Title:
CRYSTALLINE POLYMORPH OF 15Β-HYDROXY-OSATERONE ACETATE
Document Type and Number:
WIPO Patent Application WO/2017/195804
Kind Code:
A1
Abstract:
Provided is a crystalline polymorph A of 15β-hydroxy-osaterone acetate having improved stabilities (storage stability, pulverization stability, and absorption property). Diffraction peaks characteristic of this crystalline polymorph A of 15β-hydroxy-osaterone acetate, in a powder X-ray diffraction spectrum, appear at diffraction angles 2θ of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorph A has a melting point of 280-283°C, and is a prismatic crystal.
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Inventors:
NAKAGAWA TAKAYOSHI (JP)
HAYASHI HIROYUKI (JP)
MIYAZAKI KOICHI (JP)
IWASHITA SHIGEKI (JP)
HAYASHI HIROYUKI (JP)
MIYAZAKI KOICHI (JP)
IWASHITA SHIGEKI (JP)
Application Number:
PCT/JP2017/017619
Publication Date:
November 16, 2017
Filing Date:
May 10, 2017
Export Citation:
Assignee:
ASKA PHARM CO LTD (JP)
International Classes:
C07J73/00; A61K31/58; A61P13/08; A61P17/00; A61P17/02; A61P17/14; A61P35/00
Foreign References:
| JP2591640B2 | 1997-03-19 | |||
| JPH04261193A | 1992-09-17 | |||
| JPS62195398A | 1987-08-28 | |||
| JPS61204199A | 1986-09-10 | |||
| JPS61204198A | 1986-09-10 | |||
| JP2591640B2 | 1997-03-19 |
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CHEM. PHARM. BULL., vol. 41, no. 5, 1993, pages 870 - 875
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"Pharmaceutics", 1997, NANKODO, CO., LTD.
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MANGIN, DENIS ET AL.: "Polymorphism in Processes of Crystallization in Solution: A Practical Review", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 13, no. 6, 2009, pages 1241 - 1253, XP055283229, DOI: 10.1021/op900168f
MURAMATSU, MITSUO ET AL.: "Thermodynamic relationship between α‐ and β‐forms of crystalline progesterone", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 68, no. 2, 1979, pages 175 - 177, XP055599876
SHIBATA, KENYU ET AL.: "Antiandrogen. I. 2-Azapregnane and 2-Oxapregnane Steroids", CHEM. PHARM. BULL., vol. 40, no. 4, 1992, pages 935 - 941, XP002143084
CHEM. PHARM. BULL., vol. 41, no. 5, 1993, pages 870 - 875
"Japanese Pharmacopoeia, (1) Handbook of Pharmaceutical Excipients", 1989, MARUZEN COMPANY, LTD.
"Japanese Pharmaceutical Excipients Dictionary", February 2016, YAKUJI NIPPO LTD.
"Pharmaceutics", 1997, NANKODO, CO., LTD.
"Japanese Pharmaceutical Excipients", August 2003, YAKUJI NIPPO LTD.
"Japanese Pharmacopoeia"
Attorney, Agent or Firm:
KUWATA Mitsuo et al. (JP)
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