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

摘要

Disclosed is a method for preparing an aripiprazole type I microcrystal, comprising the following steps: dissolving aripiprazole in an acidic solution having an acidifier, acquiring a medicament-having acidic solution; adding an alkalizer while stirring, then adding water or aqueous ethanol of 10 to 60 wt% while stirring, and separating by precipitation the aripiprazole type I microcrystal. Also disclosed are 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[mu]m, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal of the present invention allows for reduced pollution and loss, great safety, easy and convenient operation, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low costs, and facilitated applicability in industrialized manufacturing. The solid preparation of the present invention is provided with great stability, solubility, and bioavailability, reduced individual differences, and reduced content of related substances.