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Venlafaxine hydrochloride film-controlled slow-release pellet capsule

A technology of venlafaxine hydrochloride and sustained-release pellets, which can be used in medical preparations with non-active ingredients, organic active ingredients, nervous system diseases, etc., and can solve problems such as decreased release

Active Publication Date: 2013-07-24
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problem of release decline caused by film aging of venlafaxine hydrochloride film-controlled sustained-release pellets prepared by water dispersion coating, the present invention provides a film capable of maintaining stable release performance throughout the validity period Controlled venlafaxine hydrochloride sustained-release pellet capsules are characterized in that the core of the pellets contains low-substituted hydroxypropyl cellulose with high water-swellability, and the sustained-release coating film is deformed by water-absorbing swelling, thereby Counteracts membrane aging

Method used

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  • Venlafaxine hydrochloride film-controlled slow-release pellet capsule
  • Venlafaxine hydrochloride film-controlled slow-release pellet capsule
  • Venlafaxine hydrochloride film-controlled slow-release pellet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The venlafaxine hydrochloride sustained-release pellet capsule of embodiment 1 common ball core

[0030] 1. Prescription

[0031] 1. Pill core prescription (1000 capsules)

[0032]

[0033] *75g based on venlafaxine.

[0034] 2. Prescription of sustained-release film coating solution

[0035]

[0036] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0037] Second, the preparation process:

[0038] 1. Ball core preparation process:

[0039] (1) Venlafaxine hydrochloride is crossed 60 mesh sieves;

[0040] (2) take by weighing venlafaxine hydrochloride, microcrystalline cellulose PH101 of recipe quantity, put in the wet granulator and mix homogeneously;

[0041] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft material;

[0042] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0043] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

...

Embodiment 2

[0068] Embodiment 2 Venlafaxine hydrochloride sustained-release pellet capsule containing 10% low-substituted hydroxypropyl cellulose

[0069] 1. Prescription

[0070] 1. Pill core prescription (1000 capsules)

[0071]

[0072] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0073] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0074] Second, the preparation process:

[0075] 1. Ball core preparation process:

[0076] (1) Venlafaxine hydrochloride is crossed 60 mesh sieves;

[0077] (2) Venlafaxine hydrochloride, microcrystalline cellulose PH101, and low-substituted hydroxypropyl cellulose are taken by weighing prescription quantities, and are mixed uniformly in a wet granulator;

[0078] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft materials;

[0079] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0080] (5) spheronization, the spheronizati...

Embodiment 3

[0099] Example 3 Venlafaxine Hydrochloride Sustained-release Pellet Capsules Containing 20% ​​Low-substituted Hypromellose

[0100] 1. Prescription

[0101] 1. Pill core prescription (1000 capsules)

[0102]

[0103] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0104] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0105] Second, the preparation process:

[0106] 1. Ball core preparation process: the same as in Example 2

[0107] 2. Preparation process of sustained-release film coating solution:

[0108] Same as Example 1

[0109] 3. Coating (sustained release film):

[0110] The ball core is placed in a fluidized bed for coating, and the weight gain of the coating film is controlled, and the weight gain of the coating is 27.5% and 30.7%.

[0111] 4, heat treatment: with embodiment 1

[0112] 5. Fill capsules

[0113] It is obtained by filling the coated pellets into capsules.

[0114] 3. Release, content determ...

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Abstract

The invention relates to a venlafaxine hydrochloride film-controlled slow-release pellet capsule. A slow-release film of the venlafaxine hydrochloride film-controlled slow-release pellet utilizes Kollicoat SR30D as a film-formation material. A pellet core of the venlafaxine hydrochloride film-controlled slow-release pellet contains low-substituted hydroxyprepyl cellulose having high expansibility, and also contains a pharmaceutically-acceptable common excipient for the slow-release pellet, wherein preferably, the excipient comprises microcrystalline cellulose, and the pellet core comprises 10 to 40wt% of low-substituted hydroxyprepyl cellulose. The slow-release film comprises Kollicoat SR30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Kollicoat SR30D to triethyl citrate to talcum powder is 30: 1: 4 and a film weight increasing ratio is in a range of 21 to 39%. The venlafaxine hydrochloride film-controlled slow-release pellet comprises the pellet core containing low-substituted hydroxyprepyl cellulose having high water expansibility and thus after absorbing water, the venlafaxine hydrochloride film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the venlafaxine hydrochloride film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.

Description

technical field [0001] The invention relates to a film-controlled sustained-release pellet capsule of venlafaxine hydrochloride, specifically, a film-controlled sustained-release pellet capsule of venlafaxine hydrochloride containing low-substituted hydroxypropyl cellulose in the pellet core, which belongs to medicine formulation field. Background technique [0002] Venlafaxine hydrochloride is an antidepressant that can significantly inhibit the reuptake of serotonin and norepinephrine at synaptic sites. It is used to treat various types of depression, including depression with anxiety and generalized anxiety. The basic clinical requirement for this type of drug is that it can control symptoms for a long time. [0003] The solubility of venlafaxine hydrochloride in water is very good. The earliest common preparations on the market need to be taken 2-3 times a day, and the blood drug concentration fluctuates greatly, the peak concentration is too high, and the adverse reac...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/137A61K47/32A61K47/38A61P25/22A61P25/24
Inventor 姜庆伟狄媛吕玉珠葛振中李帅唐亚坤刘俊轶
Owner 北京天衡药物研究院有限公司
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