Stable aripiprazole orally disintegrating tablet and preparation method thereof
A technology for oral disintegrating tablets and aripiprazole, which is applied in the field of oral disintegrating tablets, can solve the problems of product instability, affecting drug solubility and melting point, affecting drug stability, etc., and achieves stable product quality, good taste, and production. simple craftsmanship
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reference example 1
[0029] Reference Example 1: Preparation of Active Ingredient Aripiprazole
[0030] Take 36 kg of aripiprazole crude product, add 220 liters of methyl ethyl ketone and 22.5 liters of acetone, heat to reflux to dissolve, cool to 0-5°C, filter, vacuum-dry at 40-50°C for 3-5 hours, and then pass through airflow Pulverize to obtain micronized aripiprazole anhydrate with d(0.9) below 40 μm.
[0031] Micronized aripiprazole anhydrous X-ray powder diffraction pattern sees attached figure 1 , the hygroscopicity of the prepared aripiprazole is 1.8-2.5% after being placed under the conditions of 100% RH and 60° C. for 24 hours.
Embodiment 1
[0037]
[0038] Wherein the particle size of aripiprazole d(0.9)=37 μm.
[0039] Preparation method: mix aripiprazole, pregelatinized starch, microcrystalline cellulose, mannitol, aspartame, and tartaric acid evenly, add appropriate amount of absolute ethanol to granulate, and dry with a fluidized bed. Croscarmellose sodium, silicon dioxide and magnesium stearate are uniformly mixed and pressed into tablets.
[0040] The samples of comparative example 1 and embodiment 1 are all tested stripping curves with the same method (paddle method 60rpm, pH4.0 acetate buffer solution 900mL), and the results are as follows:
[0041] sample 5 10 15 20 30 45 60 Comparative Example 1 66 78 84 86 86 86 86 Example 1 78 88 93 95 98 99 99
[0042] In addition, the samples of Comparative Example 1 and Example 1 were simultaneously placed at 60°C and 75% relative humidity for 10 days to detect related substances, and the results were as follows:
...
Embodiment 2
[0046]
[0047] Wherein the particle size of aripiprazole d(0.9)=22 μm.
[0048] Preparation method: mix aripiprazole, pregelatinized starch, microcrystalline cellulose, mannitol, red iron oxide, aspartame, and tartaric acid evenly, add appropriate amount of absolute ethanol to granulate, and dry in a fluidized bed. After granulation, it is mixed evenly with croscarmellose sodium, vanillin, silicon dioxide and magnesium stearate, and pressed into tablets.
[0049] Mix all the materials except aripiprazole evenly, and use them as blank excipients to determine the crystal forms of aripiprazole, blank excipients, and the aripiprazole orally disintegrating tablets prepared in Example 2, and the X-ray powder diffraction Spectrum (XRPD) as attached Figure 1~3 shown. In addition, after the sample of Example 2 was placed under accelerated conditions (40±2°C, 75±5% relative humidity) for 6 months, the crystal form was determined, and its XRPD pattern is shown in the attached Fi...
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