羟丙基-β-环糊精对烯丙菊酯的增溶作用及其包合物的表征

Solubilization of hydroxypropyl-β-cyclodextrin on allethrin and properties of their inclusion complex

为了开发水溶性好、运输方便、对环境威胁小的高效拟除虫菊酯的控制释放制剂,研究了羟丙基-β-环糊精(HP-β-CD)对烯丙菊酯的包合作用。通过相溶解度图法研究了HP-β-CD对烯丙菊酯的增溶作用,并用共蒸法制备了烯丙菊酯/HP-β-CD包合物,经差示扫描量热法(DSC)、红外光谱法(IR)、热重分析法(TG)和核磁共振法(NMR)对其结构进行了表征。结果表明:HP-β-CD对烯丙菊酯有明显的增溶作用,相溶解度曲线为线性AL型,烯丙菊酯与HP-β-CD形成了物质的量之比为1∶1的包合物;DSC和TG分析均证明了该包合物的形成,IR和NMR分析显示烯丙菊酯的五元环部分已深入HP-β-CD空腔内部,且重心位于内腔H-5附近。

In order to develop new sustained, friendly environmental and controlled release formulation, an inclusion compound of allethrin with hydroxypropyl-β-cyclodextrin （HP-β-CD） was studied. HP-β-CD solubilizing ailethrin was studied by the way of the phase solubility diagram. Allethrin＇s inclusion complex with HP-β-CD was prepared using the method of coevaporation,and the inclusion complex in solid state was evaluated by differential scanning calorimetry （DSC）, Fouriertransform IR, thermal gravimetric analysis （TG） and NMR. The results showed that its solubility was significantly increased by the complexation of allethrin and HP-β-CD ;The phase solubility diagram with HP-β-CD was classfied as A：type, indicating the formation of 1：1 stoichiometric inclusion complex; The formation of the inclusion complex was demonstrated by the study of DSC, TG, IR and NMR. The configuration of allethrin/HP-β-CD complex showed that the pentagon ring of allethrin entered the cavity of HP-v-CD, and the barycenter of the pentagon ring located around the H-5 of HP-β-CD cavity.