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Chlorogenic acid long-circulating liposome as well as preparation method and application thereof

A long-circulation liposome and chlorogenic acid technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as acquisition

Pending Publication Date: 2020-04-28
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In view of its special physical and chemical properties, it is impossible to obtain relevant teachings on "chlorogenic acid long-circulation liposomes" based on existing comparative documents and textbook knowledge

Method used

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  • Chlorogenic acid long-circulating liposome as well as preparation method and application thereof
  • Chlorogenic acid long-circulating liposome as well as preparation method and application thereof
  • Chlorogenic acid long-circulating liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: film dispersion method prepares the liposome of different lipid material ratio

[0033] Fix the mass ratio of chlorogenic acid to membrane material at 1:10, prepare liposomes with different lipid-material ratios according to the method in the table below, and use a laser particle size analyzer to measure the average particle size.

[0034] Table 1 Composition and particle size results of chlorogenic acid long-circulation lipid formulations with different lipid-material ratios

[0035]

[0036] Preparation:

[0037](1) Lipid material solution preparation: Weigh soybean lecithin, cholesterol and DSPE-PEG2000-OH, add absolute ethanol to dissolve to make solutions with concentrations of 20mg / ml, 10 mg / ml and 34mg / mL respectively.

[0038] (2) Preparation of drug solution: Accurately weigh the raw material drug of chlorogenic acid, add absolute ethanol and dissolve to prepare a solution with a concentration of 1.2 mg / ml.

[0039] (3) Lipid film coating: Ac...

Embodiment 2

[0041] Embodiment 2: film dispersion method prepares the liposome of different medicine fat ratio

[0042] The lipid material ratio was fixed as soybean phospholipid: cholesterol: DSPE-PEG2000-OH = 70:20:10, liposomes with different mass ratios of chlorogenic acid and membrane material were prepared, and the average particle size was measured by laser particle size analyzer.

[0043] Table 2 The composition and particle size results of the chlorogenic acid long-circulation liposome formulations with different mass ratios of chlorogenic acid and membrane materials

[0044]

[0045] Preparation:

[0046] (1) Lipid material solution preparation: Weigh soybean lecithin, cholesterol and DSPE-PEG2000-OH, add absolute ethanol to dissolve to make solutions with concentrations of 20mg / ml, 10mg / ml and 34mg / mL respectively.

[0047] (2) Preparation of drug solution: Accurately weigh the raw material drug of chlorogenic acid, add absolute ethanol and dissolve to prepare a solution wit...

Embodiment 3

[0050] Embodiment 3: change soybean phospholipid material to be egg yolk lecithin, film dispersion method prepares the liposome of different lipid material ratio

[0051] Prepared by film dispersion method, fixed the mass ratio of chlorogenic acid to membrane material at 1:10, changed the soybean lecithin material into egg yolk lecithin, prepared liposomes with different lipid material ratios according to the following table, and measured them with a laser particle size analyzer The average particle size.

[0052] (1) Lipid material solution preparation: Weigh egg yolk lecithin, cholesterol and DSPE-PEG2000-OH, add absolute ethanol to dissolve to prepare solutions with concentrations of 20 mg / ml, 10 mg / ml and 34 mg / mL.

[0053] (2) Preparation of drug solution: Accurately weigh the raw material drug of chlorogenic acid, add absolute ethanol and dissolve to prepare a solution with a concentration of 1.2 mg / ml.

[0054] (3) Lipid film coating: According to the specified mass ra...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a chlorogenic acid long-circulating liposome as well as a preparation method and application thereof. According to the chlorogenic acid liposome disclosed by the invention, a lipid material containing PEGylated phospholipid is used as a membrane material, and chlorogenic acid active ingredients are entrapped, sothat the liposome with the average particle size of 50-500nm is prepared. The chlorogenic acid long-circulating liposome provided by the invention can prolong the residence time (MRT) of chlorogenicacid in blood, slow down the drug clearance rate (CLz) and improve the plasma exposure (AUC under a drug-time curve), and is beneficial to better exerting the biological effect of chlorogenic acid.

Description

technical field [0001] The invention relates to a chlorogenic acid long-circulation liposome technology, which belongs to the technical field of medicine preparation. Background technique [0002] Chlorogenic acid, also known as coffee tannin (Chlorogenic acid, CHA for short), is an organic acid widely found in honeysuckle, leaves of Eucommia ulmoides, sunflower seeds, capillary and blue potted flowers, etc. It has antioxidant, Antibacterial, antiviral, hypoglycemic, lipid-lowering, blood pressure-lowering and immune regulation and other pharmacological effects. The molecular structure of chlorogenic acid contains o-diphenolic hydroxyl group, which is the most suitable reaction substrate for phenolase catalysis, making its chemical properties extremely unstable, and it is easily oxidized by heat and light. [0003] There are many phenolic hydroxyl groups and a carboxyl group in the structure of chlorogenic acid, which are easily inactivated and quickly eliminated in the bod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K31/216A61P35/00A61P37/02
CPCA61K9/1271A61K31/216A61K47/24A61P35/00A61P37/02
Inventor 刘玉玲杨艳芳叶军陈晓光孟盈盈高越刘东东冯遇季鸣金晶张运廖恒峰周君卓
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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