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Inclusion Complex of Theophylline with β−Cyclodextrin: Influence of Method of Preparation ud

机译:茶碱与β-环糊精的包合物:制备方法的影响

摘要

Inclusion complexes of Theophylline (THP) with β-cyclodextrin (β−CD) were prepared in order to improve the solubility and bioavailability of the poorly water soluble drug. Solution phase interaction was studied by UV-Vis and Fluorescence techniques. The linear Benesi– Hildebrand plot indicated the formation of only one type of complex with a host-guest composition of 1:1 in the solution. The effect of method of preparation of the THP-β−CD inclusion complexes (ICs) was investigated. The ICs were prepared by the conventional methods of physical mixing (PM), kneading (KN), co-precipitation (CP) and freeze drying (FD) and also by the novel approach of microwave irradiation method (MW). The solid inclusion complexes were characterized by various spectroscopic techniques such as FTIR, XRD, DSC, SEM and 1H NMR. The characterization techniques indicated the formation of true inclusion complexes in case of CP, FD and MW. The in vitro dissolution rate of THP was considerably enhanced when the inclusion complexes were employed. Therefore, the bioavailability of THP can be improved significantly by forming inclusion complexes with cyclodextrin.
机译:制备茶碱(THP)与β-环糊精(β-CD)的包合物,以提高水溶性差的药物的溶解度和生物利用度。通过UV-Vis和荧光技术研究了溶液相的相互作用。 Benesi–Hildebrand线性图表明溶液中只有一种客体组成为1:1的复合物形成。研究了THP-β-CD包合物的制备方法的效果。通过物理混合(PM),捏合(KN),共沉淀(CP)和冷冻干燥(FD)的常规方法以及新型的微波辐照方法(MW)制备IC。通过各种光谱技术,例如FTIR,XRD,DSC,SEM和1H NMR,对固体包合物进行了表征。表征技术表明在CP,FD和MW情况下会形成真正的包合物。当使用包合物时,THP的体外溶出速率大大提高。因此,通过与环糊精形成包合物,可以显着提高THP的生物利用度。

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    Behera Anam;

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  • 年度 2015
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