硅氧烷自组装膜引导那格列奈多晶型的研究-生物化工专业论文.docxVIP

摘要本文以糖尿病治疗药物那格列奈(Nateglinide)为对象，研究自组装膜 摘要 本文以糖尿病治疗药物那格列奈(Nateglinide)为对象，研究自组装膜 (SAMs)技术对其多晶型的调节作用。 首先针对那格列奈分子中特定结构，选用三种不同类型的硅氧烷试剂，分别 是氨丙基三甲氧基硅烷(NH2CH2(CH2)2Si(OCH3)3)、3一(苯基氨基)丙基三甲 氧基硅烷(C6HsNH(CH2)3Si(OCH3)3)、11．溴十一烷基三甲氧基硅烷 (BrCH2(CH2)loSi(OCH3)3)，在玻璃基底上进行自组装膜的实验制备与表征。 利用硅氧烷SAMs引导那格列奈结晶实验中，通过调节结晶过程中过饱和度 及降温速率条件，借助X．射线粉末衍射表征及熔点测定结果，分析得到比较全 呵， 面的晶型分布信息，对比总结不同类型硅氧烷白组装膜对那格列奈晶型调控规 律，主要结论如下： l、硅氧烷SAMs能对那格列奈的晶型产生调节作用，促使那格列奈分子形成热力 学更稳定的晶型，在SAMs上得到了同条件下溶液中难以获得的单一的B、S 晶型，还有X2晶型，其中S晶型最稳定，并确定了生成各晶型的最佳反应条件。 2、烷烃类的SAMs-Si-(CH2)3-NH2和SAMs．＆．(CH9，J坷，．能够诱导热力学最稳定的 S晶型的产生，芳香族的SAMs—Si-(CH2)3．脚矗能够诱导那格列奈较稳定的H 晶型的生成，而不能诱导产生S晶型。 3、长链的SAMs一＆．(CH2)，，研比短链的SAMs．研．(CH2)3-NH2对S晶型的诱导更有 效，能够诱导产生单一的S晶型晶体。 关键词： 硅氧烷自组装膜： 那格列奈； 多晶型 ABSTRACTEffects ABSTRACT Effects of Self-assembled Monolayers on adjusting polymorphic crystals of diabetes treatment drug—nateglinide were studied in this thesis． Firstly，according to the structure of nateglinide，three different kinds of siloxane agents including NH2CH2(CH2)2Si(OCH3)3， C6HsNH(CH2)3Si(OCH3)3， and BrCH2(CH2)IoSi(OCH3)3，were selected to form SAMs on the surfaces of glass slides and the SAMs were characterized． Effects of supersaturation degree and cooling rate were considered in nateglinide crystallizing experiment，and the crystal forms were analyzed by X·ray diffraction and melting point measure．Major conclusions were obtained as below： l、Siloxane SAMs did affect nateglinide crystallization，pure stable forms B and S were observed to form on SAMs，which couldn’t be obtained from liquid at the same condition．And the optimal reaction conditions for the crystal form X2 and S were determined． 2、Different kinds of SAMs can cause different effects：S form nateglinide were observed on two alkanes SAMs．SAMs一＆-(CH2)3-NH2 and SAMs-Si-(CHe)11-B巧 while it could not appear on aromatic SAMs-Si-(CH2)3-NH-ph in whatever reaction condition．But SAMs—si一(CH2)3-NH—ph could lead H form growing on it． 3、The growth of S form nateglinide on long hydrocarbon chain alkanes SA