|Title:||Aripiprazole complex formulation and method|
|Abstract:|| An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a .beta.-cyclodextrin, preferably, sulfobutyl ether .beta.-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided.|
|Inventor(s):|| Nerurkar; Manoj (Bangalore, IN), Naringrekar; Vijay H. (Princeton, NJ) |
|Assignee:|| Otsuka Pharmaceutical Co., Ltd. (Tokyo, JP) |
|Filing Date:||Apr 29, 2013|
|Claims:||1. An aqueous injectable formulation having a pH of from about 3.5 to about 5, comprising: a) a complex comprising aripiprazole and sulfobutyl ether-.beta.-cyclodextrin; b) tartaric acid; c) sodium hydroxide; and d) wafer for injection. |
2. The formulation as defined in claim 1 which contains 2 mg aripiprazole/ml, 5 mg aripiprazole/ml or 7.5 mg aripiprazole/ml.
3. The formulation as defined in claim 1 comprising from about 0.1 to about 2.5% by weight aripiprazole.
4. The formulation as defined in claim 1 comprising from about 0.2 to about 1.5% by weight aripiprazole.
5. The formulation as defined in claim 1 wherein the sulfobutyl ether-.beta.-cyclodextrin is present in an amount from about 100 to about 700 mg/m of solution.
6. The formulation as defined in claim 1 wherein the tartaric acid is present in an amount from about 7 to about 9 mg/mi.