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Stable crystalline form I agomelatine tablets and preparation method thereof

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

Inactive Publication Date: 2015-05-06
TIANJIN TAIPU PHARMA SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] (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;
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 crystalline form I agomelatine tablets and preparation method thereof
  • Stable crystalline form I agomelatine tablets and preparation method thereof
  • Stable crystalline form I agomelatine tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Agomelatine (Crystal Form I 99%) 25g

[0134] water 20ml

[0135] Lactose 102g

[0136] Hydroxypropyl Cellulose 3g

[0137] Polyvinylpyrrolidone k30 3g

[0138] Croscarmellose Sodium 13g

[0139] Magnesium Stearate 1.3g

[0140] Stearic acid 2.6g

[0141] Silica 0.3g

[0142] Process: Sieve crystal form I agomelatine according to the above weight for later use; take hydroxypropyl cellulose and polyvinylpyrrolidone k30 and stir to dissolve in water (about 40°C), let cool to room temperature, add crystal form I agomelatine Stir the gomelatine well to obtain the protective agent containing crystalline type I agomelatine for later use; then add lactose and part (1 / 2) croscarmellose sodium into the wet mixing granulator and mix evenly , then add the protective agent containing crystalline type I agomelatine, granulate for 2 minutes, and granulate through a swing granulator (833um aperture sieve); fluidized bed drying (inlet air temperature 45°C, boiling bed temperatur...

Embodiment 2

[0144] Agomelatine (more than 90% crystal type I) 25g

[0145] water 30ml

[0146] Lactose 102g

[0147] Hypromellose 4.5g

[0148] Polyvinylpyrrolidone k30 4.5g

[0149] Cross-linked polyvinylpyrrolidone 13g

[0150] Magnesium Stearate 1.3g

[0151] Stearic acid 2.6g

[0152] Silica 0.3g

[0153] Process: Sieve crystal form I agomelatine according to the above weight for later use; take hydroxypropyl methylcellulose and polyvinylpyrrolidone k30 and dissolve them in water (about 40°C), let cool to room temperature, add crystal form I Stir agomelatine evenly; obtain the protective agent containing crystalline type I agomelatine for later use; then add lactose and part (1 / 2) cross-linked polyvinylpyrrolidone into the wet mixing granulator and mix evenly, and then Add the protective agent containing crystalline type I agomelatine, granulate for 2 minutes, and granulate through a swing granulator (833um aperture sieve); fluidized bed drying (inlet air temperature 45°C, boil...

Embodiment 3

[0155] Agomelatine (more than 85% crystal type I) 25g

[0156] water 30ml

[0157] Lactose 99g

[0158] Hypromellose 4.5g

[0159] Hydroxypropyl Cellulose 4.5g

[0160] Croscarmellose Sodium 13g

[0161] Magnesium Stearate 1.3g

[0162] Stearic acid 2.6g

[0163] Silica 0.3g

[0164] Process: Sieve agomelatine crystal I according to the above weight for later use; take hydroxypropyl methylcellulose and hydroxypropyl cellulose and stir and dissolve in water (about 40°C), let cool to room temperature, add crystal I Type agomelatine was stirred evenly; the protective agent containing crystalline type I agomelatine was obtained for later use; then lactose and part (1 / 2) croscarmellose sodium were added to the wet mixing granulator Mix well, then add the protective agent containing crystalline type I agomelatine, granulate for 2 minutes, and granulate through a swing granulator (833um aperture sieve); fluidized bed drying (inlet air temperature 45°C, boiling bed temperature ...

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Abstract

The invention discloses stable crystalline form I agomelatine tablets and a preparation method thereof. The method comprises the following steps: adding one or several protective agents into purified water, stirring, heating to the temperature of 35-40 DEG C, dissolving until the mixture is clarified, cooling to room temperature, adding crystalline form I agomelatine, and uniformly stirring to obtain a protective agent containing the crystalline form I agomelatine; uniformly mixing partial pharmaceutical excipients, adding the protective agent containing the crystalline form I agomelatine, and performing wet mixed granulating and drying to obtain granules containing the crystalline form I agomelatine; finally, adding the rest pharmaceutical excipients for uniformly mixing according to a ratio, and tabletting. According to the preparation method, the condition that the crystalline form I is not changed in the tablet preparation process can be fully guaranteed; the stability of the crystalline form I and related substances is high, and the requirement of large-scale production can be completely met.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a stable crystal type I agomelatine tablet and a preparation method thereof. Background technique [0002] 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. [0003] 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 ago...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/165A61K47/38A61K47/32A61P25/24A61P25/22A61P25/20
CPCA61K9/2027A61K9/2054A61K9/2077A61K31/165A61P25/20A61P25/22A61P25/24A61K9/2009A61K9/2013A61K9/2018A61K9/2095
Inventor 周世旺代奕安适之赵健
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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