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POLYCRYSTALLINE MESYLATE OF PHOSPHODIESTERASE TYPE 5 INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

机译:5型磷酸酯酶抑制剂的多羟甲基甲磺酸盐,其制备方法及其应用

摘要

The present invention discloses a methanesulfonate polymorph of a 5-type phosphodiesterase inhibitor. The structure of the 5-type phosphodiesterase inhibitor is as shown in formula A:;The methanesulfonate polymorph of the 5-type phosphodiesterase inhibitor includes the following diffraction peaks measured at 2θ reflection angles in an X-ray powder diffraction pattern: 7.1750°±0.2°, 7.6299°±0.2°, 8.8588°±0.2°, 13.2310°±0.2°, 14.3754°±0.2°, 14.8440±0.2°, 15.2941°±0.2°, 17.1838°±0.2°, 20.0314°±0.2°, 20.8507°±0.2°, 21.2839°±0.2°, 21.7890°±0.2°, 22.2594°±0.2°, 23.0373±0.2°, 25.1243°±0.2°, 25.4244°±0.2°, 26.1530°±0.2°, 28.1210°±0.2°, 30.0135°±0.2°, 31.4809° ±0.2°, 32.3619°±0.2°, 37.2410°±0.2°, 37.6388°±0.2° and 40.8286°±0.2°. The methanesulfonate of the 5-type phosphodiesterase inhibitor not only improves the activity of drugs, but also improves the water solubility and the bioavailability of the drugs, and makes up the blank of studies on drugs of the crystal form.
机译:本发明公开了一种5-型磷酸二酯酶抑制剂的甲磺酸盐多晶型物。 5型磷酸二酯酶抑制剂的结构如式A所示: <图像文件=“ IMGA0001.GIF” he =“ 50” imgContent =“ chem” imgFormat =“ GIF” wi =“ 51” /> ; 5的甲磺酸盐多晶型物型磷酸二酯酶抑制剂在X射线粉末衍射图中以2 <θ>反射角测得的衍射峰如下:7.1750°±0.2°,7.6299°±0.2°,8.8588°±0.2°,13.2310 °±0.2°,14.3754°±0.2°,14.8440±0.2°,15.2941°±0.2°,17.1838°±0.2°,20.0314°±0.2°,20.8507°±0.2°,21.2839°±0.2°,21.7890°±0.2 °,22.2594°±0.2°,23.0373±0.2°,25.1243°±0.2°,25.4244°±0.2°,26.1530°±0.2°,28.1210°±0.2°,30.0135°±0.2°,31.4809°±0.2°,32.3619 °±0.2°,37.2410°±0.2°,37.6388°±0.2°和40.8286°±0.2°。 5型磷酸二酯酶抑制剂的甲磺酸盐不仅提高了药物的活性,而且还提高了药物的水溶性和生物利用度,弥补了晶体药物研究的空白。

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