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Venlafaxine hydrochloride spansule and preparation method thereof

A technology of venlafaxine hydrochloride and sustained-release capsules, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of increasing coating thickness and high cost, and achieve cost reduction. Low cost, stable quality, and easy industrial production

Inactive Publication Date: 2013-07-10
浙江美华鼎昌医药科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned patents all use water dispersion for coating. Due to the high water solubility of venlafaxine hydrochloride, venlafaxine hydrochloride migrates during coating. When the thickness of the coating film is not enough, venlafaxine hydrochloride Dioxin may act as a pore-reaching agent, resulting in too rapid release of venlafaxine hydrochloride, and increasing the coating thickness would result in prohibitive cost

Method used

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  • Venlafaxine hydrochloride spansule and preparation method thereof
  • Venlafaxine hydrochloride spansule and preparation method thereof
  • Venlafaxine hydrochloride spansule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prescription with pill core:

[0030]

[0031] The preparation method is as follows:

[0032] Mix microcrystalline cellulose, hydroxypropyl methylcellulose and venlafaxine hydrochloride evenly. Use a soft material made of 5% polyvinylpyrrolidone solution to extrude in an extruder (screen diameter 0.8mm, extrusion speed: 25rpm), and put the extruded material in a spheronizer for spheronization (rotation speed 600-1000rpm, spheronization time 500 seconds ). Dry the material in a blast drying oven at 40°C-60°C for 2-4 hours, sieve, and sieve out the pellet cores larger than 16 mesh and less than 30 mesh.

[0033] Coating prescription:

[0034]

[0035]

[0036] Preparation method of coating solution: add hydroxypropyl methylcellulose into water, add talcum powder under the action of a shearing machine, add this solution into Eudragit NE30D, and stir.

[0037] Coating operation: take 500g of pill cores containing the drug and coat them with a fluidized bed bott...

Embodiment 2

[0042] Prescription with pill core:

[0043]

[0044] Preparation method: Mix microcrystalline cellulose and venlafaxine hydrochloride evenly. 3% hydroxypropyl methylcellulose solution was used as binder, and pellets were prepared by centrifugal granulation. Dry the material in a blast drying oven at 40°C-60°C for 2-4 hours, sieve, and sieve out the pellet cores larger than 16 mesh and less than 30 mesh.

[0045] Coating prescription:

[0046]

[0047]

[0048] Coating operation: take 500 g of the 30-16 mesh-containing pill core prepared in Example 2, and coat the isolation layer and the controlled-release layer respectively by the method of bottom spraying to prepare sustained-release pellets. Coating weight gain (calculated by polymer weight) 30%, 40%.

[0049] Release degree inspection: According to the Chinese drug import registration standard X20000237, the release degree of the product was inspected, and compared with Efexor XR, a product of Wyeth Pharmaceuti...

Embodiment 3

[0053] Prescription with pill core:

[0054]

[0055] Preparation method: Mix microcrystalline cellulose and venlafaxine hydrochloride evenly. 3% hydroxypropyl methylcellulose solution was used as binder, and pellets were prepared by centrifugal granulation. Dry the material in a blast drying oven at 40°C-60°C for 2-4 hours, sieve, and sieve out the pellet cores larger than 16 mesh and less than 30 mesh.

[0056] Coating prescription:

[0057]

[0058] Coating operation: take 500 g of the 30-16 mesh pellet cores prepared in Example 3, and coat the isolation layer and the release-controlling layer respectively with the method of bottom spraying to prepare sustained-release pellets. Coating weight gain (calculated by polymer weight) 30%, 40%.

[0059] Release degree inspection: According to the Chinese drug import registration standard X20000237, the release degree of the product was inspected, and compared with Efexor XR, a product of Wyeth Pharmaceutical Co., Ltd.

...

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Abstract

The invention discloses a venlafaxine hydrochloride spansule and a preparation method thereof. According to the existing method, aqueous dispersion is used for coating, and venlafaxine hydrochloride generates migration during the coating process due to high water solubility of venlafaxine hydrochloride, so that venlafaxine hydrochloride is possible to become a pore-forming agent to result in overquick release of venlafaxine hydrochloride if the thickness of a coating film is insufficient. The venlafaxine hydrochloride spansule disclosed by the invention is characterized in that the medicated micro-pill comprises a medicated pill core, an isolating layer coating the medicated pill core and a release control layer coating the isolating layer, wherein the medicated pill core is prepared from the following ingredients in percentage by weight: 30-60% of venlafaxine hydrochloride, 30-80% of filler, 1-20% of release skeleton material and 1-10% of adhesive. According to the invention, such technical problems as potential safety hazard to operators and high demands on equipment caused by utilizing organic solvents, namely dichloromethane and ethanol, for coating are completely solved.

Description

technical field [0001] The invention relates to the field of sustained-release capsules, in particular to a venlafaxine hydrochloride sustained-release capsule and a preparation method thereof. Background technique [0002] Venlafaxine hydrochloride, its chemical name is: (±)-1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]-cyclohexanol hydrochloride, is a It is a new type of antidepressant, which is the first clinical application of both 5-hydroxytryptamine (5-HT) and norepinephrine (NE) reuptake inhibitory drugs, but with adrenaline al, a2, β receptors, M choline receptors and histamine H1 receptors have little affinity. Due to its special pharmacological effects, venlafaxine hydrochloride has been widely used in clinical psychiatry for the treatment of various types of depression, including depression accompanied by anxiety. First-line treatment drugs. [0003] Chinese patent CN97109594.9 discloses a preparation method of venlafaxine hydrochloride sustained-release capsu...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/137A61K47/38A61P25/24
Inventor 王传跃何书麟李黄强刘真君
Owner 浙江美华鼎昌医药科技有限公司
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