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Atractylone lipidosome and preparation method thereof

A technology of atractylodes ketone lipid and atractylodes ketone, which is applied in the field of atractylodes ketone liposome and its preparation, can solve the problems of small intermolecular force, large particle size of liposome, and easy aggregation, etc., to expand clinical and application value, The effect of narrow and uniform particle size distribution

Inactive Publication Date: 2010-05-12
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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Embodiment 1

[0047] Example 1 Preparation and determination of atractylone liposomes

[0048] 1. Preparation of atractylone liposomes

[0049] Materials and equipment: Atractylone, an extract of Atractylodes macrocephala koedz (Atractylodes macrocephala koedz), provided by Neptunus Biotech Co., Ltd., mass fraction ≥95%, batch number 080115; medicinal materials produced in Zhejiang Pan'an, Zhejiang Pan'an Medicinal Materials Company, Batch number BZ07061501; Phosphatidylcholine and cholesterol, provided by Shanghai Boao Bioengineering Company, analytical grade, 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 used in supercritical CO 2 Completed in the rapid expansion device, the detailed flow chart is as follows figure 1 Shown.

[0051] ...

Embodiment 2

[0062] Example 2 Effect of pre-expansion pressure on the preparation of atractylone liposomes

[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 the atractylone and liposome membrane material in the supercritical fluid according to the ratio of Example 1, at a temperature of 333K, the co-solvent ethanol is in CO 2 Middle mole fraction x(CH 3 CH 2 OH) = 15%, pre-expanded at 15-30 MPa, sprayed into buffer solution without stabilizer, and measured the encapsulation efficiency of liposomes prepared under different pressures. The results are as follows figure 2 Shown.

[0064] The experimental results show that under lower pressure, liposome membrane material phospholipid and cholesterol are in SC-CO 2 The solubility is small, and it is difficult to form a uniform liposome membrane. The prepared liposome suspension contains a large number of phospholipid blocks and ...

Embodiment 3

[0065] Example 3 Effect of pre-swelling temperature on the preparation of atractylone liposomes

[0066] This example investigates the influence of pre-swelling temperature on the preparation of atractylone liposomes. Using the same method as in Example 1, after dissolving the atractylone and liposome membrane material in the supercritical fluid according to the ratio of Example 1, under the pressure of 30MPa, x(CH 3 CH 2 OH) = 15%, pre-expanded at 313K~343K, sprayed into buffer solution without stabilizer, and measured the encapsulation efficiency of liposomes prepared in different temperature ranges. The results are 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 the phospholipid, SC-CO 2 The phospholipid bilayers formed in the phospholipid are arranged tightly, and atra...

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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, and specifically relates to atractylone liposomes and a preparation method thereof. Background technique [0002] Atractylodes is the dried rhizome of Atractylodes macrocephala koidz (Atractylodes macrocephala koidz). It 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 invigorating the spleen, invigorating the stomach, drying dampness, and neutralizing the body. . Atractylodes macrocephala mainly contains volatile oil, and atractylone is the compound with the highest content in the volatile oil. Chinese medicine believes that Atractylodes macrocephala has a better effect on the symptoms of chronic hepatitis, liver ascites, liver cancer and other spleen and stomach weakness, spleen and kidney yang deficiency, or qi and blood weakness. Modern pharmacolo...

Claims

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Application Information

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