Title:
α-CRYSTAL POLYMORPHISM OF LEVONORGESTREL AND PRODUCTION METHOD THEREOF
Document Type and Number:
Japanese Patent JP2016006090
Kind Code:
A
Abstract:
PROBLEM TO BE SOLVED: To provide a novel crystal polymorphism of levonorgestrel which is useful as an emergency contraceptive or the like, and to provide a production method thereof, as well as to provide a pharmaceutical composition.SOLUTION: The invention provides an α-crystal polymorphism of levonorgestrel in which a diffraction angle 2θ has a diffraction peak at 2θ=17.2° ±0.2°, 18.6° ±0.2°, 22.7° ±0.2°, 31.1° ±0.2°, and 35.5° ±0.2° in powder X-ray diffraction spectrum. When the strength of the diffraction peak at 2θ=18.6° ±0.2° is X, and the strength of the diffraction peak at 2θ=31.1° ±0.2° is X, the intensity ratio X/Xof Xand Xis 25/100-400/100. The invention also provides a method for producing the α-crystal polymorphism by mixing a dioxane solution of levonorgestrel with a mixed solvent that contains water and dioxane in a weight ratio of water/dioxane=50/0-95/5.
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Inventors:
IWASHITA SHIGEKI
HAYASHI HIROYUKI
NAKAGAWA TAKAYOSHI
MIYAZAKI KOICHI
HAYASHI HIROYUKI
NAKAGAWA TAKAYOSHI
MIYAZAKI KOICHI
Application Number:
JP2015152482A
Publication Date:
January 14, 2016
Filing Date:
July 31, 2015
Export Citation:
Assignee:
ASKA PHARM CO LTD
International Classes:
C07J1/00; A61K31/567; A61P15/18
Domestic Patent References:
| JP5809367B2 | 2015-11-10 |
Foreign References:
| WO2009035527A2 | 2009-03-19 | |||
| WO2012110947A1 | 2012-08-23 |
Other References:
BULLETIN DES SOCIETES CHIMIQUES BELGES, vol. ９２, JPN6014029905, 1983, pages 275 - 287, ISSN: 0003661701
ACTA CRYSTALLOGRAPHICA, SECTION B: STRUCTURAL CRYSTALLOGRAPHY AND CRYSTAL CHEMISTRY, vol. Ｂ３１, JPN6014029906, 1975, pages 2040 - 2043, ISSN: 0003661702
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: 0003661695
"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: 0003661696
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: 0003661697
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: 0003661698
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: 0003661699
HELVETICA CHIMICA ACTA, vol. ７８, JPN6014029904, 1995, pages 1345 - 1391, ISSN: 0003661700
ACTA CRYSTALLOGRAPHICA, SECTION B: STRUCTURAL CRYSTALLOGRAPHY AND CRYSTAL CHEMISTRY, vol. Ｂ３１, JPN6014029906, 1975, pages 2040 - 2043, ISSN: 0003661702
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: 0003661695
"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: 0003661696
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: 0003661697
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: 0003661698
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: 0003661699
HELVETICA CHIMICA ACTA, vol. ７８, JPN6014029904, 1995, pages 1345 - 1391, ISSN: 0003661700
Attorney, Agent or Firm:
Mitsuo Kata
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