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Stable X-crystal-shaped agomelatine tablet and preparation method thereof

A stable technology of agomelatine tablets, applied in the field of pharmaceutical preparations, can solve the problems of inconsistent drug bioavailability, accelerated agomelatine crystal form transformation, infringement, etc.

Active Publication Date: 2014-03-26
天津泰普制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] (2) Narrow selection of excipients: commonly used excipients such as microcrystalline cellulose and pregelatinized starch are not available, mainly because the above excipients can accelerate the transformation of agomelatine crystal form;
[0016] The change of crystal form may cause infringement on the one hand, and may further lead to inconsistencies in the bioavailability of drugs on the other hand

Method used

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  • Stable X-crystal-shaped agomelatine tablet and preparation method thereof
  • Stable X-crystal-shaped agomelatine tablet and preparation method thereof
  • Stable X-crystal-shaped agomelatine tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] Agomelatine (Form X 99%) 25g

[0141] water 20ml

[0142] Lactose 102g

[0143] Hypromellose 3g

[0144] Polyvinylpyrrolidone k30 3g

[0145] Cross-linked polyvinylpyrrolidone 13g

[0146] Magnesium Stearate 1.3g

[0147] Stearic acid 2.6g

[0148] Silica 0.3g

[0149] Process: Sift crystalline form X agomelatine according to the above weight for later use; take hydroxypropyl methylcellulose and polyvinylpyrrolidone k30 and stir in water to dissolve, let cool to room temperature, add crystalline form X agomelatine and stir homogeneous; the protective agent containing crystalline X-type agomelatine was obtained for later use; the protective agent containing crystalline X-type agomelatine was added to the mixed granulation containing lactose and part (1 / 2) cross-linked polyvinylpyrrolidone In the machine, after 2 minutes of wet granulation, granulate through a swing granulator (screen 833μm); get wet granules; dry in a fluidized bed (inlet air temperature 45°C, boi...

Embodiment 2

[0151] Agomelatine (more than 90% crystal X) 25g

[0152] water 30ml

[0153] Lactose 102g

[0154] Hydroxypropyl Cellulose 4.5g

[0155] Polyvinylpyrrolidone k30 4.5g

[0156] Croscarmellose Sodium 13g

[0157] Magnesium Stearate 1.3g

[0158] Stearic acid 2.6g

[0159] Silica 0.3g

[0160] Process: Sieve agomelatine crystal X according to the above weight for later use; take hydroxypropyl cellulose and polyvinylpyrrolidone k30 and stir in water to dissolve, let cool to room temperature, add agomelatine crystal X and stir well ; Obtain the protective agent containing crystal X-type agomelatine for later use; add the protective agent containing crystal X-type agomelatine to the mixture containing lactose and part (1 / 2) croscarmellose sodium In the granulator, after 2 minutes of wet granulation, granulate through a swing granulator (screen 833μm); get wet granules; dry in a fluidized bed (inlet air temperature 45°C, boiling bed temperature 30°C), control the moisture con...

Embodiment 3

[0162] Agomelatine (more than 85% crystal X) 25g

[0163] water 30ml

[0164] Lactose 102g

[0165] Hypromellose 4 .5g

[0166] Hydroxypropyl Cellulose 4.5g

[0167] Croscarmellose Sodium 13g

[0168] Magnesium Stearate 1.3g

[0169] Stearic acid 2.6g

[0170] Silica 0.3g

[0171]Process: Sift crystalline form X agomelatine according to the above weight for later use; take hydroxypropyl methylcellulose and polyvinylpyrrolidone k30 and stir in water to dissolve, let cool to room temperature, add crystalline form X agomelatine and stir homogeneous; the protective agent containing crystalline X-type agomelatine was obtained for later use; In the mixing granulator, after wet granulation for 2 minutes, granulate through a swing granulator (screen size 833 μm); wet granules are obtained; dry in a fluidized bed (inlet air temperature 45°C, boiling bed temperature 30°C), control the moisture content of about 2%; whole grain; calculate the yield, add other remaining excipients,...

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Abstract

The invention discloses a stable X-crystal-shaped agomelatine tablet and a preparation method thereof. The tablet is prepared by the following steps: selecting one or more protective agents, adding the protective agents in pure water, stirring, heating the mixture to 35-40 DEG C, dissolving until the solution is clear, cooling the solution to room temperature, adding X-crystal-shaped agomelatine, stirring the mixture uniformly, obtaining the protective agent containing the X-crystal shaped agomelatine, and keeping for standby use; mixing a part of pharmaceutic adjuvant uniformly, adding the protective agent containing the X-crystal-shaped agomelatine, mixing and pelletizing according to a wet method and drying to obtain particles containing the X-crystal-shaped agomelatine; at last, adding the other pharmaceutic adjuvants in the particles according to a proportion, mixing uniformly and tabletting. The preparation method can fully ensure that the crystal form of the X-crystal-shaped in the tablet preparation process is not changed; the stability between the X-crystal-shaped and the related substance is good to completely meet demand of large-scale production.

Description

[0001] technical field [0002] The invention belongs to the technical field of pharmaceutical preparations, and relates to a crystal X-form agomelatine tablet and a preparation method thereof. Background technique [0003] Agomelatine - a melatonin-like psychiatric drug. The melatonin analogue, agomelatine, is not only the first melatonin receptor agonist, but also a 5-hydroxytryptamine 2C (5-HT2C) receptor antagonist. Animal experiments and clinical studies have shown that the drug has the effects of antidepressant, anti-anxiety, regulating sleep rhythm and regulating the biological clock. At the same time, it has few adverse reactions, no adverse effects on sexual function, and no drug withdrawal reaction. [0004] The first melatonin receptor agonist, agomelatine (Valdoxan), is a melatonin analog, which is also a 5-hydroxytryptamine 2C (5-HT2C) receptor antagonist. The affinity Ki of melatonin to its receptors MT1 and MT2 is 8.85x10 -11 and 2.63x10 -11 , similar to a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/165A61K47/38A61K47/32A61P25/24A61P25/22A61P25/00
CPCA61K9/2027A61K9/2054C07C233/22C07B2200/13A61K9/2077A61K31/165A61K9/2095A61K9/2013A61K9/2018A61K9/2009A61P25/00A61P25/22A61P25/24
Inventor 周世旺代奕安适之赵健
Owner 天津泰普制药有限公司
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