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Self-assembled lipidosome precursor of coenzyme Q10 inclusion compound and preparation method of self-assembled lipidosome precursor

A liposome precursor and self-assembly technology, which is applied in the field of medicine and health care products, can solve the problems of poor liposome stability, low oral bioavailability, poor stability, etc., and achieve significant dissolution and solubility, significant Bioabsorption characteristics, absorption-promoting effect

Active Publication Date: 2019-01-08
SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] coenzyme Q 10 It is a fat-soluble substance, hardly soluble in water, and belongs to the class II substance of biopharmaceuticals. Dissolution is the rate-limiting step of its absorption. The bioavailability of oral administration is low, and its absolute bioavailability is less than 5%.
At present, inclusion complex self-assembled liposomes are generally liquid and have poor stability.
And the liposome solid precursor reported at present basically is to prepare liposome solution first and then lyophilize into solid, and its water-covered reconstituted liposome has poor stability, and there is no self-assembly into liposome that cannot be prepared into liposome. At present, there are no literature reports and patents on inclusion compound self-assembled liposome precursors, and there is no coenzyme Q 10 Inclusion Complex Self-Assembled Liposomes and Coenzyme Q 10 Inclusion complex self-assembled liposome precursor literature and patents
None of the above patent documents relate to the technology of the present invention, and coenzyme Q has not been retrieved so far 10 Patents and literature research reports on inclusion complex self-assembled liposomes and their inclusion complex liposomes

Method used

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  • Self-assembled lipidosome precursor of coenzyme Q10 inclusion compound and preparation method of self-assembled lipidosome precursor
  • Self-assembled lipidosome precursor of coenzyme Q10 inclusion compound and preparation method of self-assembled lipidosome precursor
  • Self-assembled lipidosome precursor of coenzyme Q10 inclusion compound and preparation method of self-assembled lipidosome precursor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Oxidized coenzyme Q of the present invention 10 Inclusion compound self-assembled liposome precursor, which is prepared by weight ratio from the following raw materials, oxidized coenzyme Q 10 : β-cyclodextrin: soybean lecithin: mannitol = 1:5:0.5:5.

[0041] Take 50 parts by mass of β-cyclodextrin and 10 parts by mass of oxidized coenzyme Q 10 , add 250 parts by mass of water to mix and disperse evenly, stir to form a paste, heat to 50°C, put it into a colloid mill, grind it circularly for 5 times, add water to dilute to a solid concentration of 10%, and obtain cyclodextrin coenzyme Q 10 Grinding fluid for standby; get 5 parts by mass of soybean lecithin, add it to 250 parts by mass of water, mix and disperse evenly, and obtain a phospholipid dispersion for subsequent use; take 50 parts by mass of mannitol, put it into a fluidized bed as a mother nucleus, and spray into the above-mentioned phospholipid Dispersion liquid, so that the surface of mannitol particles is c...

Embodiment 2

[0043] Reduced coenzyme Q of the present invention 10 Inclusion compound self-assembled liposome precursor, which is prepared by weight ratio from the following raw materials, reduced coenzyme Q 10 : β-cyclodextrin: egg yolk lecithin: mannitol = 1:7:0.8:8.

[0044] Take 70 parts by mass of β-cyclodextrin and 10 parts by mass of reduced coenzyme Q 10 , add 560 parts by mass of water to mix and disperse evenly, stir to form a paste, heat to 55°C, put it into a colloid mill, grind it circularly for 7 times, add water to dilute to a solid content concentration of 10%, and obtain cyclodextrin coenzyme Q 10 Grinding liquid for standby; take 8 mass parts of egg yolk lecithin, add to 560 mass parts of water, mix and disperse evenly, and obtain a phospholipid dispersion liquid for standby; take 80 mass parts of mannitol, put it into a fluidized bed as a mother nucleus, and spray into the above-mentioned phospholipid Dispersion liquid, so that the surface of mannitol particles is coat...

Embodiment 3

[0046] Oxidized coenzyme Q of the present invention 10Inclusion compound self-assembled liposome precursor, which is prepared by weight ratio from the following raw materials, oxidized coenzyme Q 10 : β-cyclodextrin: soybean lecithin: mannitol = 1:10:1.5:10.

[0047] Take 100 parts by mass of β-cyclodextrin and 10 parts by mass of oxidized coenzyme Q 10 , add 700 parts by mass of water to mix and disperse evenly, stir to form a paste, heat to 60°C, put it into a colloid mill, grind 10 times in a cycle, add water to dilute to a solid concentration of 10%, and obtain cyclodextrin coenzyme Q 10 Grinding liquid for standby; take 15 parts by mass of soybean lecithin, add to 700 parts by mass of water, mix and disperse evenly, and obtain a phospholipid dispersion for subsequent use; take 100 parts by mass of mannitol, put it into a fluidized bed as a mother nucleus, and spray into the above-mentioned phospholipid Dispersion liquid, so that the surface of mannitol particles is coat...

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Abstract

The invention discloses a self-assembled lipidosome precursor of a coenzyme Q10 inclusion compound and a preparation method of the self-assembled lipidosome precursor, and belongs to the technical field of drugs and health care products. The self-assembled lipidosome precursor of the coenzyme Q10 inclusion compound is prepared from raw materials including coenzyme Q10, cyclodextrin, lecithin and mannitol in a weight ratio being 1:5-15:0.5-1.5:5-15. A lipidosome solution can be self-assembled from the prepared lipidosome precursor in presence of intestinal juice containing cholic acid, and hasthe characteristics of higher dissolution rate and higher bioavailability.

Description

technical field [0001] The present invention relates to a kind of coenzyme Q 10 Inclusion compound self-assembled liposome precursor and preparation method thereof, the inclusion compound self-assembled liposome precursor has good therapeutic and health care effects on diseases such as cardiovascular disease, high mountain hypoxia, diabetes, low immunity, etc. It belongs to the technical field of medicines and health care products. Background technique [0002] coenzyme Q 10 (Coenzyme Q 10 ) is a compound synthesized by the human body. It is named for its side chain-polyisoprenyl at the six-position of the mother nucleus with a degree of polymerization of 10, and its structure is similar to vitamin K. coenzyme Q 10 reduced coenzyme Q 10 (Co Q 10 h 2 , Ubiquinol, ubiquinol) and oxidized coenzyme Q 10 (Co Q 10 , Ubiquinone, ubiquinone) two forms, CoQ 10 h 2 is Co Q 10 the two-electron reducer. In vivo, Co Q 10 h 2 with CoQ 10 As a type of hydrogen-donating / elec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/69A61K47/24A61K47/26A61K31/122A61P9/00A61P39/00A61P3/10A61P37/04
CPCA61K47/24A61K47/26A61K47/6951A61P3/10A61P9/00A61P37/04A61P39/00A61K9/1271A61K9/1277A61K31/122
Inventor 董英杰艾莉李晓怡邹晓峰韩亚男丁爽东长青许永超
Owner SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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