Aripiprazole type I microcrystal, aripiprazole solid preparations, and preparation method

摘要

A method for preparing an aripiprazole type I microcrystal, including the following steps: dissolving aripiprazole in an acidifier, acquiring a medicament-having acid solution; adding an alkalizer while stirring, then adding water or aqueous ethanol 10 to 60 wt % while stirring, and separating by precipitation the aripiprazole type I microcrystal. Furthermore, a method for preparing a solid preparation having the aripiprazole type I microcrystal, an aripiprazole microcrystal having an average particle size of less than 20 μm, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal allows reduced pollution and loss, great safety, easy and convenient, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low cost, and facilitated applicability in industrialized manufacturing. This solid preparation provides great stability, solubility, and bioavailability, reduced individual differences, and reduced content of related substances.

主权项

1. A method of preparing an aripiprazole type I microcrystal having an average particle size of no more than 50 μm, comprising:
adding aripiprazole to an aqueous ethanol solution containing an acid to dissolve the aripiprazole and obtain a medicament-having acid solution; adding an alkalizer while stirring at room temperature; then adding water or 10-60 wt. % aqueous ethanol while stirring at room temperature; and separating a precipitated aripiprazole type I microcrystal.