β-环糊精与凝胶型二氧化硅包载冰片性能的比较研究

Comparative study on the loading performance of borneol by β-cyclodextrin and silica gel

关键词:  冰片  β-环糊精  凝胶型二氧化硅  包载能力  效能比较

Key words:  borneol  β-cyclodextrin  silica gel  loading capacity  performance comparison

摘要:

[目的] 研究旨在比较β-环糊精（β-CD，一种常用的药用辅料）和凝胶型二氧化硅SYLOID 244FP两种辅料包载冰片的能力和效能，以期为冰片在中药制剂中的应用提供更多选择。[方法] 采用饱和水溶液法制备β-CD冰片包合物，直接加入法制备SYLOID 244FP冰片复合物。通过傅里叶红外光谱法（FT-IR）、差示扫描量热法（DSC）进行物相表征，气相色谱法测定含量，考察体外溶出速率，并采用加速实验法比较两者稳定性。[结果] β-CD冰片包合物中冰片的平均含量为11.57%，而SYLOID 244FP冰片复合物中冰片的平均含量为46.32%。体外溶出速率方面，SYLOID 244FP冰片复合物最快，其次是β-CD冰片包合物，最后是纯冰片。在温度40 ℃、相对湿度75%的条件下加速实验14 d后，冰片相对含量分别下降至0（纯冰片）、92.88%（β-CD冰片包合物）和1.91%（SYLOID 244FP冰片复合物）。[结论] β-CD和SYLOID 244FP均能较好地包载冰片，但β-CD在提高冰片稳定性方面表现更优，而SYLOID 244FP则具有更高的包封率和更快的体外溶出速率。研究为冰片在中药制剂中的应用提供了更多选择。

Abstract:

[Objective] The study aimed to compare the loading capacity and efficiency of borneol using β-cyclodextrin(β-CD,a common pharmaceutical excipient) and silica gel SYLOID 244FP,to provide more options for the application of borneol in traditional Chinese medicine preparations. [Methods] The β-CD-borneol inclusion complex was prepared using the saturated aqueous solution method,while the SYLOID 244FP-borneol complex was prepared by direct mixing. Phase characterization was performed using Fourier transform infrared spectroscopy(FT-IR) and differential scanning calorimetry(DSC). The content was determined by gas chromatography(GC),and the in vitro dissolution rate was investigated. The stability of the two complexes was compared using an accelerated stability test. [Results] The average borneol content in the β-CD inclusion complex was 11.57%,whereas that in the SYLOID 244FP complex was 46.32%. Regarding the in vitro dissolution rate,the SYLOID 244FP-borneol complex demonstrated the fastest release,followed by the β-CD-borneol inclusion complex,and finally pure borneol. After 14 days of accelerated testing at 40℃ and 75% relative humidity,the relative content of borneol decreased to 0%(pure borneol),92.88%(β-CD-borneol inclusion complex),and 1.91%(SYLOID 244FP-borneol complex),respectively. [Conclusion] Both β-CD and SYLOID 244FP can effectively load borneol. However,β-CD demonstrated superior performance in enhancing the stability of borneol,while SYLOID 244FP exhibited a higher loading capacity and faster in vitro dissolution rate. The study provides valuable insights for selecting appropriate excipients for borneol in traditional Chinese medicine preparations.