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Magnolin preparation, preparation method and application

A technology of magnolialine and magnolialine phospholipids, which is applied in the field of medicine, can solve the problems of low bioavailability and low fat solubility of magnolialine, and achieve high bioavailability, improved oral availability, and increased fat solubility Effect

Active Publication Date: 2021-02-26
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The invention provides a magnolia preparation and its preparation method and application, solving the problems of low fat solubility and low bioavailability of magnolia in the prior art

Method used

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  • Magnolin preparation, preparation method and application
  • Magnolin preparation, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation method of Magnolin

[0041] (1) Preparation of crude extract:

[0042] Grind 250g jujube kernels, pass through a 40-mesh sieve, degrease with petroleum ether, add 1200ml, 800ml, 600ml of 70% ethanol aqueous solution, heat and reflux for extraction 3 times, each time for 1 hour, filter, and combine the extracts , the filtrate is concentrated with ethanol until it has no alcohol smell, then dissolved with 2 times the amount of water, extracted 5 times with n-butanol, the extract is concentrated under reduced pressure, and the solvent is recovered to obtain the n-butanol crude extract, which is the sample to be separated. figure 1 shown.

[0043](2) Adopt high-speed countercurrent chromatography to separate magnolialine and spinosin, 6 "'-feruloylspinosin:

[0044] Take n-butanol, ethyl acetate and water at a volume ratio of 2:3:5, place them in a separatory funnel to prepare a two-phase solvent system, take the upper phase as the stationary phase, and the lo...

Embodiment 2

[0049] Pharmacodynamic experiment of magnolanine on CUMS depression and insomnia mouse model

[0050] 1 Experimental materials

[0051] 1.1 Experimental animals

[0052] Healthy male ICR mice (weight 20±2g) were purchased from the Experimental Animal Center of the Institute of Radiological Medicine, Chinese Academy of Medical Sciences; they were bred for 3 days to adapt to the environment before the experiment. The room temperature is 22±2°C, and the relative humidity is 65% to 70%. Sunlight for 12 hours, free diet and water intake.

[0053] 1.2 Reagents and medicines:

[0054] Magnolin, spinosin (self-made in this laboratory); venlafaxine hydrochloride sustained-release capsules (Chengdu Kanghong Pharmaceutical Group Co., Ltd.)

[0055] 1.3 Instruments

[0056] Stopwatch (Switzerland Hoyer-Olidas factory);

[0057] AUX 120 analytical balance (Shimadzu (Hong Kong) Co., Ltd.);

[0058] ZH-YLS-1A animal autonomous activity recorder (Anhui Zhenghua Biological Instrument Eq...

Embodiment 3

[0108] Preparation and detection of magnolia alkali phospholipid complex

[0109] 1 Experimental materials

[0110] 1.1 Drugs and reagents

[0111] Magnolin (made in laboratory, purity>98%);

[0112] Soy lecithin (Shanghai Lanji Biological Co., Ltd., batch number: 20160628);

[0113] Absolute ethanol, dichloromethane, methanol, ethyl acetate, n-butanol (analytical grade, Tianjin Benchmark Chemical Reagent Co., Ltd.);

[0114] 1.2 Instruments

[0115] RCT basic magnetic stirrer (Guangzhou Yike Laboratory Technology Co., Ltd.);

[0116] 214-type differential scanning calorimeter (Germany Netzsch);

[0117] Model 380 Fourier transform infrared spectrometer (Hitachi High-Tech Corporation, Japan);

[0118] HT7700 Transmission Electron Microscope (Hitachi High-Tech Corporation, Japan);

[0119] Agilent1100 high performance liquid chromatography (Agilent Technologies Co., Ltd.);

[0120] AUX120 analytical balance (Shimadzu (Hong Kong) Co., Ltd.);

[0121] 2 Experimental meth...

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Abstract

The invention discloses magnolialine preparations, preparation methods and applications, one of which is a magnolialine phospholipid complex, and the other is a magnolialine phospholipid complex-temperature-sensitive in-situ gel for nasal use. The preparation method of the invention has the characteristics of good separation effect, large preparation amount, less loss and simple operation. The mass ratio of magnolialine and phospholipids in the magnolialine-phospholipid complex is 1-4:2-1, and the preparation method involves dissolving and mixing the components of the formula amount in an organic solvent, preparation. The obtained magnolialine phospholipid complex is added with temperature-sensitive in-situ gel auxiliary materials to prepare magnolialine-phospholipid complex-temperature-sensitive in-situ gel. Animal pharmacodynamic experiments show that magnolialine and its two preparations have significant improvement and therapeutic effects on depression and insomnia.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a magnolanine preparation, an active ingredient of alkaloids, a preparation method thereof, and an application in treating depression and insomnia. Background technique [0002] Depression is a syndrome characterized by significant and persistent depression as the main clinical manifestation. In severe cases, suicide and self-mutilation will occur. At present, the global incidence of depression has reached 3.3%, while in developed countries it exceeds 6%. There are more than 700 million people with depression worldwide, and the prevalence of depression in my country is between 3% and 5%. With the development of society, this figure is still rising. Insomnia refers to the inability to sleep normally. The specific symptoms are tossing and turning, poor sleep quality, and reduced sleep time. Severe cases may cause insomnia all night [3] . In today's society, more and more people suffer from i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/473A61K9/06A61K47/24A61P25/24A61P25/20
CPCA61K9/0043A61K9/06A61K31/473A61K47/24A61P25/20A61P25/24
Inventor 乔卫李冰洁
Owner TIANJIN MEDICAL UNIV
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