Title:
DARUNAVIR POLYMORPH AND PROCESS FOR PRODUCTION THEREOF
Document Type and Number:
Japanese Patent JP2016028085
Kind Code:
A
Abstract:
PROBLEM TO BE SOLVED: To provide a stable polymorph of darunavir which is crystalline, stable, non-hygroscopic in nature and free from other pseudopolymorphs or solvates, and a process for its production.SOLUTION: There is provided a crystalline darunavir hydrate substantially free of any non-aqueous solvent. Also provided is a process for producing a crystalline form of darunavir (Form C) which is a hydrate having an X-ray diffraction pattern of the figure 1, the process comprising: stirring darunavir represented by the formula (I) having at least one non-aqueous solvent in the crystal lattice, in a mixture of water miscible solvent and water; then filtering the mixture to obtain a solid; stirring the solid in water; filtering the solid/water mixture; and drying it.SELECTED DRAWING: Figure 1
Inventors:
MANJINDER SINGH PHULL
DHARMARAJ RAMACHANDRA RAO
RAJENDRA NARAYANRAO KANKAN
DHARMARAJ RAMACHANDRA RAO
RAJENDRA NARAYANRAO KANKAN
Application Number:
JP2015182821A
Publication Date:
February 25, 2016
Filing Date:
September 16, 2015
Export Citation:
Assignee:
CIPLA LTD
International Classes:
C07D493/04; A61K31/343; A61P31/18; A61P43/00
Domestic Patent References:
| JP2005533068A | 2005-11-04 |
Foreign References:
| WO2011073993A1 | 2011-06-23 | |||
| WO2011048604A2 | 2011-04-28 |
Other References:
EUR. J. PHARM. SCI., vol. ３８, JPN6014020101, 2009, pages 489 - 497, ISSN: 0003444985
川口洋子ら: "医薬品と結晶多形", 生活工学研究, vol. 4, no. 2, JPN6014015069, 2002, pages 310 - 317, ISSN: 0003444986
"新医薬品の規格及び試験方法の設定について", 医薬審発第５６８号, JPN6010021254, 2001, ISSN: 0003444987
大島寛: "結晶多形・擬多形の析出挙動と制御", PHARM STAGE, vol. 6, no. 10, JPN6011001457, 15 January 2007 (2007-01-15), pages 48 - 53, ISSN: 0003444988
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0003444989
山野光久: "医薬品のプロセス研究における結晶多形現象への取り組み", 有機合成化学協会誌, vol. 65, no. 9, JPN6010003277, 1 September 2007 (2007-09-01), pages 907 - 69, ISSN: 0003444990
BYRN S: "PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS", PHARMACEUTICAL RESEARCH, vol. V12 N7, JPN5013009960, 1 July 1995 (1995-07-01), US, pages 945 - 954, XP055307460, ISSN: 0003444991, DOI: 10.1023/A:1016241927429
J. MOL. BIOL., vol. ３３８, JPN6014020102, 2004, pages 341 - 352, ISSN: 0003444992
川口洋子ら: "医薬品と結晶多形", 生活工学研究, vol. 4, no. 2, JPN6014015069, 2002, pages 310 - 317, ISSN: 0003444986
"新医薬品の規格及び試験方法の設定について", 医薬審発第５６８号, JPN6010021254, 2001, ISSN: 0003444987
大島寛: "結晶多形・擬多形の析出挙動と制御", PHARM STAGE, vol. 6, no. 10, JPN6011001457, 15 January 2007 (2007-01-15), pages 48 - 53, ISSN: 0003444988
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0003444989
山野光久: "医薬品のプロセス研究における結晶多形現象への取り組み", 有機合成化学協会誌, vol. 65, no. 9, JPN6010003277, 1 September 2007 (2007-09-01), pages 907 - 69, ISSN: 0003444990
BYRN S: "PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS", PHARMACEUTICAL RESEARCH, vol. V12 N7, JPN5013009960, 1 July 1995 (1995-07-01), US, pages 945 - 954, XP055307460, ISSN: 0003444991, DOI: 10.1023/A:1016241927429
J. MOL. BIOL., vol. ３３８, JPN6014020102, 2004, pages 341 - 352, ISSN: 0003444992
Attorney, Agent or Firm:
Toru Ishikawa
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