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目的 :研究苯丙醇与 β- 环糊精包合作用 ,探讨乙醇和硬脂酸镁对其包合作用的影响 ,为改进苯丙醇药物剂型提供理论基础。方法 :紫外分光光度法测定苯丙醇 / β- 环糊精包合常数及乙醇、硬脂酸镁对其包合常数的影响 ;沉淀法制备包合物 ;1HNMR法验证包合物以及乙醇、硬脂酸镁对包合的影响。结果 :中性条件下 ,苯丙醇 / β- 环糊精的包合常数为 1772M-1(2 5 1nm) ,加入微量乙醇或硬脂酸镁后 ,其包合常数分别降为 791M-1,12 2 5M-1(2 5 1nm) ;增加乙醇和硬脂酸镁浓度后 ,包合常数又分别降为 377M-1、774M-1(2 5 1nm) ;1HNMR图谱显示苯丙醇与 β- 环糊精形成了 1∶1二元包合物 ,乙醇、硬脂酸镁分别与苯丙醇 / β- 环糊精形成了三元包合物。 结论 :β- 环糊精技术可改进苯丙醇药物的剂型 ;乙醇和硬脂酸镁可降低 β 环糊精对苯丙醇的包合作用 ,故制备包合物时不宜用乙醇助溶或添加硬脂酸镁。
OBJECTIVE: To study the inclusion effect of phenylpropanol and β-cyclodextrin to investigate the effect of ethanol and magnesium stearate on the inclusion effect of phenylpropanol and β-cyclodextrin, and to provide a theoretical basis for improving the dosage form of phenylpropanol. METHODS: UV-Vis spectrophotometry was used to determine the inclusion constants of phenylpropyl alcohol / β-cyclodextrin and the influence of ethanol and magnesium stearate on their inclusion constants. The inclusion complex was prepared by precipitation method. The inclusion complex, ethanol, Effect of magnesium stearate on inclusion. Results: Under the neutral condition, the inclusion constant of phenylpropanol / β-cyclodextrin was 1772M-1 (215 nm). The inclusion constants were reduced to 791M-1 , 12 2 5M-1 (215 nm). After increasing the concentrations of ethanol and magnesium stearate, the inclusion constants decreased to 377M-1,774M-1 (215 nm) - cyclodextrin to form a 1: 1 binary inclusion complex. Ethanol and magnesium stearate form ternary inclusion complexes with phenylpropanol / β-cyclodextrin respectively. Conclusion: β-Cyclodextrin can improve the formulation of phenylpropanol. Ethanol and magnesium stearate can reduce inclusion of β-cyclodextrin to phenylpropanol. Therefore, it is not advisable to use ethanol to dissolve or prepare the inclusion compound Add magnesium stearate.