Polymorph control of pharmaceutical compounds

2016 Fiscal Year Final Research Report

• Project/Area Number: 15K14942
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Physical pharmacy
• Research Institution: Osaka University
• Principal Investigator: YOSHIMURA MASASHI 大阪大学, レーザーエネルギー学研究センター, 教授 (60314382)
• Project Period (FY): 2015-04-01 – 2017-03-31
• Keywords: 薬剤有機分子 / アセトアミノフェン / 準安定形選択晶出 / ソノクリスタリゼーション / ポリマー誘起核発生 / 溶液媒介相転移

Outline of Final Research Achievements

We have developed an original method for selective crystallization of metastable phase acetaminophen form II　by applied ultrasonic irradiation. In this research, we attempted to control the crystallinity in order to improve temporal stability of form II.　We found that crystals of form II grown at low growth rate have high transparency and fewer defects. Powder X-ray diffraction measurement reveals that form II grown at low growth rate shows higher temporal stability than seed crystals nucleated by ultrasonic irradiation. We have also developed a new method of obtaining the metastable phase form II crystals of acetaminophen. Solution-mediated phase transformation (SMPT) from trihydrate into form II is utilized to obtain form II crystals. SMPT is triggered by seeding form II crystals into a saturated solution including trihydrate crystals, which are less stable than form II crystals.

Free Research Field

結晶工学