Fast-dissolving oral film preparation comprising aripiprazole

• US 9,694,008 B2
• Filed: 08/07/2013
• Issued: 07/04/2017
• Est. Priority Date: 08/08/2012
• Status: Active Grant

• Current Assignee: CMG Pharmaceutical CO.,LTD
• Original Assignee: CMG Pharmaceutical CO.,LTD
• Inventors: Kim, Yong Soo, Shin, Jun Ho
• Primary Examiner(s): Song, Jianfeng
• Application Number:
  US14/419,231
• Publication Number:
  US 20150196558A1
• Time in Patent Office: 1,427 Days
• Field of Search: None
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays

Abstract

The present invention relates to an orally fast dissolving film formulation including aripiprazole. The orally fast dissolving film formulation includes aripiprazole or a pharmaceutically acceptable salt thereof and an organic acid. The orally fast dissolving film formulation has a pH in the range of 4.7 to 6.0. The orally fast dissolving film formulation may further include a film base polymer. The orally fast dissolving film formulation has a high dissolution rate, causes no risk of damage to oral tissues, masks a bitter taste of aripiprazole, and gives a good feeling upon taking.

Claims

1. An orally fast dissolving film formulation comprising aripiprazole or a pharmaceutically acceptable salt thereof and an organic acid,

wherein:

the film formulation has a pH in the range of 4.95 to 5.18;

the aripiprazole or the pharmaceutically acceptable salt thereof and the organic acid have a weight ratio in the range of 2;

1 to 66;

1;

the organic acid is citric acid; and

the orally fast dissolving film formulation has a pH in the range of 6.2 to 6.4 when dissolved in an oral cavity.

2. The orally fast dissolving film formulation according to claim 1, wherein the citric acid is present in an amount of 0.2 to 1.0% by weight, based on the total weight of the orally fast dissolving film formulation.

3. The orally fast dissolving film formulation according to claim 1, further comprising a sweetening agent comprising sucralose and acesulfame potassium.

4. The orally fast dissolving film formulation according to claim 1, further comprising a film base polymer essentially comprising hydroxypropyl methylcellulose and optionally polyvinyl alcohol.