Venlafaxine slow-release preparation and preparation method thereof

A technology of sustained-release preparations and venlafaxine, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, and medical preparations containing active ingredients, etc., which can solve the potential safety hazards of operators, high cost, and high viscosity. problems, to achieve the effect of reducing the number of medications, lowering equipment requirements, and improving compliance

Active Publication Date: 2013-08-14
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many relevant literature reports on venlafaxine sustained-release preparations, and 97109594.9 discloses venlafaxine sustained-release preparation pellets, a mixture composed of venlafaxine, microcrystalline cellulose, and hypromellose. Squeeze and spheronize to obtain vegetarian pills, add ethyl cellulose and hydroxypropyl methylcellulose coating materials to the mixture of dichloromethane and absolute ethanol to obtain sustained-release preparations, and the coating solution of this method contains highly toxic Dichloromethane and flammable and explosive absolute ethanol not only pose safety hazards to operators, but also have extremely high requirements on equipment
200610165403.7 discloses a sustained-release coated pellet for 24 hours, comprising a ball core, an isolation layer, a sustained-release layer, a hypromellose coating for an isolation layer, and an acrylic resin coating for a sustained-release layer. Layer coating method, the process is cumbersome and the cost is high
200680032546.9 discloses a controlled-release pharmaceutical composition of venlafaxine hydrochloride and its preparation method. Venlafaxine hydrochloride is sprayed onto an inert core composed of sucrose and starch and coated with a lipophilic material. This method is adopted in Lipophilic materials require a large amount of organic solvents to dissolve, requiring high equipment and potential safety hazards
200810204299.7 discloses the preparation method of venlafaxine sustained-release preparation, venlafaxine, ethyl cellulose, and hydroxypropyl methyl cellulose are evenly dispersed in isopropanol, sprayed onto sucrose pellet cores, and dried to obtain drug-coated pellets ;Polyacrylic acid resin water dispersion coating, however, the viscosity of ethyl cellulose and isopropanol is extremely high after mixing, and the spraying process cannot be precisely controlled, so suitable pellets cannot be obtained

Method used

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  • Venlafaxine slow-release preparation and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0020] Composition of pellets:

[0021] 16 parts of microcrystalline cellulose blank pills, 80 parts of venlafaxine, 78 parts of microcrystalline cellulose, 20 parts of dextrin, 12 parts of hypromellose, 14 parts of ethyl cellulose, 210ml of water

[0022] Coating composition:

[0023] 330 parts of polyacrylic resin, 51 parts of talcum powder, 0.4 parts of simethicone

[0024] Preparation:

[0025] (1) Preparation of ball core: sieve and mix the prescribed amount of venlafaxine, microcrystalline cellulose, dextrin, hypromellose, and ethyl cellulose, and put them into the powder supply chamber, and the microcrystalline cellulose is blank The pellets are placed in the coating granulator, and the powder is supplied while spraying water until the powder is all layered on the inert core.

[0026] (2) Coating solution configuration: take the prescribed amount of talcum powder, defoamer and 60ml of water and mix evenly, and then mix evenly with polyacrylic acid resin to obtain a c...

Embodiment 2

[0029] Composition of pellets: 18 parts of microcrystalline cellulose blank pills, 85 parts of venlafaxine, 83 parts of microcrystalline cellulose, 20 parts of dextrin, 12 parts of hypromellose, 13 parts of ethyl cellulose, 220ml of water

[0030] Coating composition: 340 parts of polyacrylic acid resin, 48 parts of talcum powder, 0.3 part of simethicone

[0031] Preparation:

[0032] (1) Preparation of ball core: sieve and mix the prescribed amount of venlafaxine, microcrystalline cellulose, dextrin, hypromellose, and ethyl cellulose, and put them into the powder supply chamber, and the microcrystalline cellulose is blank The pellets are placed in the coating granulator, and the powder is supplied while spraying water until the powder is all layered on the inert core.

[0033] (2) Coating solution configuration: take the prescribed amount of talcum powder, defoamer and 58ml of water and mix evenly, and then mix evenly with polyacrylic acid resin to obtain a coating solution....

Embodiment 3

[0036] Composition of pellets: 11 parts of microcrystalline cellulose blank pills, 62 parts of venlafaxine, 79 parts of microcrystalline cellulose, 28 parts of dextrin, 10 parts of hypromellose, 11 parts of ethyl cellulose, 180ml of water

[0037] Coating composition: 310 parts of polyacrylic acid resin, 43 parts of talcum powder, 0.3 part of simethicone

[0038] Preparation:

[0039] (1) Preparation of ball core: sieve and mix the prescribed amount of venlafaxine, microcrystalline cellulose, dextrin, hypromellose, and ethyl cellulose, and put them into the powder supply chamber, and the microcrystalline cellulose is blank The pellets are placed in the coating granulator, and the powder is supplied while spraying water until the powder is all layered on the inert core.

[0040] (2) Coating solution configuration: take the prescribed amount of talcum powder, defoamer and 48ml of water and mix evenly, and then mix evenly with polyacrylic acid resin to obtain a coating solution. ...

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Abstract

The invention provides a venlafaxine slow-release preparation as an antidepressant medicament and a preparation method thereof. The venlafaxine slow release preparation can be released persistently and stably to keep stable plasma concentration, and is bound to be taken once every day. The preparation process is simple and feasible, requires no solvent, and is suitable for industrialized production.

Description

technical field [0001] The invention relates to an antidepressant drug and a preparation method thereof, in particular to a venlafaxine sustained-release preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations Background technique [0002] Depression is recognized by the medical community as a common mental illness. One out of every 20 people in the world suffers from depression, and about 850 million people suffer from it every year, causing suicidal tendencies or dying of suicide, which brings great harm to society and families. economic and psychological burden. In response to the increasing incidence of depression and social harm, medical workers continue to develop new antidepressant drugs. According to the different mechanisms of action, currently commonly used antidepressants can be simply divided into four categories: monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants (TCAs), selective serotonin reuptake inhib...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/137A61K9/52A61K47/38A61K47/36A61K47/32A61P25/24
Inventor 黄河耿玉先
Owner BEIJING WINSUNNY PHARMA CO LTD
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