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Agomelatine oral liquid preparation as well as preparation method and application thereof

A technology for agomelatine and liquid preparations, which is applied in the field of agomelatine preparations, which can solve the problems of not being able to reach the solubilization level of agomelatine, and achieve the reduction of individual absorption differences, rapid and uniform absorption, and stability good effect

Active Publication Date: 2017-05-24
ANCUREALL PHARMA SHANGHAI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor of this patent repeatedly prepared the agomelatine-cyclodextrin powder of the above two patents and found that these two technologies are far from reaching the same solubilization level of agomelatine as this patent (25mg / ml)

Method used

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  • Agomelatine oral liquid preparation as well as preparation method and application thereof
  • Agomelatine oral liquid preparation as well as preparation method and application thereof
  • Agomelatine oral liquid preparation as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055]

[0056] Add appropriate amount of water to hydroxypropyl-β-cyclodextrin, heat and stir at 70°C and 600rpm to dissolve, then add agomelatine, continue heating and stirring for 5 hours, add preservatives methyl paraben and propyl paraben Stir to dissolve the ester, cool to room temperature, and dilute to 500ml with ultrapure water, shake well to obtain a colorless, clear and transparent agomelatine oral solution, the pH of which is 7.1 after testing.

[0057] Under sterile conditions, the solution was filtered through a 0.22 μm filter membrane into a sterile container, subpackaged and stored at 4°C and 60°C, and the precipitation and purity content stability were investigated on the 10th day. The sample was stable at 4°C, no crystals of agomelatine precipitated, and the content of related substances passed the test after 10 days at 60°C.

[0058] The average degree of substitution of hydroxypropyl-β-cyclodextrin is 3.5.

[0059] The crystal form of agomelatine is cry...

Embodiment 2

[0061]

[0062] Add appropriate amount of water to hydroxypropyl-β-cyclodextrin, heat and stir at 55°C and 700rpm to dissolve, add agomelatine, continue heating and stirring for 2.5h, add preservatives methyl paraben and paraben Propyl ester, stirred until dissolved, cooled to room temperature, dilute to 500ml with ultra-pure water, shake well to obtain colorless, clear and transparent agomelatine oral solution, pH is 7.1 after testing.

[0063] Under sterile conditions, the solution was filtered through a 0.22 μm filter membrane into a sterile container, subpackaged and stored at 4°C and 60°C, and the precipitation and purity content stability were investigated on the 10th day. The sample was stable at 4°C, no crystals of agomelatine precipitated, and the content of related substances passed the test after 10 days at 60°C.

[0064] The average degree of substitution of hydroxypropyl-β-cyclodextrin is 6.0.

[0065] The crystal form of agomelatine is crystal form I.

Embodiment 3

[0067]

[0068] Add appropriate amount of water to hydroxypropyl-β-cyclodextrin, heat and stir at 65°C and 800rpm to dissolve, then add agomelatine powder, continue heating and stirring for 1.5h, add preservative sorbic acid, and add sodium hydroxide to adjust pH , stir until dissolved, after cooling to room temperature, dilute to 500ml with ultrapure water, shake well to obtain a colorless, clear and transparent agomelatine oral solution, the pH of which is 4.5 after testing.

[0069] Under sterile conditions, the solution was filtered through a 0.22 μm filter membrane into a sterile container, subpackaged and stored at 4°C and 60°C, and the precipitation and purity content stability were investigated on the 10th day. The sample was stable at 4°C, no crystals of agomelatine precipitated, and the content of related substances passed the test after 10 days at 60°C.

[0070] The average degree of substitution of hydroxypropyl-β-cyclodextrin was 5.0.

[0071] Agomelatine is a...

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Abstract

The invention discloses an Agomelatine oral liquid preparation as well as a preparation method and application thereof. The Agomelatine oral liquid preparation comprises Agomelatine, cyclodextrin and a pharmaceutically-acceptable adjuvant, wherein the mass ratio of Agomelatine to cyclodextrin is (1:1) to (1:50). The oral liquid is in a stable and uniform aqueous solution state, solves the problem of low dissolution rate of an Argomeline tablet, ensures the rapid and uniform absorption of the Agomelatine in body gastrointestinal tracts and reduces the individual absorption difference of the Argomeline. The oral liquid preparation disclosed by the invention is less in adjuvant dosage, simple in preparation process, low in cost and suitable for large-scale production. Therefore, the developed oral liquid has significant market values and prospects.

Description

technical field [0001] The invention relates to an agomelatine preparation for treating depression. Background technique [0002] Agomelatine (Agomelatine) is a common oral tablet first developed by the French Servier company, which was approved in the European Union in 2009. Molecular formula C 15 h 17 NO 2 , the molecular weight is 243.3. Its structural formula is as follows: [0003] [0004] Agomelatine is a melatonin-like compound that is a melatonin receptor (Melatonin Receptor, MT 1 / MT 2 ) agonists and 5-HT receptors (Serotonin Receptor, 5-HT 2C ) antagonist, in addition to having a good antidepressant effect, agomelatine also shows a good sleep regulation effect. At the same time, agomelatine does not affect the level of extracellular serotonin, has no obvious effect on the reuptake of monoamine neurotransmitters, and has no significant effect on the reuptake of α, β-adrenergic receptors, histamine receptors, and cholinergic receptors. and benzodiazepine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/165A61K47/40A61P25/24A61P25/22A61P25/20
Inventor 司聚同明从梅季苏南
Owner ANCUREALL PHARMA SHANGHAI CO LTD
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