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Title:
オルタタキセルの固体形態
Document Type and Number:
Japanese Patent JP2011509957
Kind Code:
A
Abstract:
The present invention relates to solid forms of 13-(N-Boc-²-isobutylserinyl)-14-²-hydroxybaccatin III 1,14-carbonate (Ortataxel). Amorphous Form A, crystalline Form B, mixtures thereof and processes for preparing them are disclosed. Amorphous Form A is prepared by fast precipitation of Ortataxel from a mixture of acetone and water. Form A transforms in Form B when suspended and stirred in a mixture of ethanol and water for 4-8 hours. If the suspension is stirred for less than 4 hours, mixtures of Form B and Form A are obtained. Form B or mixtures of Forms A and B can also be obtained dissolving Ortataxel in a protic organic solvent, followed by addition of water.

Inventors:
Chicheri, Daniele
Nikola, Sardone
Gabbetta, Bruno
Ricotti, Maurizio
Application Number:
JP2010542566A
Publication Date:
March 31, 2011
Filing Date:
January 12, 2009
Export Citation:
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Assignee:
Indena Sochieta Pell Azioni
International Classes:
C07D493/08; A61K31/357; A61P35/00
Domestic Patent References:
JP2004519434A2004-07-02
JP2003503502A2003-01-28
JPH10502627A1998-03-10
Foreign References:
US7232916B12007-06-19
WO2007078050A22007-07-12
Other References:
DRUGS OF THE FUTURE, vol. 26(6), JPN6013045403, 2001, pages 533 - 544, ISSN: 0002629250
平山令明, 有機化合物結晶作製ハンドブック, JPN6014022315, 2008, pages 10 - 11, ISSN: 0003080235
HALEBLIAN,J.K.: "Characterization of Habits and Crystalline Modification of Solids and Their Pharmaceutical Applicati", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 64, no. 8, JPN6008019570, 1975, pages 1269 - 1288, ISSN: 0003080232
松本光雄編, 薬剤学マニュアル, vol. 第1版, JPN6008019571, 1989, pages 28 - 76, ISSN: 0003080233
松岡正邦: "有機物の結晶化技術の高度化−粒径,形態,多形,純度の制御−", PHARM TECH JAPAN, vol. 19, no. 6, JPN6009053754, 1 May 2003 (2003-05-01), pages 91 - 955, ISSN: 0003080234
Attorney, Agent or Firm:
Shinjiro Ono
Kazuo Shamoto
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Ken Matsumoto