Atractylone lipidosome and preparation method thereof

The technology of Atractylodes ketone lipid and Atractylodes ketone is applied in the field of Atractylodes ketone liposome and its preparation, which can solve the problems of small intermolecular force, large particle size of liposome, easy agglomeration and the like, and achieves uniform distribution, small particle size, Overcome the effect of easy agglomeration

Inactive Publication Date: 2011-07-06
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the problem at this stage is that due to CO 2 The polarity of water is very different, and the force between the two molecules is very small, directly in the supercritical CO 2 It is very difficult to disperse the liposome membrane material in water in the medium, and the obtained liposome has a large particle size and is easy to agglomerate

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  • Atractylone lipidosome and preparation method thereof
  • Atractylone lipidosome and preparation method thereof
  • Atractylone lipidosome and preparation method thereof

Examples

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Effect test

Embodiment 1

[0047] Preparation and determination of embodiment 1 atractylone liposome

[0048] 1. Preparation of atractylone liposomes

[0049] Materials and devices: Atractylone, the extract of Atractylodes macrocephala koedz, provided by Neptunus Biological Co., Ltd., with a mass fraction ≥ 95%, batch number 080115; the medicinal material is produced in Pan'an, Zhejiang, provided by Zhejiang Pan'an Medicinal Materials Company, Batch number BZ07061501; phosphatidylcholine and cholesterol, provided by Shanghai Boao Bioengineering Co., Ltd., analytically pure, batch number BA20071206, BA20071125; supercritical fluid reaction experimental device, designed and manufactured by the Modern Technology Center of South China University of Technology.

[0050] Preparation method: In one embodiment, the method for preparing atractylone liposomes of the present invention can be carried out under supercritical CO 2 Completed in the rapid expansion device, the detailed flow chart is as follows figu...

Embodiment 2

[0062] The influence of embodiment 2 pre-expansion pressure on the preparation of atractylone liposome

[0063] This example investigates the effect of pre-expansion pressure on the preparation of atractylone liposomes. Using the same method as in Example 1, after dissolving atractylone and liposome membrane material in the supercritical fluid according to the ratio of Example 1, the temperature is 333K, and the co-solvent ethanol is in CO 2 Middle mole fraction x(CH 3 CH 2 OH)=15%, in 15~30MPa condition pre-expansion, spray in the buffer solution that does not contain stabilizer, measure the encapsulation efficiency of preparing liposome under different pressures, the result is as follows figure 2 shown.

[0064] The experimental results showed that under lower pressure, liposome membrane materials phospholipids and cholesterol were in SC-CO 2 The solubility is small, and it is difficult to form a uniform liposome membrane. There are a large number of phospholipid bloc...

Embodiment 3

[0065] The influence of embodiment 3 pre-expansion temperature on the preparation of atractylone liposome

[0066]This example investigates the effect of pre-expansion temperature on the preparation of atractylone liposomes. Adopt the method identical with embodiment 1, atractylone and liposome membrane material are dissolved in the supercritical fluid after the ratio of embodiment 1, under pressure is 30MPa, x (CH 3 CH 2 OH)=15% condition, pre-expansion under 313K~343K, spray in the buffer solution that does not contain stabilizer, measure the encapsulation efficiency of liposome preparation in different temperature ranges, the result is as follows image 3 shown.

[0067] The experimental results show that the physical properties of liposomes are closely related to the preparation temperature. When the temperature is lower than 323K, which is lower than the phase transition temperature Tm of phospholipids, SC-CO 2 The phospholipid bilayers formed in the liposomes are c...

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Abstract

The invention discloses an atractylone lipidosome containing atractylone and a lipidosome membrane material, wherein the atractylone is an Atractylis ovata extract, and the lipidosome membrane material is phosphatidylcholine or cholesterol. A method for preparing the atractylone lipidosome by adopting a supercritical fluid dispersing precipitation technology comprises the following steps of: (1) dissolving the atractylone and the lipidosome membrane material in a supercritical CO2 / alcohol mixed solvent, then obtaining a supercritical solution; (2) dissolving a surface active agent as a stabilizer in an aqueous medium, then obtaining a stabilizer solution; (3) and rapidly jetting the supercritical solution to the stabilizer solution at a certain pre-swelling pressure and pre-swelling temperature, and then obtaining an atractylone lipidosome mixed suspension by forcible dispersion and precipitation. The preparation process of the lipidosome is completed in the chemically inert CO2 medium; toxic organic solvents are not used, and the envelop rate of the lipidosome is improved, thereby effectively avoiding the agglomeration phenomenon caused by colliding among lipidosome particles, and ensuring the stability of the atractylone lipidosome in the preparation process.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to atractylone liposome and a preparation method thereof. Background technique [0002] Atractylodes macrocephala is the dried rhizome of Atractylodes macrocephala koidz, which is one of the most widely used medicinal materials in clinical practice. Traditional Chinese medicine believes that it is warm in nature, pungent and bitter in taste, and has the effects of nourishing the spleen, benefiting the stomach, drying dampness, and harmonizing the heart. . Atractylodes macrocephala mainly contains volatile oil, among which atractylone is the compound with the highest content in volatile oil. Traditional Chinese medicine believes that Atractylodes macrocephala has a good effect on chronic hepatitis, liver ascites, liver cancer and other symptoms of weakness of the spleen and stomach, deficiency of spleen and kidney yang or weakness of qi and blood. Modern pharmacological s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K9/127A61K36/284A61P31/14A61P1/16A61P7/10A61K31/343A61K47/28A61P31/20
Inventor 文震刘波郑宗坤游新奎蒲一涛米宏伟
Owner SHENZHEN UNIV
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