Agomelatine oral liquid preparation and its preparation method and application
A technology of agomelatine hydroxypropyl and liquid preparations, which is applied in the field of agomelatine preparations, and can solve problems such as the inability to reach the solubilization level of agomelatine, reduce individual absorption differences, and solve dissolution rate Reduce and reduce the effect of oral irritation
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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.
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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