发明名称 一种结晶型恩替卡韦
摘要 本发明涉及一种新的结晶型恩替卡韦及该结晶型恩替卡韦的制备方法,所述新的结晶型恩替卡韦的X射线粉末衍射图在2θ=16.435°(d=5.38925),2θ=19.704°(d=4.50199),2θ=25.376°(d=3.50703)处有较强的衍射峰,差热分析图谱上,在79.1℃开始出现一个脱水吸热熔融峰,在140.1℃出现一个吸热熔融峰,在244.6℃左右出现一个尖锐的吸热熔融峰,到299.2℃左右时,样品开始溶解。本发明所述结晶型恩替卡韦较恩替卡韦一水合物结晶制成制剂时,具有更好的溶出度,晶型具有相对更好稳定性。
申请公布号 CN103304566B 申请公布日期 2015.11.04
申请号 CN201310286506.9 申请日期 2013.07.09
申请人 北京凯因科技股份有限公司 发明人 李鹏;杨健
分类号 C07D473/18(2006.01)I;A61K31/522(2006.01)I;A61P31/20(2006.01)I 主分类号 C07D473/18(2006.01)I
代理机构 代理人
主权项 恩替卡韦,其特征在于,所述恩替卡韦为结合了3分子DMF的恩替卡韦,其铜靶X射线粉末晶体衍射具有以下特征的吸收峰:<tables num="0001" id="ctbl0001"><table><tgroup cols="3"><colspec colname="c001" colwidth="25%" /><colspec colname="c002" colwidth="43%" /><colspec colname="c003" colwidth="32%" /><tbody><row><entry morerows="1">峰号</entry><entry morerows="1">衍射角2θ(°)</entry><entry morerows="1">晶面距d</entry></row><row><entry morerows="1">1</entry><entry morerows="1">9.856</entry><entry morerows="1">8.96714</entry></row><row><entry morerows="1">2</entry><entry morerows="1">10.066</entry><entry morerows="1">8.78058</entry></row><row><entry morerows="1">3</entry><entry morerows="1">11.275</entry><entry morerows="1">7.84132</entry></row><row><entry morerows="1">4</entry><entry morerows="1">11.868</entry><entry morerows="1">7.45084</entry></row><row><entry morerows="1">5</entry><entry morerows="1">14.284</entry><entry morerows="1">6.19550</entry></row><row><entry morerows="1">6</entry><entry morerows="1">14.443</entry><entry morerows="1">6.12763</entry></row><row><entry morerows="1">7</entry><entry morerows="1">16.435</entry><entry morerows="1">5.38925</entry></row><row><entry morerows="1">8</entry><entry morerows="1">17.476</entry><entry morerows="1">5.07053</entry></row><row><entry morerows="1">9</entry><entry morerows="1">17.730</entry><entry morerows="1">4.99838</entry></row><row><entry morerows="1">10</entry><entry morerows="1">18.182</entry><entry morerows="1">4.87516</entry></row><row><entry morerows="1">11</entry><entry morerows="1">18.792</entry><entry morerows="1">4.71831</entry></row><row><entry morerows="1">12</entry><entry morerows="1">19.154</entry><entry morerows="1">4.62987</entry></row><row><entry morerows="1">13</entry><entry morerows="1">19.704</entry><entry morerows="1">4.50199</entry></row><row><entry morerows="1">14</entry><entry morerows="1">21.251</entry><entry morerows="1">4.17753</entry></row><row><entry morerows="1">15</entry><entry morerows="1">21.793</entry><entry morerows="1">4.07499</entry></row><row><entry morerows="1">16</entry><entry morerows="1">23.983</entry><entry morerows="1">3.70757</entry></row><row><entry morerows="1">17</entry><entry morerows="1">24.380</entry><entry morerows="1">3.64810</entry></row><row><entry morerows="1">18</entry><entry morerows="1">25.376</entry><entry morerows="1">3.50703</entry></row><row><entry morerows="1">19</entry><entry morerows="1">25.676</entry><entry morerows="1">3.46684</entry></row><row><entry morerows="1">20</entry><entry morerows="1">26.595</entry><entry morerows="1">3.34897</entry></row><row><entry morerows="1">21</entry><entry morerows="1">27.541</entry><entry morerows="1">3.23609</entry></row><row><entry morerows="1">22</entry><entry morerows="1">28.815</entry><entry morerows="1">3.09571</entry></row><row><entry morerows="1">23</entry><entry morerows="1">29.212</entry><entry morerows="1">3.05468</entry></row><row><entry morerows="1">24</entry><entry morerows="1">30.008</entry><entry morerows="1">2.97548</entry></row><row><entry morerows="1">25</entry><entry morerows="1">30.942</entry><entry morerows="1">2.88770</entry></row><row><entry morerows="1">26</entry><entry morerows="1">31.268</entry><entry morerows="1">2.85834</entry></row><row><entry morerows="1">27</entry><entry morerows="1">31.857</entry><entry morerows="1">2.80686</entry></row><row><entry morerows="1">28</entry><entry morerows="1">32.290</entry><entry morerows="1">2.77018</entry></row><row><entry morerows="1">29</entry><entry morerows="1">33.341</entry><entry morerows="1">2.68521</entry></row><row><entry morerows="1">30</entry><entry morerows="1">34.210</entry><entry morerows="1">2.61895</entry></row><row><entry morerows="1">31</entry><entry morerows="1">34.509</entry><entry morerows="1">2.59696</entry></row></tbody></tgroup></table></tables>。
地址 100176 北京市大兴区亦庄经济技术开发区荣京东街6号