Application of bilobalide as synergist in preparation of drug for preventing cranial nerve injury diseases

A technology of bilobalide and synergist, which is applied in the directions of nervous system diseases, drug combinations, medical preparations containing active ingredients, etc., can solve problems such as no data display, etc. stable effect

Inactive Publication Date: 2017-05-31
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] There is no data in the existing literature to show that bilobalide, bilobalide extract, bilobalide or bilobalide extract’s hydroxyl derivatives, especially its glycoside, ester, ether derivatives, etc., can improve the permeability of the blood-brain barrier. Functional report of promoting drug molecule entry into brain tissue

Method used

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  • Application of bilobalide as synergist in preparation of drug for preventing cranial nerve injury diseases
  • Application of bilobalide as synergist in preparation of drug for preventing cranial nerve injury diseases
  • Application of bilobalide as synergist in preparation of drug for preventing cranial nerve injury diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Ginkgo lactone and its extracts on the blood-brain barrier in vitro (in vitro BBB model) open research test:

[0044] 1. Experimental scheme:

[0045] 1.1 Establishment of an in vitro blood-brain barrier model (BBB): culture and resuscitate human glial cells (HEB cells) and immortalized brain microvascular endothelial cells (hCMEC / D3 cells), after the cells are confluent, digest and centrifuge HEB cells for 3×10 5 Cells / ml were inoculated in the lower chamber of the transwell 12-well plate. After the cells adhered to the wall, low-glucose medium was added for culture. When the cells grew to 80%, the cells were placed in the upper layer of the transwell chamber with 7 × 10 cells. 5 hCMEC / D3 cells were seeded at a density of cells / ml. After the cells were confluent, the transendothelial cell electrical resistance (TEER) of the co-culture model was measured by Millicell ERS, which was the sum of endothelial cells (EC) and filter layer TEER. The culture pool was used as a...

Embodiment 2

[0054] Ginkgo lactone extract (ginkgo lactone content ≥ 99.0%) 5, 15g;

[0055] Active ingredients of traditional Chinese medicine: ginsenoside extract (ginsenoside Rg1 content ≥ 95%) 300g;

[0056] Weigh the above-mentioned various extracts in the recipe quantity, and mix them uniformly according to the equal increment method, and the obtained mixture is recorded as YXN1-1 (containing 5g ginkgo lactone extract and 300g ginsenoside extract) and YXN1-2 (containing 15g ginkgo internal ester extract and 300g ginsenoside extract).

[0057] Efficacy test:

[0058] Treatment group: YXN1-1 and YXN1-2 were made into a suspension, and the YXN1-1 treatment group was given a dose of 101.6 mg / kg (equivalent to 100 mg / kg of ginsenoside extract), 20 ml / kg volume, and 5 SD rats were given orally. Rats; YXN1-2 treatment group was given 5 SD rats by gavage at a dose of 105 mg / kg (equivalent to 100 mg / kg of ginsenoside extract) and a volume of 20 ml / kg;

[0059] Control group: another ginsen...

Embodiment 3

[0067] Bilobalide extract (bilobalide content ≥ 20.0%) 20, 40g;

[0068] Active ingredients of traditional Chinese medicine: ginsenoside extract (ginsenoside Rg1 content ≥ 30%) 200g;

[0069] Take the above-mentioned various extracts of the prescription amount, mix them uniformly by the method of equal increase, and the obtained mixture is recorded as YXN2-1 (containing 20g bilobalide extract and 200g ginsenoside extract) and YXN2-2 (containing 40g bilobalide extract). ester extract and 200g ginsenoside extract).

[0070] Drug efficacy experiment:

[0071] Treatment group: YXN2-1 and YXN2-2 were made into suspension, and YXN2-1 treatment group was dosed at 220mg / kg (equivalent to 200mg / kg of ginsenoside extract) and 20ml / kg capacity, and 5 SD large Rats; YXN2-2 treatment group was given a dose of 240mg / kg (equivalent to 200mg / kg of ginsenoside extract), 20ml / kg capacity, and 5 SD rats were administered orally;

[0072] Control group: another ginsenoside extract was taken to...

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PUM

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Abstract

The present invention discloses application of bilobalide as a synergist in preparation of a drug or a heath product for preventing cranial nerve injury diseases. An inventor discovers that compounds of bilobalides, particularly bilobalide, bilobalide extracts, and hydroxyl derivatives of bilobalides, particularly glucoside derivatives, ester derivatives and ether derivatives can well promote drug molecules with a treating or health care function on cranial nerve injury diseases to enter brain tissues, wherein the drug molecules comprise ginsenoside, stibene glucoside, resveratrol, levodopa, edaravone, vinpocetine, nicergoline, citicoline, oxiracetam and the like; under the conditions of not increasing drug concentration in blood, the concentration of bilobalide can be increased to a large extent in the brain tissues, so that the efficacy of the drug can be improved, and side effects and adverse reactions of the drug can be reduced.

Description

technical field [0001] The invention relates to a new application of a compound and a new drug or health care product composition based on the application, in particular to the application of bilobalide as a synergist in the preparation of drugs or health care products for preventing and treating cranial nerve injury diseases. Background technique [0002] Cerebral ischemic injury diseases, neurodegenerative diseases and other brain diseases related to the central nervous system, such as ischemic stroke, chronic cerebral ischemia, stroke sequelae, senile dementia, Parkinson's disease, Alzheimer's disease The development of new drugs to treat these diseases is constrained by many factors, the most important of which is how the drugs pass through the blood-brain barrier. Basically, 100% of macromolecular drugs, including peptides, recombinant proteins, monoclonal antibodies, drugs based on RNA interference technology, and gene therapy-related drugs, cannot cross the blood-brai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P25/28A61P25/00A61K36/258A61K31/198A61K31/4375A61K31/48A61K31/05A61K31/7028A61K31/4152A61K31/7068A61K31/4015
CPCA61K31/05A61K31/198A61K31/365A61K31/4015A61K31/4152A61K31/4375A61K31/48A61K31/7028A61K31/7068A61K36/258A61K2300/00
Inventor 贝伟剑郭姣
Owner GUANGDONG PHARMA UNIV
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