Claims for Patent: 11,701,352
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Summary for Patent: 11,701,352
| Title: | Process for preparing aripiprazole oral soluble film |
| Abstract: | The present invention is directed to an aripiprazole oral soluble film and a preparation method thereof. The aripiprazole oral soluble film comprises 10-60% w/w of aripiprazole in a crystalline state and 30-95% w/w of one or more film-forming materials, wherein 90% of the aripiprazole particles have a size of ≤14.3 μm and are uniformly blended in the film without visible undispersed particles. The aripiprazole oral soluble film has excellent bioavailability, uniformity, stability, and palatability. The oral soluble film preparation is prepared by first grinding aripiprazole particles to have desired small particle sizes, then blending the aripiprazole particles with film forming materials in an aqueous solution to a uniform suspension, defoaming the suspension, and coating the suspension on a substrate and drying it to form a film. |
| Inventor(s): | Rongbin Ling, Lingyu Cai, Fuxiang LIN, Yong Yu, Xiaojin Xiao |
| Assignee: | Xiamen LP Pharmaceutical Co Ltd |
| Application Number: | US17/552,333 |
| Patent Claims: |
1. A process for preparing an aripiprazole oral soluble film comprising aripiprazole in a crystalline state, comprising the steps of: (a) grinding a starting material of aripiprazole by a milling process until 90% of the aripiprazole particles have a size of <14.3 μm, wherein the aripiprazole maintains a crystalline state; (b) blending the aripiprazole particles of (a) and one or more film-forming materials in an aqueous solution by homogenization blending at a speed of at least 1500 rpm followed by plate-and-frame blending to prepare a uniform suspension, (c) defoaming the suspension; and (d) coating the defoamed suspension on a substrate and drying the suspension to form the film. 2. The process according to claim 1, wherein the milling process is bead milling, air crushing, or colloid milling. 3. The process according to claim 2, wherein the bead milling has a scatter axis speed of >3000 rpm and the milling cycles >3 cycles. 4. The process according to claim 1, wherein the film-forming material is selected from the group consisting of hypromellose, polyvinyl alcohol, copovidone, povidone, hydroxyethyl cellulose, hydroxypropyl cellulose, and any combination thereof. 5. The process according to claim 1, wherein the aqueous solution of step (b) does not contain an organic solvent. 6. The process according to claim 1, where in step (b), the aqueous solution further comprises a defoamer. 7. The process according to claim 6, wherein the defoamer comprises dimethicone, simethicone, oleyl alcohol, or a combination thereof. 8. The process according to claim 6, wherein deforming is a vacuum deforming. |
