氟苯尼考β-环糊精包合物的制备与表征研究

Study on Preparation and Characteristics of Florfenicol/β-Cyclodextrin Inclusion Complexes

为提高氟苯尼考的溶解度和生物利用度,制备氟苯尼考β-环糊精包合物。以β-环糊精为包合材料,采用饱和水溶液法制备包合物。包合物用红外分光光度法、相溶解度图法、差热分析法、溶出速率法验证,并计算包合常数,比较了氟苯尼考原料、物理混合物和包合物的溶解度。结果显示,氟苯尼考和β-环糊精包合完全,相溶解度图为AL型,形成了摩尔比为1∶1的包合物,包合常数为298.2 L/mol,在25℃时包合物的溶解度提高了7.63倍,氟苯尼考在50.0～350.0μg/mL浓度范围内吸光度与浓度间线性关系良好。氟苯尼考β-环糊精包合物制备方法简单,可以显著提高药物的溶解度和溶出度。

To improve the solubility and bioavailability of florfenicol,florfenicol/β-cyclodextrin inclusion complex was prepared by saturated aqueous solution method and then validated by infrared spectroscopy,phase solubility diagram,differential thermal analysis and dissolution rate.Furthermore,the stability constant,solubility of florfenicol,physical mixture and inclusion complex were measured;and UV spectrophotometer method was developed to determinate the concentration.The results showed that the florfenicol was included by β-cyclodextrin completely and showed a typical Al-type as the stability constant was 298.2 mol/L at 25℃.The spectra of infrared spectroscopy,differential thermal analysis,and phase solubility diagram pattern of the inclusion complex were remarkably different from the florfenicol and physical mixture.Solubility rate of florfenicol was enhanced by the formation of inclusion complex and increased by 7.63 fold.The calibration curve was linear with correlation coefficient r=0.9999 in the range of 50.0～350.0 μg/mL.The preparation and determination method of inclusion complex was simple and practical as the solubility and dissolution rate was improved significantly.