Application of 5'-methoxy-3',4'-methylenedioxy cinnamic acid isobutyl amide in preparing antidepressant medicaments

A technology of cinnamic acid isobutylamide and methylenedioxy, applied in the preparation of antidepressant drugs, in the field of amide compounds, can solve problems such as difficult to obtain satisfactory curative effect, no antidepressant drugs, emotional depression, depression, etc. , to achieve good therapeutic and preventive effects

Active Publication Date: 2011-11-16
TIANJIN TASLY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] 4. Secondary depression, such as some hypertensive patients, after taking antihypertensive drugs, lead to continuous depression and depression
Clinical studies have also shown that synthetic d

Method used

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  • Application of 5'-methoxy-3',4'-methylenedioxy cinnamic acid isobutyl amide in preparing antidepressant medicaments
  • Application of 5'-methoxy-3',4'-methylenedioxy cinnamic acid isobutyl amide in preparing antidepressant medicaments
  • Application of 5'-methoxy-3',4'-methylenedioxy cinnamic acid isobutyl amide in preparing antidepressant medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0157] Embodiment 1 Preparation of compound G-1 of the present invention

[0158]Take the above-ground part of the betel leaf, crush it, add 8 times the amount of 95% ethanol, reflux extraction twice, each time for 2 hours, filter, combine the extracts, and concentrate under reduced pressure at 60°C to a paste. The extract is dissolved with 40% ethanol, separated through a macroporous adsorption resin column (crude drug-resin ratio 3:1), removed with 50% ethanol, then eluted with 95% ethanol, and the eluate is collected and concentrated to a paste. The extract was mixed with 100-200 mesh silica gel, separated by column according to the dry weight of the sample-silica gel ratio 1:30, and eluted successively with petroleum ether-ethyl acetate (5:1 and 3:1) as the mobile phase. Thin-layer chromatography detection, combined the same parts, to get G-1 ~ G-13, wherein the G-1 part was recrystallized with ethanol-water to get the monomer, compound G-1 (ie: compound 5'-methoxy- 3',4'...

Embodiment 2

[0159] The preparation of embodiment 2 tablet

[0160] G-1 20g

[0161] Microcrystalline Cellulose 50g

[0162] Lactose 50g

[0163] Starch 51g

[0164] Sodium carboxymethyl starch 12g

[0165] 5% PVP absolute ethanol appropriate amount

[0166]

[0167] Magnesium Stearate 3g

[0168] Made into 1000 pieces

[0169] G-1 and other excipients in the prescription were passed through a 100-mesh sieve, and the prescription amount of G-1 was weighed, mixed with microcrystalline cellulose, starch and sodium carboxymethyl starch, and mixed evenly with an appropriate amount of PVP absolute ethanol solution. Soft material, granulated with a 14-mesh sieve, dried at 50-60°C for 1 hour, added the prescribed amount of magnesium stearate and granulated with a 14-mesh sieve. Take the granules and press them into tablets with a special diamond-shaped special-shaped die.

Embodiment 3

[0170] The preparation of embodiment 3 capsules

[0171] G-1 20g

[0172] Starch 200g

[0173] Sodium carboxymethyl starch 12g

[0174] 5% PVP absolute ethanol appropriate amount

[0175] Magnesium Stearate 3g

[0176]

[0177] Make 1000 capsules

[0178] G-1 and other excipients in the prescription were passed through a 100-mesh sieve, and the prescription amount of G-1 was weighed and mixed with starch and sodium carboxymethyl starch in equal amounts, and the soft material was made with an appropriate amount of PVP absolute ethanol solution, 14 mesh Sieve and granulate, dry at 50-60°C for 1 hour, add the prescribed amount of magnesium stearate and granulate with a 14-mesh sieve. Get the granules and pack into capsules to make G-1 capsules.

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation, and relates to application of an amide compound 5'-methoxy-3',4'-methylenedioxy cinnamic acid isobutyl amide extracted from plants in preparing antidepressant medicaments.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to the preparation of antidepressant drugs by using amide compound 5′-methoxy-3′,4′-methylenedioxycinnamic acid isobutylamide extracted from plants application. Background technique [0002] Depression is a psychiatric syndrome characterized by mood disorders caused by a variety of reasons. Its clinical manifestations are significant and persistent depression; inattention or decreased thinking ability; insomnia, loss of appetite; tired of daily life; mental irritability or sluggishness; thoughts of suicide. Depression has so far become a major mental health problem worldwide. The incidence of depression in western developed countries is 8-10%. According to the announcement of the World Health Organization, there are currently about 340 million people with various depressions in the world, accounting for about 5% of the world's total population. Among adults aged...

Claims

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Application Information

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IPC IPC(8): A61K31/36A61P25/24
CPCA61K31/16A61K9/2059A61K36/67A61P25/24
Inventor 马晓慧靳元鹏周水平罗学军周王谊张莉华陈晓鹏王晶王根辈
Owner TIANJIN TASLY PHARMA CO LTD
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