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&bgr;-CRYSTAL POLYMORPHISM OF LEVONORGESTREL AND PRODUCTION METHOD THEREOF
专利权人:
ASKA PHARMACEUTICAL CO LTD;あすか製薬株式会社
发明人:
IWASHITA SHIGEKI,岩下 茂樹,HAYASHI HIROYUKI,林 博之,NAKAGAWA TAKAYOSHI,中川 隆義,MIYAZAKI KOICHI,宮崎 宏一
申请号:
JP2015152491
公开号:
JP2016006091A
申请日:
2015.07.31
申请国别(地区):
JP
年份:
2016
代理人:
摘要:
PROBLEM TO BE SOLVED: To provide a novel crystal polymorphism of levonorgestrel which is a steroid useful as an emergency contraceptive or the like, and to provide a production method thereof, as well as to provide a pharmaceutical composition containing the crystal polymorphism.SOLUTION: The invention provides: a &bgr;-crystal polymorphism of levonorgestrel in which a diffraction angle 2&thetas; has a diffraction peak at 2&thetas;=13.9° ±0.2°, 14.5° ±0.2°, 21.3° ±0.2°, 24.9° ±0.2°, and 28.2° ±0.2° in powder X-ray diffraction spectrum; and a pharmaceutical composition containing the crystal polymorphism. The diffraction peak is not substantially shown at 2&thetas;=18.6° ±0.2°, and when the strength of the diffraction peak at 2&thetas;=13.9°±0.2° is Xand the strength of the diffraction peak at 2&thetas;=14.5°±0.2° is X, X/X=5/100-2000/100. The invention also provides a method for producing the &bgr;-crystal polymorphism by mixing a dioxane solution of levonorgestrel with hexane as a deposition solvent.【課題】緊急避妊薬などとして有用なステロイドであるレボノルゲストレルの新規結晶多形、及びその製造方法、並びに該結晶多形を含む医薬組成物の提供。【解決手段】粉末X線回折スペクトルにおいて、回折角度2θが、2θ=13.9°±0.2°,14.5°±0.2°,21.3°±0.2°,24.9°±0.2°及び28.2°±0.2°の角度に回折ピークを有し、2θ=18.6°±0.2°の角度に回折ピークを実質的に示さず、2θ=13.9°±0.2°での回折ピークの強度をX1、2θ=14.5°±0.2°での回折ピークの強度をX2としたとき、X1/X2=5/100~2000/100であるレボノルゲストレルの結晶多形β、並びに該結晶多形を含む医薬組成物。前記結晶多形βを、レボノルゲストレルのジオキサン溶液と析出溶媒としてのヘキサンとを混合する、製造方法。【選択図】なし
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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