Controlled release sterile injectable aripiprazole formulation and method

The formulation as defined in claim 2, wherein upon injection into a subject, said formulation releases aripiprazole over a period of at least three weeks from the date of administration.

The formulation as defined in claim 2, wherein said aripiprazole has a mean particle size of about 2.5 microns.

The formulation as defined in claim 2, wherein said formulation further comprisesn(c) one or more bulking agents; and(d) one or more buffering agents.

The formulation as defined in claim 2, wherein said formulation comprises:n(a) aripiprazole having a mean particle size of about 1 to 10 microns,(b) carboxymethyl cellulose or its sodium salt,(c) mannitol,(d) sodium phosphate to adjust pH to about 7, and(e) optionally sodium hydroxide to adjust pH to about 7, andwherein upon injection into a subject, said formulation releases aripiprazole over a period of at least about three weeks from the date of administration.

The formulation as defined in any one of claims 2, 5 and 7, wherein upon injection into a subject, said formulation releases aripiprazole over a period of three or four weeks from the date of administration.

The formulation as defined in claim 2, wherein the aripiprazole is in the form of anhydrous crystals or in the form of a monohydrate.

The formulation as defined in claim 2, wherein said formulation comprises from about 100 to about 400 mg aripiprazole per 1 mL.

The formulation as defined in claim 2, 5 or 7, wherein the aripiprazole has a mean particle size of about 2 to 4 microns.

A controlled release sterile aripiprazole injectable formulation as defined in claim 2 which is obtained by a process which comprises the steps of:n(a) preparing sterile bulk aripiprazole having a desired particle size distribution,(b) preparing a sterile vehicle comprising one or more suspending agents for the sterile bulk aripiprazole,(c) combining said sterile aripiprazole and said sterile vehicle comprising one or more sterile suspending agents to form a sterile primary suspension,(d) reducing the mean particle size of the aripiprazole in said sterile primary suspension to within the range from about 1 to about 10 microns to form a sterile final suspension containing from about 0.1 to about 400 mg of aripiprazole per mL,(e) freeze-drying said sterile final suspension to form a freeze-dried product, and(f) adding water to the freeze-dried product.

The formulation as defined in claim 2, wherein said formulation comprises from about 50 to about 400 mg aripiprazole per 2 mL.

The formulation as defined in claim 2, wherein said formulation comprises from about 100 to about 200 mg aripiprazole per 1 mL.

The formulation as defined in claim 23, wherein said formulation further comprisesn(c) one or more bulking agents; and(e) one or more buffering agents.