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Sustained-release microtablet capsule of 5-hydroxytryptamine, norepinephrine and dopamine reuptake inhibitor and preparation method of sustained-release microtablet capsule

A norepinephrine and reuptake inhibitor technology, applied in the field of medicine, can solve the problems of high production cost, unfavorable, inconsistent coating thickness of pellets, etc., to reduce energy consumption and production cost, reduce variation and individual differences, The effect of reducing the incidence of adverse reactions

Pending Publication Date: 2021-04-30
蒋海松
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] When preparing venlafaxine hydrochloride sustained-release rubber pellets by extrusion spheronization, special extrusion equipment and spheronization equipment are required. The single production yield of this process route is low, and materials that do not meet the particle size requirements need to be re- Extrusion, spheronization, multiple prescriptions to obtain higher yield, therefore, the continuity of production is very poor
In addition, due to the wide particle size range of the pellets, the coating thickness of the pellets with different particle sizes is inconsistent when the fluidized bed coating is used. Thin, resulting in differences in the release curves of pellets with different particle sizes, which results in poor repeatability of the dissolution curves
The fluidized bed coating process takes a long time, consumes a lot of energy, and the production cost is high, which is not conducive to reducing production costs

Method used

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  • Sustained-release microtablet capsule of 5-hydroxytryptamine, norepinephrine and dopamine reuptake inhibitor and preparation method of sustained-release microtablet capsule
  • Sustained-release microtablet capsule of 5-hydroxytryptamine, norepinephrine and dopamine reuptake inhibitor and preparation method of sustained-release microtablet capsule
  • Sustained-release microtablet capsule of 5-hydroxytryptamine, norepinephrine and dopamine reuptake inhibitor and preparation method of sustained-release microtablet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] According to the prescription ratio in the table, take water and add hydroxypropyl cellulose, stir to dissolve, as a binder.

[0020] Take the venlafaxine hydrochloride and microcrystalline cellulose in the prescription ratio and put them in a wet mixing granulator, add a binder to granulate, and the wet granules are sized and dried to make tablet-table granules, and magnesium stearate is added. Use a circle with a diameter of 4 mm to punch into microtablets of 53 ± 5 mg.

[0021] Hydroxypropyl Cellulose 30g water 260g Venlafaxine Hydrochloride 425g microcrystalline cellulose 500g Magnesium stearate 10g

Embodiment 2

[0023] According to the prescription ratio in the table below, take ethyl cellulose and add ethanol to dissolve; take triethyl citrate and add it to water to disperse, add it to the ethyl cellulose solution, add talcum powder to disperse evenly, and use it as a coating solution.

[0024] Get the microtablet of Example 1 and put it into the coating of a microporous high-efficiency coating machine, spray into the coating solution to make sustained-release microtablets.

[0025] Embodiment 1 microchip 965g Ethyl cellulose 100g ethanol 1500g triethyl citrate 12g talcum powder 20g water 75g

Embodiment 3

[0027] Add ethyl cellulose and Eudragit S100 into ethanol according to the prescription in the table below, stir and dissolve, add triethyl citrate, talcum powder and water to disperse evenly, and make a slow-release coating solution; take the prescription according to Example 1 The microtablets made by the preparation process are put into a microporous high-efficiency coating machine, and sprayed into the coating solution to make sustained-release microtablets.

[0028]

[0029]

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Abstract

The invention relates to a sustained-release microtablet capsule of 5-hydroxytryptamine, norepinephrine and a dopamine reuptake inhibitor and a preparation method of sustained-release microtablet capsule. According to the invention, 5-hydroxytryptamine, norepinephrine and the dopamine reuptake inhibitor are prepared into sustained-release micro-tablets, and then the capsules are filled with the sustained-release micro-tablets, such that the micro-tablet sustained-release capsules are prepared.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of a reuptake inhibitor of 5-hydroxytryptamine, norepinephrine and dopamine for the treatment of severe depression and a sustained-release microtablet capsule preparation, including sustained-release venlafaxine hydrochloride Microtablet capsules and desvenlafaxine succinate extended-release microtablet capsules. Background technique [0002] Both venlafaxine and desvenlafaxine are reuptake inhibitors of 5-hydroxytryptamine, norepinephrine and dopamine, and are clinically used for the treatment of severe depression and anxiety. The commonly used clinical dosage forms include tablets, Sustained-release capsules and sustained-release tablets, etc. The patent publication number of Venlafaxine Hydrochloride Sustained-release Capsules is CN1278165A, which adopts the extrusion and spheronization process to prepare micropills containing venlafaxine hydrochloride, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/62A61K31/137A61P25/24A61K9/36
CPCA61K31/137A61K9/5084A61P25/24A61K9/5089A61K9/2886A61K9/2866
Inventor 蒋海松
Owner 蒋海松
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