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A kind of venlafaxine hydrochloride sustained-release capsule composition

A technology of venlafaxine hydrochloride and sustained-release capsules, applied in the field of medicine, can solve problems such as adhesion and excessive softening of macromolecular polymers, and achieve the effect of reducing side effects and avoiding adhesion

Active Publication Date: 2019-12-13
HAINAN HERUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the plasticizer can reduce the adhesion between pellets, if the dosage is not well controlled, it will cause excessive softening of the polymer and also cause adhesion

Method used

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  • A kind of venlafaxine hydrochloride sustained-release capsule composition
  • A kind of venlafaxine hydrochloride sustained-release capsule composition
  • A kind of venlafaxine hydrochloride sustained-release capsule composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] According to above-mentioned screening result, decide to adopt the prescription (specification: 75mg) as shown below to carry out the preparation of sustained-release capsule composition:

[0085]

[0086] The preparation method is as follows:

[0087] (1) Take by weighing 6660g of ethanol, place in a clean container, add 1273g of venlafaxine hydrochloride, stir to make the dissolution even, then slowly add 225g of hypromellose, vigorously stir to make the dispersion uniform, cross a 100 mesh sieve, and obtain Drug-loaded layer liquid;

[0088] (2) Put 1650g of microcrystalline cellulose pellet cores in a fluidized bed, set the air inlet temperature to 39°C, set the frequency, and after drying for 30 minutes, set a certain atomization pressure and needle pressure, and adjust The height of the guide tube is to make the core of the microcrystalline cellulose pellets fluidized evenly. After controlling the temperature of the material at 33-37°C, the drug-loaded layer l...

Embodiment 2

[0093] According to above-mentioned screening result, decide to adopt the prescription (specification: 150mg) as shown below to carry out the preparation of sustained-release capsule composition:

[0094]

[0095]

[0096] The preparation method is as follows:

[0097] (1) Take by weighing 6660g of ethanol, place in a clean container, add 1273g of venlafaxine hydrochloride, stir to make the dissolution even, then slowly add 225g of hypromellose, vigorously stir to make the dispersion uniform, cross a 100 mesh sieve, and obtain Drug-loaded layer liquid;

[0098] (2) Put 1650g of microcrystalline cellulose pellet cores in a fluidized bed, set the air inlet temperature to 39°C, set the frequency, and after drying for 30 minutes, set a certain atomization pressure and needle pressure, and adjust The height of the guide tube is to make the core of the microcrystalline cellulose pellets fluidized evenly. After controlling the temperature of the material to 33-37°C, start to spr...

Embodiment 3

[0103] According to above-mentioned screening result, decide to adopt the prescription (specification: 75mg) as shown below to carry out the preparation of sustained-release capsule composition:

[0104]

[0105] The preparation method is as follows:

[0106] (1) Take by weighing 9300g of ethanol, place in a clean container, add 1867g of venlafaxine hydrochloride, stir to make the dissolution even, then slowly add 320g hypromellose, vigorously stir to make the dispersion uniform, cross a 100 mesh sieve, and obtain Drug-loaded layer liquid;

[0107] (2) Put 2337g of microcrystalline cellulose pellet cores in a fluidized bed, set the air inlet temperature to 39°C, set the frequency, and after drying for 30 minutes, set a certain atomization pressure and needle pressure, and adjust The height of the guide tube is to make the core of the microcrystalline cellulose pellets fluidized evenly. After controlling the temperature of the material to 33-37°C, start to spray the core of...

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PUM

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Abstract

The invention relates to the field of medicines and in particular to a venlafaxine hydrochloride sustained-release capsule composition. The content of the venlafaxine hydrochloride sustained-release capsule composition comprises a sustained-release micropill composed of a medicine carrying micropill and a sustained-release layer; the medicine carrying micropill is composed of 58-66 parts by weight of venlafaxine hydrochloride, 75-85 parts by weight of filler and 8-12 parts by weight of an adhesive; the sustained-release layer is composed of 3.5-6 parts by weight of a sustained-release coating material and 18-27 parts by weight of a pore-foaming agent; the mass of the sustained-release layer is 14-17% of that of the medicine carrying layer. The invention also provides a preparation method of the venlafaxine hydrochloride sustained-release capsule composition. The medicine carrying micropill is manufactured by using a fluidized bed and the micropill is coated by the sustained-release layer to obtain the sustained-release micropill. The venlafaxine hydrochloride sustained-release capsule composition prepared by the method does not contain auxiliary materials such as an antisticking agent and a plasticizer. The manufacturing condition can be met by adjusting the process of the fluidized bed to obtain a drug which is close to an original drug in effect; the cost is lowered and the process difficulty is reduced.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a sustained-release capsule composition of venlafaxine hydrochloride. Background technique [0002] Venlafaxine is a brand new antidepressant. The chemical name is (R / S)-1-[2-(dimethylamine)-1-(4-methoxyphenyl)ethyl]cyclohexanol, and the antidepressant mechanism of venlafaxine on the human body is to enhance the central nervous system Its neurotransmitter activity in the nervous system. Preclinical studies have shown that venlafaxine and its major metabolite O-desmethylvenlafaxine (ODV) are potent inhibitors of serotonin and norepinephrine reuptake. Venlafaxine also slightly inhibits dopamine uptake. Animal studies have shown reduced beta-adrenergic responsiveness only after chronic administration of tricyclic antidepressants. However, both venlafaxine and O-desmethylvenlafaxine decreased beta-adrenergic reactivity after single or chronic doses of venlafaxine. Venlafaxine and O-desme...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K47/38A61K31/137A61P25/24
CPCA61K9/0002A61K9/4866A61K9/5042A61K31/137
Inventor 钟正明
Owner HAINAN HERUI PHARMA
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