Aripiprazole long-acting controlled-release microgranule injection and preparation method thereof
A technology of aripiprazole and sustained-release microparticles, which is applied in the field of aripiprazole long-acting sustained-release microparticle injections and its preparation, which can solve the problem that the drug cannot be completely released from the microparticles, and the ideal in vitro drug release behavior cannot be achieved. Slowness and other problems, to achieve the effect of overcoming sudden release, low burst release, and complete release
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[0053] Example 1
[0054] Preparation of Aripiprazole Microparticles:
[0055]
[0056] Dissolve polylactic acid-glycolic acid and aripiprazole with a solvent and release characteristics regulator, then add them to a mixed solution of PVA and water, keep the solidification temperature at 0°C, and emulsify at 1000 (rpm) under magnetic stirring for 30 minutes Then, reduce the speed and stir to 500 (rpm) for 1 hour to volatilize the solvent. After the particles are solidified, the particles are separated, and the particles are continuously washed with sterile water for 8 hours. Filter out and dry in vacuum at room temperature for 24h;
[0057] The diameter of the prepared particles is 73.56±24.34μm, the drug loading is 35.97%, and the encapsulation efficiency is 89.94%.
[0058] Detected by HPLC and GC methods, the weight percentage content of each component of the particles:
[0059]
[0060]
Example Embodiment
[0061] Example 2
[0062] Preparation of Aripiprazole Microparticles:
[0063]
[0064] Dissolve polylactic acid and aripiprazole with a solvent and drug release characteristics regulator, then add them to a mixed solution of PVA and water, keep the solidification temperature at 5°C, emulsify at 2000 (rpm) under magnetic stirring for 15 minutes, and reduce Stir at 500 (rpm) for 0.5h to volatilize the solvent. After the particles are solidified, the particles are separated, and the particles are continuously washed with sterile water for 8 hours. Filter out and dry in vacuum at room temperature for 24h;
[0065] The diameter of the prepared particles is 77.02±25.48μm, the drug loading is 44.80%, and the encapsulation efficiency is 89.17%.
[0066] Detected by HPLC and GC methods, the weight percentage content of each component of the particles:
[0067]
Example Embodiment
[0068] Example 3
[0069] Preparation of Aripiprazole Microparticles:
[0070]
[0071]
[0072] Dissolve polylactic acid-glycolic acid and aripiprazole with a solvent and release characteristics regulator, then add them to the mixed solution of PVA and water, keep the curing temperature at 20℃, and emulsify at 1000 (rpm) under magnetic stirring for 20 minutes Then, reduce the speed and stir to 500 (rpm) for 1 hour to volatilize the solvent. After the particles are solidified, the particles are separated, and the particles are continuously washed with sterile water for 8 hours. Filter out and dry in vacuum at room temperature for 24h;
[0073] The diameter of the prepared particles is 80.39±20.38 μm, the drug loading is 25.03%, and the encapsulation efficiency is 75.87%.
[0074] Detected by HPLC and GC methods, the weight percentage content of each component of the particles:
[0075]
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