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A NOVEL POLYMORPHIC FORM OF TENOFOVIR PRODRUG AND ITS PREPARATION AS WELL AS THE USE THEREOF
专利权人:
发明人:
CHEN, MING,陈明,陳明,TIAN, CHENGYAO,田承耀,田承耀,ZHAO, MINGLI,赵明礼,趙明禮,YU, JUN,余俊,余俊,YANG, BAOHAI,杨宝海,楊寶海,LU, AIFENG,吕爱锋,呂愛鋒
申请号:
TW104123520
公开号:
TW201623323A
申请日:
2015.07.21
申请国别(地区):
TW
年份:
2016
代理人:
摘要:
The present invention relates to a novel polymorphic form of the compound 9-[(R)-2-[[(S)-[[[1-(isopropoxy-carbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxyl] propyl] adenine fumarate and its preparation as well as the use thereof. In particular, the present invention relates to the novel polymorph of formula (I), 9-[(R)-2-[[(S)-[[[1-(isopropoxy-carbonyl)-1-methyl]ethyl]amino] phenoxyphosphinyl]methoxyl]propyl] adenine fumarate, characterized by an XRPD pattern at least comprising of the diffraction peaks (2θ ± 0.20°): 5.08, 12.44, 13.18, 22.37, 23.37, 28.56. The said polymorphic form has advantages of high bioavailability, significantefficacy, good stability, high yield and high purity, which are helpful to choose and design administration route and determinate the process parameters of pharmaceutical formulation, the form of this invention can improve drug production quality.本發明涉及9-[(R)-2-[[(S)-[[[1-(異丙氧基羰基)-1-甲基]乙基]胺基]苯氧基氧膦基]甲氧基]丙基]腺嘌呤富馬酸鹽新晶型及其製備方法和用途。具體地,本發明涉及式(I)所示9-[(R)-2-[[(S)-[[[1-(異丙氧基羰基)-1-甲基]乙基]胺基]苯氧基氧膦基]甲氧基]丙基]腺嘌呤富馬酸鹽的新晶型,其特徵在於,該晶型XRPD圖譜中至少包含2θ±0.20°為:5.08,12.44,13.18,22.37,23.37,28.56的衍射峰。本發明晶型具有生物利用度高,藥效顯著,穩定性好,收率高,純度高等特點,有助於藥物给藥途徑的選擇與設計,以及藥物製劑工藝參數的確定,從而提高藥品生產質量。
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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