Iloperidone inclusion compound included by beta-cyclodextrin and medicinal composition thereof
A technology of iloperidone and cyclodextrin, which is applied in the field of iloperidone β-cyclodextrin inclusion complex and its pharmaceutical composition, and can solve the problems such as failure to solve the rapid onset of iloperidone
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Embodiment 1
[0053] prescription:
[0054] Imperidone 10g
[0055] Hydroxypropyl β-cyclodextrin 500g
[0056] Tartaric acid 50g
[0057] 1mol / L sodium hydroxide solution appropriate amount
[0058] Water for injection up to 10L
[0059] The preparation is as follows: (50:1, 5:1)
[0060] Add an appropriate amount of water for injection into a stainless steel dispenser, under constant stirring, add 50 grams of tartaric acid buffer and 500 grams of hydroxypropyl β-cyclodextrin into the quantitative container and dissolve in water, add 10 grams of ipoperidone to the quantitative The container, continue to stir until the iloperidone is dissolved, add an appropriate amount of 1mol / L sodium hydroxide into the container, adjust the pH to about 4, and obtain a solution. Under stirring conditions, add water for injection to the above solution and adjust the final batch to 10L to obtain an injection solution.
[0061] The above injection solution is sterilized and filtered through a 0.22μm filter membrane, fil...
Embodiment 2
[0063] prescription:
[0064] Imperidone 20g
[0065] Hydroxypropyl β-cyclodextrin 1600g
[0066] Tartaric acid 20g
[0067] 1mol / L sodium hydroxide solution appropriate amount
[0068] Water for injection up to 10L
[0069] The preparation is as follows: (80:1, 1:1)
[0070] Add an appropriate amount of water for injection into a stainless steel dispenser. Under constant stirring, add 20 grams of tartaric acid buffer and 1600 grams of hydroxypropyl β-cyclodextrin to the quantitative container and dissolve in water. Add 20 grams of ipoperidone to the quantitative In the container, continue to stir until the iloperidone is dissolved, add an appropriate amount of 1mol / L sodium hydroxide to the container, and adjust the pH to about 4.5. Under stirring conditions, add water for injection to the above solution and adjust the final batch to 10L to obtain injection.
[0071] The above injection solution is sterilized and filtered through a 0.22 μm filter membrane, filtered into a sterilized con...
Embodiment 3
[0073] prescription:
[0074] Imperidone 40g
[0075] Hydroxypropyl β-cyclodextrin 400 g
[0076] Citric acid 300g
[0077] 1mol / L sodium hydroxide solution appropriate amount
[0078] Water for injection up to 10L
[0079] The preparation is as follows: (10:1, 7.5:1)
[0080] Add an appropriate amount of water for injection into a stainless steel dispenser, under constant stirring, add 300 grams of citric acid buffer and 400 grams of hydroxypropyl β-cyclodextrin into the quantitative container and dissolve in water, add 40 grams of ipoperidone In the quantitative container, continue to stir until the iloperidone is dissolved, add an appropriate amount of 1 mol / L sodium hydroxide to the container, adjust the pH to about 4.5, and obtain a solution. Under stirring conditions, add water for injection to the above solution and adjust the final batch to 10L to obtain injection.
[0081] The above injection solution is sterilized and filtered through a 0.22 μm filter membrane, filtered into a ...
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