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Pharmaceutical composition of ginsenosides RG5 and RZ1 and application of pharmaceutical composition in brain protection

A technology of ginsenosides and compositions, applied in the field of pharmaceutical compositions, which can solve the problems of low drug concentration, hindering chemical components, and affecting drug efficacy, etc.

Active Publication Date: 2017-12-08
牛敏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The blood-brain barrier (BBB) ​​is a unique defense mechanism of the mammalian central nervous system (CNS). The brain microvascular endothelial cells in the brain tissue are closely connected, there is no gap between the endothelial cells, and the outer surface of the capillaries is almost all astrocytes. Surrounded by cells, this special structure forms a physiological barrier to protect the brain. This physiological barrier blocks pathogenic microorganisms, toxic products, and foreign particles, including dye particles, from the blood into the brain tissue and cerebrospinal fluid to protect the CNS from damage. , also hinders most of the chemical components from entering the CNS, or makes the concentration of the drug entering the CNS very low, seriously affecting the efficacy of the drug

Method used

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  • Pharmaceutical composition of ginsenosides RG5 and RZ1 and application of pharmaceutical composition in brain protection
  • Pharmaceutical composition of ginsenosides RG5 and RZ1 and application of pharmaceutical composition in brain protection
  • Pharmaceutical composition of ginsenosides RG5 and RZ1 and application of pharmaceutical composition in brain protection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Ginsenosides RG5 and RZ1 synergistically promote blood-brain barrier penetration

[0022] 1. Experimental method

[0023] 1. Culture and cryopreservation of mouse bEnd.3 cells

[0024] Mouse bEnd.3 cells (provided by Shanghai Cell Bank, Chinese Academy of Sciences) were cultured in DMEM high-glucose medium (containing 15% FBS, 1% 100 U / mL penicillin-streptomycin) at 37°C, 95% humidity, 5% CO 2 Culture in a constant temperature incubator, change the medium every other day, digest the cells with 0.25% trypsin when the cells grow to about 85% confluence in the culture flask, and passage them at a ratio of 1:2. Pre-prepared freezing solution (mixed solution of 10% DMSO and 90% FBS), stored in a 40°C refrigerator for pre-cooling. Take the cells in the logarithmic growth phase, discard the medium in the culture flask, wash 3 times with pre-warmed PBS, digest the cells with 0.25% trypsin, observe under the microscope, and add fresh pre-warmed medium when the cel...

Embodiment 2

[0045] Embodiment 2: Brain protection ginsenoside injection

[0046]The active ingredients are ginsenosides RG5 and RZ1, prepared with sterile water and surfactants.

Embodiment 3

[0047] Embodiment 3: brain protection ginsenoside tablet

[0048] The active ingredients are ginsenosides RG5 and RZ1, which are made into tablets with one or more solid, semi-solid or liquid excipients.

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Abstract

The invention relates to a pharmaceutical composition of ginsenosides RG5 and RZ1 and application of the pharmaceutical composition in brain protection. Active components of the pharmaceutical composition are the ginsenosides RG5 and RZ1 and can be used for preparing a medicine for the brain protection. A pharmaceutical preparation provided by the invention contains the pharmaceutical composition of the ginsenosides RG5 and RZ1 and pharmaceutically-acceptable carriers, and is prepared into pharmaceutically-acceptable dosage forms; the pharmaceutically-acceptable carriers comprise one or more of solids, semisolids or auxiliary liquid materials; the pharmaceutically-acceptable dosage forms comprise injections, tablets, capsules, granules, pills, syrup, powder and ointment. In the pharmaceutical composition provided by the invention, the ginsenosides RG5 and RZ1 have an effect of mutually promoting the permeability of a blood brain barrier; the permeability of the blood brain barrier of the ginsenosides RG5 and RZ1 is remarkably higher than that of single ginsenosides RG5 or RZ1, therefore, the ginsenosides RG5 and RZ1 can be combined for a drug.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a pharmaceutical composition of ginsenosides RG5 and RZ1 and its application in brain protection. Background technique [0002] Ginsenosides are known to have various pharmacological effects, including brain protection and brain neuroprotection. Ginsenoside RG5 and RZ1 are rare saponins obtained by dehydration of ginsenoside RG3, and they are isomers of each other. The only difference is that the former is C20-C22 cisene and the latter is C20-C22 transene (see the formula below). The applicant's research found that ginsenosides RG5 and RZ1 have more excellent brain protection and brain neuroprotection than ginsenoside RG3. However, ginsenosides RG5 and RZ1 have relatively large molecular weights and a disaccharide group in their side chains, resulting in low blood-brain barrier passage rates and low availability. [0003] [0004] The blood-brain barrier (BBB) ​​is a unique de...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P25/00
CPCA61K31/704A61K2300/00
Inventor 张丹丹杨勇彭雨泽
Owner 牛敏
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