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Paroxetine hydrochloride tablet and preparation method thereof

The technology of paroxetine hydrochloride tablets and paroxetine hydrochloride is applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., and can solve the problems of being unsuitable for mass production, cumbersome technological process, and high risk of sticking and flushing, Achieve the effect of reducing the risk of uneven content and sticking, simple process flow, and reducing the risk of sticking

Pending Publication Date: 2021-04-13
江苏睿实生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] (1) The wet granulation and tabletting process, although it can ensure that the raw materials are mixed evenly, but the solvent is introduced in the preparation process and drying and heating are required, the process is relatively cumbersome, and there are many types of excipients involved
[0007] (2) The mixed powder direct compression process, although there are fewer types of excipients involved and the preparation process is simple, but due to the small proportion of raw materials, the risk of uneven content is high
This process has a high risk of sticking during tablet compression and is not suitable for mass production

Method used

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  • Paroxetine hydrochloride tablet and preparation method thereof
  • Paroxetine hydrochloride tablet and preparation method thereof
  • Paroxetine hydrochloride tablet and preparation method thereof

Examples

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preparation example Construction

[0037] The present invention also provides a preparation method for preparing the paroxetine hydrochloride tablet, which adopts the preparation method of powder mixing and direct tablet compression, and the preparation method comprises the following steps:

[0038] Weighing of S1 raw materials, successively weighing paroxetine hydrochloride, filler, disintegrant, lubricant and coating powder for later use;

[0039] S2 mixing, put paroxetine hydrochloride, filler, and disintegrating agent into the mixing granulator in sequence and mix evenly. The mixing speed is 1000-2000 rpm, the stirring speed is 50-200 rpm, and the mixing time is 5-15 minutes;

[0040] S3 lubrication, add lubricant, continue to mix evenly, the stirring speed of mixing is 5-20rpm, and the mixing time is 2-15min;

[0041] S4 tablet molding, the uniformly mixed powder is directly compressed into a tablet to obtain a tablet core;

[0042] S5 Coating and shaping, the tablet core is coated with coating powder and...

Embodiment 1

[0045] Prepare paroxetine hydrochloride tablet, every 1000 comprises the component (unit is g) of following weight:

[0046] 22.8g of paroxetine hydrochloride with a D90 particle size of 9μm≤D90≤15μm, 318.0g of calcium hydrogen phosphate (D90≤200μm), 6.0g of sodium carboxymethyl starch, 3.2g of magnesium stearate, and 7g of coating powder;

[0047] The paroxetine hydrochloride tablet adopts the powder mixing direct compression preparation method, and the preparation method comprises the following steps:

[0048] Weigh the raw materials of S1, and successively weigh paroxetine hydrochloride, calcium hydrogen phosphate, sodium carboxymethyl starch, magnesium stearate and coating powder for later use;

[0049] S2 Mixing, put paroxetine hydrochloride, calcium hydrogen phosphate, sodium carboxymethyl starch into the mixing granulator in turn and mix evenly, the mixing speed of chopping is 1000rpm, the stirring speed is 50rpm, and the mixing time is 15min;

[0050] S3 lubrication, ad...

Embodiment 2

[0054] Prepare paroxetine hydrochloride tablet, every 1000 comprises the component (unit is g) of following weight:

[0055] 22.8g of paroxetine hydrochloride with a D90 particle size of 33μm≤D90≤40μm, 318.0g of calcium hydrogen phosphate (D90≤200μm), 6.0g of sodium carboxymethyl starch, 3.2g of magnesium stearate, and 7g of coating powder;

[0056] The paroxetine hydrochloride tablet adopts the powder mixing direct compression preparation method, and the preparation method comprises the following steps:

[0057] The chopping speed of S2 mixing is 1500rpm, the stirring speed is 100rpm, and the mixing time is 8min;

[0058] The stirring speed of S3 mixing is 10rpm, and the mixing time is 8min;

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Abstract

The invention provides a paroxetine hydrochloride tablet. The paroxetine hydrochloride tablet is prepared from the following components in parts by weight: 6-7 parts of paroxetine hydrochloride, 85-92 parts of filler, 0.5-2 parts of a disintegrating agent, 0.2-1.5 parts of a lubricating agent and 1-4 parts of coating powder. On the basis of an existing mixed powder direct tabletting process, the paroxetine hydrochloride tablet is obtained through the steps of raw material weighing, mixing, lubricating, tabletting forming and coating shaping. The particle size of the active pharmaceutical ingredients is controlled within a small range, so that the active pharmaceutical ingredients can be quickly dissolved out. Meanwhile, calcium hydrophosphate accounts for a large proportion, and the particle size distribution of the calcium hydrophosphate is controlled within a proper range, so that the calcium hydrophosphate and the active pharmaceutical ingredients cannot be layered, and the risk of non-uniform content is reduced. The fluidity of the materials can be guaranteed, and the risk of sticking in the long-time tabletting process is reduced.

Description

technical field [0001] The invention relates to the technical field of medicine preparation for treating depression, in particular to a paroxetine hydrochloride tablet and a preparation method of the tablet. Background technique [0002] Paroxetine hydrochloride tablets are a drug for the treatment of depression listed in the 1990s. Paroxetine hydrochloride is a potent and highly selective 5-hydroxytryptamine (5-HT) reuptake inhibitor class (SSRI) antidepressant. It can increase the concentration of 5-HT in the synaptic gap and enhance the nerve function of central 5-HT. It is currently the most widely used antidepressant in clinical practice. It is used for the treatment of various mental diseases and has brought good results to patients. Widely used worldwide. There are two adjacent chiral centers on the piperidine ring of the drug. Paroxetine hydrochloride contains aromatic ether and secondary ammonia structure. The chemical name of paroxetine hydrochloride is: (3S,4R)-4...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K47/02A61K47/38A61K47/36A61K31/4525A61P25/24
CPCA61K9/2866A61K9/2853A61K9/2095A61K9/2059A61K9/2054A61K31/4525A61P25/24
Inventor 殷建光高慧丽梁志寿殷昌青
Owner 江苏睿实生物科技有限公司
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