Low hygroscopic aripiprazole drug substance and processes for the preparation thereof

• US 8,580,796 B2
• Filed: 01/13/2012
• Issued: 11/12/2013
• Est. Priority Date: 09/25/2001
• Status: Expired due to Term

• Current Assignee: Otsuka Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
• Original Assignee: Otsuka Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
• Inventors: Bando, Takuji, Aoki, Satoshi, Kawasaki, Junichi, Ishigami, Makoto, Taniguchi, Youichi, Yabuuchi, Tsuyoshi, Fujimoto, Kiyoshi, Nishioka, Yoshihiro, Kobayashi, Noriyuki, Fujimura, Tsutomu, Takahashi, Masanori, Abe, Kaoru, Nakagawa, Tomonori, Shinhama, Koichi, Utsumi, Naoto, Tominaga, Michiaki, Ooi, Yoshihiro, Yamada, Shohei, Tomikawa, Kenji
• Primary Examiner(s): Wilson, James O
• Assistant Examiner(s): Sackey, Ebenezer O
• Application Number:
  US13/350,117
• Publication Number:
  US 20120315302A1
• Time in Patent Office: 669 Days
• Field of Search: 514/253.07, 544/363
• US Class Current: 514/253.07
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/32 Alcohol-abuse
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: C07B 2200/13 Crystalline forms, e.g. polymorphs
• CPC Class Codes: C07D 215/22 attached in position 2 or 4
• CPC Class Codes: C07D 215/227 only one oxygen atom which is attached in position 2
• CPC Class Codes: Y10T 428/2982 Particulate matter [e.g., sphere, flake, etc.]

Abstract

The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.

Claims

1. Anhydrous Aripiprazole Crystals B having low hygroscopicity wherein said low hygroscopicity is defined as a moisture content of 0.40% or less when said Crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°

C. and a humidity level of 100%.

2. Anhydrous Aripiprazole Crystals B having low hygroscopicity wherein said low hygroscopicity is defined as a moisture content of 0.10% or less when said Crystals are placed for 24 hours in a dessicator maintained at a temperature of 60°

C. and a humidity level of 100%.