Venlafaxine hydrochloride controlled-release pellet and preparation method thereof

A technology of venlafaxine hydrochloride and sustained-release pellets, applied in the field of medicine, can solve the problems of large side effects, short half-life, and patients need frequent administration, and achieves small influence of individual differences, stable blood drug concentration, and reduced gastrointestinal effect of side effects

Active Publication Date: 2013-02-20
QINGDAO HUANGHAI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Venlafaxine hydrochloride is a new type of antidepressant, which has the remarkable characteristics of quick effect, good tolerance, and good short-term and long-term therapeutic effects. However, venlafaxine in common preparations has a short half-life (about 5±2 hours) ), patients need frequent administration (2-3 times / day), and the side effects are relatively large

Method used

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  • Venlafaxine hydrochloride controlled-release pellet and preparation method thereof
  • Venlafaxine hydrochloride controlled-release pellet and preparation method thereof
  • Venlafaxine hydrochloride controlled-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The venlafaxine hydrochloride sustained-release pellets provided by the present invention are composed of three parts: a blank pellet core, a venlafaxine hydrochloride drug-containing layer evenly covering the surface of the blank pellet core, and a sustained-release pellet uniformly covering the surface of the drug-containing layer. membrane.

[0027] 1. Choice of blank pill heart

[0028] Blank cores can be selected from pharmaceutically acceptable cores such as sucrose pellets, microcrystalline cellulose pellets, starch pellets, and lactose pellets. Qualified samples can be prepared when the particle size distribution is between 500-1000 μm. The present invention has passed a large number of experiments. It is found that when the core of blank pellets is sucrose pellets, the particle size of 710-850μm is the optimal choice. Through the RSD comparison test of the release degree, it is proved that the particle size of 710-850μm is the best.

[0029] Table 1: Influenc...

Embodiment 2

[0038] The preparation process of the pills described in this example is as follows: 3.1 kg of blank ball cores with a particle size distribution of 710-850 μm are added to the fluidized bed, and 1.9 kg of venlafaxine hydrochloride and 190 g of talcum powder are suspended in 3.8 kg75 % ethanol solution, the suspension is evenly sprayed on the surface of the pellet core by the bottom spraying process. The main parameters of the drug in the fluidized bed are recorded as follows:

[0039] parameters

value

Inlet air temperature

55℃

material temperature

45℃

Liquid supply speed

50rpm

Fan frequency

25Hz

atomization pressure

0.14Mpa

[0040] An appropriate amount of talcum powder is added to the prescription, and 75% ethanol solution is used instead of distilled water as a solvent, which greatly reduces the viscosity of the solution, makes the drug application process continuous and fast, and the pellets have n...

Embodiment 3

[0045] The preparation of containing pill is the same as embodiment 2.

[0046] The preparation process of the slow-release pill described in the present embodiment is specifically as follows: 250g EC (45 centipoise), 12.5g polyacrylic resin III, 12.5g HPMC E5, 25g castor oil are dissolved in 6.25kg75% ethanol solution, and pass flow The coating solution was sprayed onto the surface of the 5 kg pill-containing pellets prepared in Example 1 by chemical bed bottom spraying process to prepare the sustained-release pellet preparation. The main parameters of fluidized bed coating are recorded as follows:

[0047] parameters

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Abstract

The invention provides a venlafaxine hydrochloride controlled-release pellet and a preparation method thereof. The venlafaxine hydrochloride controlled-release pellet comprises a blank pellet core, a venlafaxine hydrochloride-containing layer and a controlled-release film, wherein the venlafaxine hydrochloride-containing layer comprises active components including venlafaxine hydrochloride and talcum powder which are in a weight ratio of 12:1-8:1, and the weight ratio of the venlafaxine hydrochloride to the blank pellet core is 4:10-8:10. The venlafaxine hydrochloride controlled-release pellet is prepared by adopting a fluidized bed bottom-spraying venlafaxine hydrochloride applying mode; by using 75 percent alcohol as a solvent, the viscosity of the venlafaxine hydrochloride in a water solution is remarkably lowered, the venlafaxine hydrochloride applying speed is increased; and the prepared venlafaxine hydrochloride containing pellet adopts a bottom-spraying coating process, thus the problem of static electricity generated because of the adoption of the pure organic solvent is overcome; the application process and the wrapping process can be continuously operated in the same device, thus the production efficiency is increased and the production cost is lowered; and no toxic organic solvent is adopted in the whole process, thus the venlafaxine hydrochloride controlled-release pellet is environmental-friendly and is good in stability, and almost no broken pellets or dust is produced.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a venlafaxine hydrochloride sustained-release pellet preparation and a preparation method thereof. Background technique [0002] Depression is a common mood disorder, which can be caused by various reasons. The main clinical feature is marked and persistent low mood, and the low mood is not commensurate with the situation. In severe cases, suicidal thoughts and behaviors may appear. Most cases have a tendency to relapse, and most of each attack can be relieved, and some may have residual symptoms or become chronic. [0003] 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 meta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/137A61K47/02A61K47/32A61K47/34A61K47/38A61P25/24A61K47/10
Inventor 张兴跃刘少梅尤恒刘晓华胡杰
Owner QINGDAO HUANGHAI PHARM CO LTD
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