Preparation method of chrysophanol proliposome

A technology of proliposome and chrysophanol, which is applied in the direction of liposome delivery, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of uneven dispersion, complicated process, cumbersome operation, etc., and meet the reaction conditions Mild, simple process operation, high drug encapsulation efficiency

Inactive Publication Date: 2018-10-23
HEBEI NORTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above method has the problems of cumbersome operation, complex process, slow hydration rate of the prepared liposome during use, imperfect local dissolution, uneven dispersion, etc.

Method used

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  • Preparation method of chrysophanol proliposome
  • Preparation method of chrysophanol proliposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Experimental equipment: rotary evaporator (RE52-99); UV-visible spectrophotometer (TU-1810); circulating water vacuum pump (SHZ-D(III)); low-speed centrifuge (SU-05).

[0019] Experimental reagents: chrysophanol standard substance (National Institute for the Control of Pharmaceutical and Biological Products); chrysophanol test substance (Weiwei Phytochemical Research Institute, Wei'an City, Jiangsu Province); lecithin (Beijing Huaqing Meiheng Natural Products Technology Development Co., Ltd.); cholesterol (Beijing Dingguo Biotechnology Co., Ltd.); PEG-2000 (Beijing Dingguo Biotechnology Co., Ltd.); others are analytical reagents.

[0020] experimental method:

[0021] Dissolve chrysophanol (3mg) in dehydrated ethanol (10mL) containing lecithin (24mg), cholesterol (6mg), PEG-2000 (12mg), vitamin E (10mg) to obtain a mixed solution, and the resulting mixed solution was micro- After filtering and sterilizing the pore filter membrane (pore size is 0.45 μm), inject directly...

Embodiment 2

[0027] Chrysophanol (3mg) was dissolved in absolute ethanol (10mL) containing lecithin (24mg), cholesterol (4.8mg), PEG-2000 (6mg), vitamin E (10mg), to obtain a mixed solution, and the resulting mixed solution was subjected to After microporous filter membrane (0.45μm pore size) is filtered and sterilized, it is directly injected into water (constant volume to 25mL), at room temperature, pH = 7.8, rapidly self-assembles into chrysophanol proliposomes, sealed and kept at 4°C Store at low temperature.

[0028] The detection method for the encapsulation efficiency of the obtained chrysophanol self-assembled proliposomes is the same as in Example 1, and the results are shown in Table 1.

Embodiment 3

[0030] Dissolve chrysophanol (3mg) in absolute ethanol (10mL) containing lecithin (30mg), cholesterol (5mg), PEG-2000 (15mg), vitamin E (10mg) to obtain a mixed solution, and the resulting mixed solution was subjected to micro After filtering and sterilizing through a pore filter membrane (0.45 μm in pore size), inject it directly into water (constant volume to 25 mL), at room temperature, pH=7.8, rapidly self-assemble into chrysophanol proliposomes, seal and store at 4°C save.

[0031] The detection method for the encapsulation efficiency of the obtained chrysophanol self-assembled proliposomes is the same as in Example 1, and the results are shown in Table 1.

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Abstract

The invention provides a preparation method of chrysophanol proliposomes. The preparation method includes: dissolving chrysophanol in absolute ethyl alcohol containing lecithin, cholesterol, PEG-2000 and vitamin E to obtain mixed liquid, filtering the mixed liquid with a microporous filter membrane to remove bacteria, directly injecting the filtered liquid into a hydration medium, allowing self-assembly at room temperature to obtain chrysophanol proliposomes, and hermetically storing the chrysophanol proliposomes at 0-4 DEG C. The reaction mixed liquid is directly injected into the hydration medium, and self-assembled is allowed at room temperature to obtain the proliposomes, reaction conditions are mild, technical operations are simple, the time is short, industrial production of liposome drugs is facilitated, and the obtained proliposomes are higher than those prepared by rotary evaporation, in drug encapsulation rate.

Description

(1) Technical field [0001] The invention relates to a preparation method of chrysophanol proliposome, in particular to a method for preparing chrysophanol proliposome by a self-assembly method. (2) Background technology [0002] Chrysophanol is one of the active ingredients in rhubarb of the Polygonaceae plant. It belongs to anthraquinone compounds. However, chrysophanol has low solubility, is easy to oxidize, and is highly irritating to the gastrointestinal tract. It cannot be stored for a long time, and it is difficult to administer it clinically. Liposome is a microscopic sphere composed of one or more layers of lipid bilayers arranged concentrically with the central aqueous core, which has the functions of slowing down drug release, increasing drug targeting, reducing drug side effects, improving drug stability, and increasing drug resistance. It is a new type of pharmaceutical preparation because of its affinity to tissue cells, promotion of drug absorption, improvemen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/122A61P11/14A61P31/04A61P39/06A61P7/10A61P35/00A61P7/04A61P3/10A61P9/14
Inventor 王永利庚丽丽魏珍王立华吴亮飞
Owner HEBEI NORTH UNIV
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