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目的研究α-细辛脑-β-环糊精包合物的制备方法及包合前后α-细辛脑物理性能变化情况。方法采用研磨法制备α-细辛脑-β-环糊精包合物,运用正交试验法优选最佳制备工艺,测定了α-细辛脑及α-细辛脑-β-环糊精包合物的溶解度和溶出度,并比较了二者的X-射线衍射图谱、红外光谱、紫外光谱的变化,以验证包合物的形成。结果最佳制备工艺条件为α-细辛脑与β-环糊精为1:6(m:m),β-环糊精与水为1:1.5(m:V),α-细辛脑与乙醇为1:3(m:V),研磨时间为90 min;α-细辛脑经β-环糊精包合后,溶解度为原药的5.31倍,α-细辛脑及包合物的溶出度参数t50分别为46.2、18.9 min,经红外光谱、紫外光谱、X-射线衍射图谱确证了包合物的形成。结论α-细辛脑被β-环糊精包合后呈现出新的物相特征,为α-细辛脑加工成各种剂型开辟良好的前景。
Objective To study the preparation of α-asarone-β-cyclodextrin inclusion complex and the change of physical properties of α-asarone brain before and after inclusion. Methods The inclusion complex of α-asarone-β-cyclodextrin was prepared by grinding method. The optimal preparation process was optimized by orthogonal test. The effects of α-asarone and α- The solubility and dissolution of the inclusion complex were compared. The X-ray diffraction patterns, infrared spectra and UV spectra of the two complexes were compared to verify the formation of the inclusion complex. Results The optimum preparation conditions were 1: 6 (m: m) for α-asarone and β-cyclodextrin, 1: 1.5 for m- And ethanol for 1: 3 (m: V), grinding time was 90 min; α-Asarone brain β-cyclodextrin inclusion, the solubility of 5.31 times the original drug, α- asarone brain and inclusion complex The dissolution parameters t50 were 46.2 and 18.9 min, respectively. The formation of inclusion complex was confirmed by IR, UV and X-ray diffraction. Conclusions α-asarone is a new phase character after β-cyclodextrin inclusion, which opens up a good prospect for the processing of α-asarone into various dosage forms.