical process corresponding to Example 1a, the lipid Body solution is based on the characteristics of hydration temperature. In Examples 2a to 2d, the particle size, drug content, and formation / non-formation of liposomes according to the hydration temperature are recorded in Table 2.

[0058] Table 1

[0059] [Table 1]

[0060] [table]

[0061] In Examples 1a to 1f, the particle size and drug content according to the temperature and pressure of the reaction vessel

[0062]

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Abstract

Disclosed is a method for preparing a liposome formulation. In the disclosed method, a lipid fraction is dissolved in an organic solvent. The solution including a bioactive component and the lipid fraction, together with a carrier, is put in a reaction vessel, and a supercritical fluid is introduced thereto, so as to prepare particles coated with the bioactive component-lipid. The supercritical fluid is discharged by compression to obtain proliposome particles, and then the proliposome particles are hydrated by an aqueous solution including water so as to form a liposome solution. Preferably, the formulation may include one or more bioactive components. As required, the liposome formulation may be further processed by methods such as particle size reduction, removal of organic solvent, and freeze-drying. The preparation method can be easily carried out at a laboratory scale.; Furthermore, the same method can be employed in liposome formulation preparation in mass production, or at a commercial scale.

Description

Technical field [0001] The present invention relates to a new method for preparing liposomes and a device for preparing liposomes, and preferably the liposome preparation may include one or more biologically active components. More specifically, the present invention relates to a method and device for preparing liposome preparations, wherein the liposome preparations have stability of anti-biologically active components and preparation stability, and can be mass-produced with high yield. Background technique [0002] Liposomes are vesicles that include phospholipids and their derivatives. When phospholipid and its derivatives are dispersed in water, it spontaneously forms vesicles and has the characteristic of a lipid bilayer including an aqueous core inside. Various liposomes have been used as carriers for drugs, enzymes, and therapeutic agents such as gene sequences in the medical, pharmaceutical, and biochemical fields. [0003] Examples of liposome compositions are disclosed ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/36C12M1/02
CPCA61K9/1277A61J3/07A61K9/19A61K9/127A61K31/70B01D11/0411A61P31/10
Inventor 黄成柱朴熺俊赵原庆车光浩朴峻成朴灿赫具东键
Owner BC WORLD PHARM LTD
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