发明名称 阿考替胺水合物晶型及其制备方法和用途
摘要 本发明属于医药技术领域,具体涉及阿考替胺盐酸盐水合物晶型及其制备方法,本发明得到的阿考替胺盐酸盐,含有三水化合物,具有的优点:化学纯度99.9%,最大杂质小于1‰,光学纯度高达99.95%ee;稳定性好。本发明还涉及使用这种水合物的组合物制造治疗胃容纳障碍病症的药物中的应用。
申请公布号 CN104447612A 申请公布日期 2015.03.25
申请号 CN201310419735.3 申请日期 2013.09.16
申请人 天津市汉康医药生物技术有限公司 发明人 严洁;李轩
分类号 C07D277/56(2006.01)I;A61K31/426(2006.01)I;A61P1/14(2006.01)I 主分类号 C07D277/56(2006.01)I
代理机构 代理人
主权项 式1所示阿考替胺盐酸盐三水化合物晶型,<img file="2013104197353100001dest_path_image001.GIF" wi="359" he="133" />(1)用卡尔费休法测定,所述三水化合物的晶型含有8.90%—9.06%(重量百分比) 的水分;所述阿考替胺盐酸盐三水化合物的晶型,用CuKa射线作为特征X射线粉末测定中,其图谱具有下列2θ衍射角和d值,<tables num="0001" id="ctbl0001"><table><tgroup cols="4"><colspec colname="c001" colwidth="24%" /><colspec colname="c002" colwidth="25%" /><colspec colname="c003" colwidth="25%" /><colspec colname="c004" colwidth="24%" /><tbody><row><entry morerows="1">谱线号</entry><entry morerows="1">2θ角(°)实测值</entry><entry morerows="1">d(Å)实测值</entry><entry morerows="1">I/I<sub>0</sub></entry></row><row><entry morerows="1">1</entry><entry morerows="1">5.500</entry><entry morerows="1">23.5213</entry><entry morerows="1">56</entry></row><row><entry morerows="1">2</entry><entry morerows="1">7.880</entry><entry morerows="1">11.9310</entry><entry morerows="1">89</entry></row><row><entry morerows="1">3</entry><entry morerows="1">9.230</entry><entry morerows="1">9.7741</entry><entry morerows="1">53</entry></row><row><entry morerows="1">4</entry><entry morerows="1">11.600</entry><entry morerows="1">9.6315</entry><entry morerows="1">19</entry></row><row><entry morerows="1">5</entry><entry morerows="1">12.510</entry><entry morerows="1">8.5214</entry><entry morerows="1">48</entry></row><row><entry morerows="1">6</entry><entry morerows="1">13.920</entry><entry morerows="1">7.8414</entry><entry morerows="1">8</entry></row><row><entry morerows="1">7</entry><entry morerows="1">14.520</entry><entry morerows="1">7.6125</entry><entry morerows="1">100</entry></row><row><entry morerows="1">8</entry><entry morerows="1">14.810</entry><entry morerows="1">6.5727</entry><entry morerows="1">18</entry></row><row><entry morerows="1">9</entry><entry morerows="1">15.720</entry><entry morerows="1">6.3515</entry><entry morerows="1">9</entry></row><row><entry morerows="1">10</entry><entry morerows="1">16.410</entry><entry morerows="1">5.8928</entry><entry morerows="1">9</entry></row><row><entry morerows="1">11</entry><entry morerows="1">16.790</entry><entry morerows="1">5.0447</entry><entry morerows="1">9</entry></row><row><entry morerows="1">12</entry><entry morerows="1">17.190</entry><entry morerows="1">4.8863</entry><entry morerows="1">2</entry></row><row><entry morerows="1">13</entry><entry morerows="1">18.520</entry><entry morerows="1">4.6471</entry><entry morerows="1">28</entry></row><row><entry morerows="1">14</entry><entry morerows="1">19.550</entry><entry morerows="1">4.3545</entry><entry morerows="1">1</entry></row><row><entry morerows="1">15</entry><entry morerows="1">20.120</entry><entry morerows="1">4.3225</entry><entry morerows="1">4</entry></row><row><entry morerows="1">16</entry><entry morerows="1">20.440</entry><entry morerows="1">3.9124</entry><entry morerows="1">3</entry></row><row><entry morerows="1">17</entry><entry morerows="1">21.420</entry><entry morerows="1">3.5415</entry><entry morerows="1">22</entry></row><row><entry morerows="1">18</entry><entry morerows="1">22.540</entry><entry morerows="1">3.2101</entry><entry morerows="1">25</entry></row></tbody></tgroup></table></tables>2θ 衍射角的误差为±0.2。
地址 300409 天津市北辰区北辰科技园区华实道88号