蒿甲醚/羟丙基-β-环糊精主客体体系：表征、相溶解度及包合模式
Artemether/hydroxypropyl-beta-cyclodextrin host-guest system: characterization, phase-solubility and inclusion mode.
作者信息
Yang Bo, Lin Jun, Chen Yong, Liu Yu
机构信息
School of Chemistry, Key Laboratory of Medicinal Chemistry for Natural Resource (Ministry of Education), Yunnan University, Kunming 650091, PR China.
出版信息
Bioorg Med Chem. 2009 Sep 1;17(17):6311-7. doi: 10.1016/j.bmc.2009.07.060. Epub 2009 Jul 28.
An inclusion complex of the antimalarial artemether (ATM) in hydroxypropyl-beta-cyclodextrin (HPbetaCD) was prepared and characterized. The phase-solubility diagram for the drug showed an increase in water solubility and gave an apparent binding constant of 220 M(-1). According to (1)H NMR and 2D NMR spectroscopy (ROESY), the inclusion mode involves two CH(3) from the drug orientated in the HPbetaCD cavity. The complex was characterized by Powder X-ray diffraction and thermal analysis. In addition, the complex produces a 1.81-fold enhancement in apparent bioavailability compared to artemether.
制备并表征了抗疟药物蒿甲醚（ATM）与羟丙基-β-环糊精（HPβCD）形成的包合物。该药物的相溶解度图显示其水溶性增加，表观结合常数为220 M⁻¹。根据¹H NMR和二维NMR光谱（ROESY），包合模式涉及药物中的两个CH₃定位在HPβCD腔内。通过粉末X射线衍射和热分析对该包合物进行了表征。此外，与蒿甲醚相比，该包合物的表观生物利用度提高了1.81倍。
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