Medicine composition for anesthesia and sedation hypnosis and application of medicine composition for anesthesia and sedation hypnosis

An anesthesia hypnosis and composition technology, applied in the field of medicine, can solve problems such as social function impairment, influence on work and study, cognitive ability decline, etc., and achieve remarkable effects.

Inactive Publication Date: 2015-10-07
周玉梅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 2. Impaired social function. Symptoms such as dizziness, fatigue, lack of energy, fatigue, drowsiness, and lack of concentration during the day. In severe cases, cognitive decline will affect work and study
At present, there is no literature report that this kind of compound has sedative and hypnotic biological activity

Method used

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  • Medicine composition for anesthesia and sedation hypnosis and application of medicine composition for anesthesia and sedation hypnosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Effect test of QSK-02 on mouse non-alcoholic fatty liver model

[0022] 36 clean-grade Kunming mice, half male and half female, weighing (20±2) g, were randomly divided into blank control group, diazepam positive control group (2mg / kg), QSK-02 group (50mg / kg), Once a day, for 3 consecutive days, the volume of gavage was 20ml / kg, and the blank control group was gavaged with the same volume of distilled water. After 60 min of administration on the second day, the mouse autonomic activity meter was used to record the number of standing and the number of activities of the mice within 5 min after they were put into the box. After 60 minutes of the last administration, the mice in each group were intraperitoneally injected with pentobarbital sodium 50 mg / kg, and sleep was indexed by the disappearance of righting reflex, and those who kept the animal’s back-down posture for more than 30 seconds were judged as the disappearance of righting reflex. The time from the ...

Embodiment 2

[0027] Embodiment 2: Preparation of 1-azetidin-3-yl-4-propionylpiperazine

[0028] (a) 1-[1-(Diphenylmethyl)azetidin-3-yl]piperazine

[0029] 1-(Diphenylmethyl)azetidin-3-yl methanesulfonate (see J.Org.Chem.; 56; 1991; 6729; 25 g, 78.6 mmol) was stirred under nitrogen at 60°C , piperazine (67.7 g, 0.79 mol) and a mixture of anhydrous acetonitrile overnight. The mixture was cooled and partitioned between water and dichloromethane. The organic layer was washed with water and brine. The solution was dried over Na2SO4, and the solvent was evaporated. The residue was purified by silica gel column chromatography (methanol-dichloromethane 5:95). 17.5 g (72%) of 1-[1-(diphenylmethyl)azetidin-3-yl]piperazine were obtained as a yellow oil. 1HNMR (400MHz, CDCl3): 2.1-2.4(m, 4H), 2.8-2.9(m, 2H), 3.0(m, 4H), 3.4-3.5(m, 2H), 3.7-3.9(m, 1H), 4.4 (s, 1H), 7.2-7.4 (m, 10H); LCMS: m / z 308 (M+1)+.

[0030] (b) 1-[1-(diphenylmethyl)azetidin-3-yl]-4-propionylpiperazine

[0031] 1-[1-(Diphe...

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Abstract

The invention belongs to the technical field of medicines, and discloses a medicine composition for anesthesia and sedation hypnosis and an application of the medicine composition for anesthesia and sedation hypnosis. The composition is prepared by an active ingredient and a pharmaceutically acceptable auxiliary material; and the active ingredient comprises 1-azetidine-3-yl-4-propionyl piperazine. The medicine composition is obvious in effect when being used for anesthesia and sedation hypnosis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition for anesthesia, sedation and hypnosis and its application. Background technique [0002] In anesthesia technology, according to different medical operations and patients' needs, the depth and degree of anesthesia are not the same, including not only surgical anesthesia, analgesia anesthesia, but also effective sedative anesthesia, and the treatment of insomnia is also a part of sedative anesthesia. kind. Insomnia is a subjective experience that affects daytime social function due to difficulties in falling asleep and maintaining insomnia. The quality or quantity of sleep does not meet the normal physiological needs. It is the most common sleep disorder disease. Insomnia is a very common phenomenon in today's fast-paced society and intensified competition. The prevalence of insomnia is very high. The prevalence in Europe and the United St...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61P25/20A61P25/08A61P23/00
Inventor 周玉梅
Owner 周玉梅
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