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Application of Boropinol-B in preparation of medicines for treating insomnia

A technology for drugs and insomnia, applied in the field of preparation of drugs for the treatment of insomnia, to achieve the effects of short biological half-life, enhanced activity, and fast elimination of metabolism in the body

Active Publication Date: 2022-01-14
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the effect of Boropinol-B in the treatment of insomnia has not been reported

Method used

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  • Application of Boropinol-B in preparation of medicines for treating insomnia
  • Application of Boropinol-B in preparation of medicines for treating insomnia
  • Application of Boropinol-B in preparation of medicines for treating insomnia

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1B

[0067] Preparation of Example 1 Boropinol-B

[0068] Experimental Materials:

[0069] 3,4,5-Trimethoxycinnamic acid (C10067426, Shanghai Macklin Company)

[0070] Methanol (2021091602, Chengdu Kelong Reagent Factory)

[0071] Concentrated sulfuric acid (170303, Sichuan Xilong Chemical Company)

[0072] Ethyl acetate (20210922, Chengdu Jinshan Chemical Reagent Company)

[0073] Diisobutylaluminum hydride (C11337170, Shanghai McLean Company)

[0074] Anhydrous magnesium sulfate (Q / 12KM3936-2019, Tianjin Kemiou Company)

[0075] Anhydrous tetrahydrofuran (MOTRRBDK, Shanghai Sarn Chemical Technology Co., Ltd.)

[0076] N,N-Dimethylformamide (MQRD1HIE, Shanghai Saen Chemical Technology Co., Ltd.)

[0077] Petroleum ether (July 20, 2019, Tianjin Fuyu Fine Chemical Co., Ltd.)

[0078] NaH (C10255393, Shanghai McLean Company)

[0079] CH 3 I (MA1229A, Shanghai McLean Company).

[0080] Experimental steps:

[0081] Take 2.0 ~ 5.0 g of 3,4,5-trimethoxycinnamic acid and dissol...

preparation Embodiment 2B

[0082] Preparation of Example 2 Boropinol-B Oral Emulsion

[0083] Experimental Materials:

[0084] Boropinol-B (20210530, self-made in the laboratory);

[0085] Soybean oil (DD20200603, Shandong Ruisheng Pharmaceutical Excipients Co., Ltd.);

[0086] Egg yolk lecithin (202008013, Shanghai Taiwei Pharmaceutical Co., Ltd.);

[0087] Glycerin (20191213, Zhejiang Suichang Huikang Pharmaceutical Co., Ltd.).

[0088] Experimental steps:

[0089] Add 5.0~22.0 g of egg yolk lecithin and 10.0~25.0 g of medically acceptable glycerin into an appropriate amount of pharmaceutical water, heat to 60~80°C under nitrogen protection, stir to dissolve, and prepare an aqueous phase; Boropinol-B 0.5 ~30.0 g is added to 50~150 g of medicinal soybean oil, heated to 60~80°C, stirred to dissolve, and prepared into an oil phase. Add the oil phase to the water phase, and after 5 minutes of high-speed shearing, add pharmaceutical water to 1000 mL to prepare colostrum. Continue to transport the col...

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Abstract

The invention discloses a new application of a compound Boropinol-B in preparation of medicines for treating insomnia for the first time. Boropinol-B as shown in a formula I acts on a neuron GABAA receptor, and enhances chloride ion internal flow to hyperpolarize nerve cells, thereby achieving central nervous sedation and inhibiting effects. The Boropinol-B can be used for improving GABA level in the brain by enhancing the activity of GABAergic neurons in a VLPO region in the brain of an insomnia model mouse and thus increasing the release of GABA. The compound has remarkable sedative and hypnotic effects, fast onset of action, quick in-vivo metabolism elimination, short biological half-life period, neither obvious residual effect nor obvious toxic side effects, and is expected to become medicines for treating insomnia with great application prospects.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the application of compound Boropinol-B in the preparation of drugs for treating insomnia. Background technique [0002] Insomnia is the most common sleep disorder, manifested as difficulty in falling asleep, maintaining sleep and impaired daytime function. About 30% of the world's people are suffering from insomnia. Long-term insomnia will make patients sleepy during the day, lack of energy, weaken the body's immunity, and may even induce cardiovascular and cerebrovascular diseases or psychological disorders. [0003] Drug therapy is an important means of treating insomnia. The currently approved drugs for the treatment of insomnia include nonbenzodiazepines (NBZDs), benzodiazepines (BZDs), and melatonin receptors. Agonists, antidepressants, and antipsychotics. At present, there are still many side effects of sedative and hypnotic drugs. For example, non-benzodiazepine drugs represente...

Claims

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Application Information

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IPC IPC(8): A61K31/09A61K36/75A61P25/20
CPCA61K31/09A61K36/75A61P25/20
Inventor 毛声俊母珂蔓张检冯欣倩张迪李康宁杨鹏
Owner SICHUAN UNIV
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