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Desmethylvenlafaxine sustained-release pellet and preparation method thereof

A technology of sustained-release pellets and venlafaxine, which can be applied to pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., and can solve the problems that there are no sustained-release pellets

Inactive Publication Date: 2012-05-02
COSCI MED TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no sustained-release pellets and other products on the market

Method used

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  • Desmethylvenlafaxine sustained-release pellet and preparation method thereof
  • Desmethylvenlafaxine sustained-release pellet and preparation method thereof
  • Desmethylvenlafaxine sustained-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 desvenlafaxine sustained-release pellets and tablets (1000 preparation units)

[0029] The prescription of preparation and preparation method thereof are:

[0030] prescription

[0031] Pellets:

[0032]

[0033] Tablets:

[0034] Eudragit L100 24g

[0035] Microcrystalline Cellulose 12g

[0036] Magnesium Stearate 2g

[0037] Preparation:

[0038] Get the desvenlafaxine raw material and pass through an 80-mesh sieve for subsequent use. Take povidone and add 80% alcohol to dissolve, and use it as a binder for later use; ethyl cellulose, triethyl citrate, polyethylene glycol, add ethanol or acetone and dissolve it, and use it as a slow-release coating solution for later use;

[0039] Take blank pellet cores, put them in a coating pan or a centrifugal coating granulator, spray povidone ethanol solution as a binder, add desvenlafaxine powder, and make pellets. Spray into the sustained-release coating solution, wrap the pellets with a sustained-rele...

Embodiment 2

[0043] Embodiment 2 Desvenlafaxine sustained-release pellets and tablets (1000 preparation units)

[0044] prescription

[0045] Pellets:

[0046]

[0047] Tablets:

[0048]

[0049] Preparation:

[0050] Get the desvenlafaxine raw material and pass through an 80-mesh sieve for subsequent use. Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; hydroxypropyl methylcellulose E50, triethyl citrate, polyethylene glycol and add ethanol or acetone to dissolve it, and use it as a slow-release coating solution for later use;

[0051] Get the blank ball core, put it in the coating pot or in the centrifugal coating granulator, spray into the povidone ethanol solution as the binding agent, add desvenlafaxine powder, and make micropills. Spray into the sustained-release coating solution, wrap the pellets with a sustained-release film, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[005...

Embodiment 3

[0055] Embodiment 3 desvenlafaxine sustained-release pellets and tablets (1000 preparation units)

[0056] prescription

[0057] Ball core:

[0058] Desvenlafaxine 20g

[0059] Sucrose powder 20g

[0060] Povidone 5g

[0061] Pellets:

[0062] Ball core

[0063]

[0064] Tablets:

[0065] Microcrystalline Cellulose 12g

[0066] Ethyl cellulose 10g

[0067] Magnesium Stearate 2g

[0068] Preparation:

[0069] Get the desvenlafaxine raw material and pass through an 80-mesh sieve for subsequent use. Get the main drug of the prescription amount of the ball core, and dissolve povidone with 80% ethanol, and use it as an adhesive for standby; mix the main drug and sucrose powder evenly and add the adhesive to prepare the ball core;

[0070] Dissolve hydroxypropyl methylcellulose E50, triethyl citrate, propylene glycol with ethanol or acetone, and use it as a slow-release coating solution for later use; take the core containing pills, put them in a coating pan or a centri...

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Abstract

The invention provides a desmethylvenlafaxine sustained-release pellet and a capsule or a tablet prepared from the obtained pellet. The pellet comprises a medicament-containing or blank pill core, a medicament layer and a sustained-release coating layer, wherein the sustained-release coating layer comprises a difficultly-water-soluble or water-insoluble polymer or an enteric polymer or a gastric-soluble polymer, and the pellet prepared by using a hydrophilic plasticizing agent is round and has high medicament release curve repeatability. The invention further discloses a method for preparing the pellet.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to sustained-release pellets for changing the drug release behavior of desvenlafaxine and a preparation method thereof. Background technique [0002] Pellets refer to all kinds of pills with a diameter of less than 2.5mm, which can be made into quick-release or sustained-release pellets according to different needs. The focus of current research is on sustained-release pellets, which are made by mixing drugs and blockers or making ordinary ball cores and then wrapping controlled-release membranes. The pellets can be compressed into tablets, and the pellets can also be packed in capsules to make capsules. Now many companies at home and abroad all produce this preparation, such as Contac (Contac) sustained-release capsules produced by Sino-US SmithKline, aspirin sustained-release capsules produced by the Pharmaceutical Factory of China Pharmaceutical University, and importe...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/22A61K31/137A61P25/24
Inventor 蒋海松王锦刚
Owner COSCI MED TECH CO LTD