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High-drug-loading venlafaxine hydrochloride sustain release pellet composition, sustained-release capsule and preparation method thereof

A technology of venlafaxine hydrochloride and sustained-release pellets, which is applied in the field of medicine and can solve the problems of too fast release of venlafaxine hydrochloride

Active Publication Date: 2019-01-15
HUNAN DONGTING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing method adopts aqueous dispersion to carry out coating, because the high water solubility of venlafaxine hydrochloride causes venlafaxine hydrochloride to migrate when coating, under the situation that coating film thickness is not enough, venlafaxine hydrochloride Sine may act as a pore-reaching agent, causing too rapid release of venlafaxine hydrochloride

Method used

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  • High-drug-loading venlafaxine hydrochloride sustain release pellet composition, sustained-release capsule and preparation method thereof
  • High-drug-loading venlafaxine hydrochloride sustain release pellet composition, sustained-release capsule and preparation method thereof
  • High-drug-loading venlafaxine hydrochloride sustain release pellet composition, sustained-release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0241] Embodiment 1: Preparation of venlafaxine hydrochloride sustained-release pellets and sustained-release capsules

[0242] formula:

[0243]

[0244]

[0245] Preparation method:

[0246] (1) Provide a blank ball core, put it in a fluidized bed coating machine (at a temperature of 42-45 degrees Celsius) to make it in a fluidized state;

[0247] (2) Wrap the drug-loaded coating layer: dissolve the adhesive in the first solvent, add venlafaxine hydrochloride that is crushed to pass through a 150 mesh sieve in advance, mix uniformly to obtain a suspension, and spray The suspension is sprayed on the blank ball core in a fluidized state in the fluidized bed coating machine, and after the spraying is completed, the fluidization is continued until the solvent is removed to obtain drug-loaded pellets; [after testing, the residual amount of the first solvent is less than 500ppm , far below the general requirement limit in this field]

[0248] (3) Wrapping the slow-relea...

Embodiment 2

[0251] Embodiment 2: Preparation of venlafaxine hydrochloride sustained-release pellets and sustained-release capsules

[0252] formula:

[0253]

[0254]

[0255] Preparation method:

[0256] (1) Provide a blank ball core, put it in a fluidized bed coating machine (at a temperature of 42-45 degrees Celsius) to make it in a fluidized state;

[0257] (2) Wrap the drug-loaded coating layer: dissolve the adhesive in the first solvent, add venlafaxine hydrochloride that is crushed to pass through a 150 mesh sieve in advance, mix uniformly to obtain a suspension, and spray The suspension is sprayed on the blank ball core in a fluidized state in the fluidized bed coating machine, and after the spraying is completed, the fluidization is continued until the solvent is removed to obtain drug-loaded pellets; [after testing, the residual amount of the first solvent is less than 500ppm , far below the general requirement limit in this field]

[0258] (3) Wrapping the slow-relea...

Embodiment 3

[0261] Embodiment 3: Preparation of venlafaxine hydrochloride sustained-release pellets and sustained-release capsules

[0262] formula:

[0263]

[0264]

[0265] Preparation method:

[0266] (1) Provide a blank ball core, put it in a fluidized bed coating machine (at a temperature of 42-45 degrees Celsius) to make it in a fluidized state;

[0267] (2) Wrap the drug-loaded coating layer: dissolve the adhesive in the first solvent, add venlafaxine hydrochloride that is crushed to pass through a 150 mesh sieve in advance, mix uniformly to obtain a suspension, and spray The suspension is sprayed on the blank ball core in a fluidized state in the fluidized bed coating machine, and after the spraying is completed, the fluidization is continued until the solvent is removed to obtain drug-loaded pellets; [after testing, the residual amount of the first solvent is less than 500ppm , far below the general requirement limit in this field]

[0268] (3) Wrapping the slow-relea...

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Abstract

The invention relates to a high-drug-loadingvenlafaxine hydrochloride sustained-release pellet composition, a sustained-release capsule and a preparation method. Specifically, the venlafaxine hydrochloride sustained-release pellets comprise a blank pellet core, a drug-carrying coating layer coated on the outer surface of the blank pellet core, and a sustained-release coating layer coated on the outer surface of the drug-carrying coating layer, wherein the drug-carrying coating layer comprises venlafaxine hydrochloride as an active ingredient. 50 to 65 percent of venlafaxine hydrochloride active ingredient in that venlafaxine hydrochloride sustain release pellets, wherein the venlafaxine hydrochloride sustain release pellets can pass through a 14-mesh sieve but cannot pass through a 30-meshsieve, and the venlafaxine hydrochloride active ingredient in the venlafaxine hydrochloride sustain release pellets accounts for 50 to 65 percent of the weight of the sustained release pellets; Whichcan pass through a 16-mesh sieve but not a 25-mesh sieve; according to the dissolution determination method, the dissolution amount is not more than 30% in 2 hours, 40%-60% in 4 hours, 60%-80% in 8 hours, 70%-90% in 12 hours, and 85% in 24 hours. The venlafaxine hydrochloride sustained-release pellets and the sustained-release capsules of the invention exhibit excellent pharmaceutical properties.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an oral venlafaxine pharmaceutical composition for treating depression, generalized anxiety disorder, recurrence prevention of depressive episodes, social anxiety disorder, panic disorder, etc., especially venlafaxine Sustained release capsule compositions, and methods for their preparation. Background technique [0002] Venlafaxine (venlafaxine), often used as its hydrochloride, the molecular formula of venlafaxine hydrochloride: C 17 h 27 NO 2 HCl, molecular weight: 313.86, CAS registration number: 99300-78-4, chemical name: (±)-1-[α-[(dimethylamino)methyl]-p-methoxybenzyl] ring Hexanol hydrochloride, [0003] [0004] Sustained-release capsules are serotonin and noradrenaline reuptake inhibitor (SNRI) antidepressants. Animal experiments have found that the drug has antidepressant effects, and has no obvious affinity for muscarinic or histamine-like receptors. Therefore...

Claims

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Application Information

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IPC IPC(8): A61K9/58A61K47/34A61K47/38A61K31/137A61P25/22A61P25/24A61P25/18G01N30/02
CPCA61P25/18A61P25/22A61P25/24G01N30/02A61K9/5031A61K9/5042A61K9/5078A61K31/137
Inventor 侯奇伟李晓云后旻旸
Owner HUNAN DONGTING PHARMA
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