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Combination formulation of two antiviral compounds
专利权人:
GILEAD PHARMASSET LLC
发明人:
Chal, Ben,Mogalian, Erik,Zia, Vahid,Oliyai, Reza,Pakdaman, Rowchanak,Stefanidis, Dimitrios
申请号:
NZ72917214
公开号:
NZ729172A
申请日:
2014.01.30
申请国别(地区):
NZ
年份:
2018
代理人:
摘要:
Disclosed is the use of ledipasvir and sofosbuvir in the manufacture of a medicament for the treatment of hepatitis C virus infection in a patient, wherein the medicament is in the form of a fixed dose combination tablet comprising: a) from about 10% to about 25% w/w of a solid dispersion comprising ledipasvir dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of ledipasvir to copovidone in the solid dispersion is about 1:1 and wherein the ledipasvir is substantially amorphous; b) from about 35% to about 45% w/w of sofosbuvir, wherein sofosbuvir is substantially crystalline with XRPD 2theta-reflections (° ± 0.20) at: 6.1, 12.7 and 20.8; c) from about 5.0% to about 25% w/w of lactose monohydrate; d) from about 5.0% to about 25% w/w of microcrystalline cellulose; e) from about 1.0% to about 10% w/w of croscarmellose sodium; from about 0.5% to about 3% w/w of colloidal silicon dioxide; and g) from about 0.1% to about 3% w/w of magnesium stearate. In a preferred embodiment the fixed dose combination tablet comprises about 180 mg of a solid dispersion comprising ledipasvir dispersed within a polymer matrix formed by copovidone and about 400 mg of sofosbuvir; or else about 90 mg of a solid dispersion comprising ledipasvir dispersed within a polymer matrix formed by copovidone, and about 400 mg of sofosbuvir. The fixed dose combination tablet preferably further comprises a film coating.
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中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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