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Application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation

A kind of technology with honokiol and uses, applied in the field of medicine

Active Publication Date: 2014-06-18
CHENGDU JINRUI FOUND BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no report about the ability of honokiol to penetrate the blood-brain barrier and the blood-cerebrospinal fluid barrier and enter the solid tissue of the brain to prevent or treat intracranial space-occupying lesions and inflammatory diseases of intracranial tissues and organs

Method used

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  • Application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation
  • Application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation
  • Application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of embodiment one honokiol injection

[0040] Prepared a kind of intravenous injection preparation of honokiol, formula is: honokiol 0.2%, Cremophor EL (polyoxyethylene castor oil) 1.5%, ethanol 1.5%, vitamin C 0.2%, EDTA disodium salt 0.03% , the water balance.

[0041] Preparation method: Accurately weigh the drug, add Cremophor EL and ethanol, stir until the drug is completely dissolved, add the aqueous solution of vitamin C and EDTA disodium salt, stir evenly, add water for injection to the specified amount, stir evenly until clear, and dilute hydrochloric acid or Adjust the pH to neutral with dilute sodium hydroxide. Filtration, potting, sterilization.

Embodiment 2

[0042] Example 2 Honokiol Injection Penetrates Blood Brain Barrier and Blood Cerebrospinal Fluid Barrier Test after Intravenous Administration

[0043] Laboratory method: 30 male SD rats with a body weight of 220-260g (from the West China Animal Room of Sichuan University), 6 for the determination of drug concentration-time curves in plasma, and another 24 for 5 minutes, 10 Minutes, 60 minutes and 120 minutes four time points (6 rats for each time point) drug concentration test in the brain and cerebrospinal fluid. After 6 rats were anesthetized, they were fixed in a supine position, and the right common carotid artery was intubated; the tail vein was given honokiol 20 mg / kg body weight, and the injection was prepared according to the magnolol injection in Example 1. Blood was collected at 0 minutes, 5 minutes, 10 minutes, 15 minutes, 30 minutes, 45 minutes, 60 minutes, 90 minutes and 120 minutes, and centrifuged at low temperature to obtain plasma. HPLC analysis drug concent...

Embodiment 3

[0053] Example 3 In vitro proliferation test of honokiol inhibiting mouse 9L gliosarcoma cells and human U251 glioma cells

[0054] Laboratory method: Mouse 9L gliosarcoma cells and human U251 glioma cells were cultured in 96-well plates, and the plating density was 5×10 4 After the cells adhered to the wall, honokiol of different concentrations (0-32 μg / mL) was added, and the fresh DMEM medium was used as a blank. After incubation for 24 hours, the absorbance value was measured at 570 nm by the MTT method, and the IC was calculated. 50 . see results image 3 (A, C), the IC of honokiol on mouse 9L gliosarcoma cells 50 was 15.61μg / mL, while IC for human U251 glioma cells 50 It was 16.38 μg / mL.

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Abstract

The invention relates to the technical field of medicines and aims at solving the technical problem about providing a new effective choice for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation. The scheme for solving the technical problem provides an application of Honokiol to preparing drugs for preventing or treating intracranial space occupying lesion and intracranial tissues and organs inflammation. The invention further provides the application of Honokiol combined with carmustine (BCNU) to preventing or treating primary or metastatic tumors of brain, and the application prospect is bright.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the use of honokiol in the preparation of medicines for preventing or treating intracranial space-occupying lesions and intracranial tissue and organ inflammation. Background technique [0002] Intracranial space-occupying lesions and inflammation of intracranial tissues and organs are one of the main diseases that endanger human health. However, the restriction of blood-brain barrier and blood-cerebrospinal fluid barrier on the entry of drugs into the central nervous system hinders the treatment of these diseases with traditional drugs and targeted drugs. Therefore, a prerequisite for the treatment of these diseases is that the drug must penetrate the blood-brain barrier and the blood-cerebrospinal fluid barrier. The blood-brain barrier and the blood-cerebrospinal fluid barrier are formed by capillary endothelial cells, tight junctions between endothelial cells, basement membranes, and gli...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/17A61K31/05A61K9/08A61P25/00A61P29/00A61P35/04
Inventor 陈俐娟魏于全赖新天王先火
Owner CHENGDU JINRUI FOUND BIOTECH CO LTD
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