氟苯尼考PEG6000固体分散体的无溶剂熔融法制备与分析

摘要

The solvent -free hot -melt method was explored to assess how to enhances the dissolution of hydrophobic drug- florfenicol . The florfenicol （FF） - polyethyleneglyeol 6000 （PEG 6000 ） solid dispersion （SDs） were prepared with PEG 6000 as carriers. The SDs were detected by x - ray diffraction, infrared spectroscopy, electron microscope and dissolution rate. The high performance liquid chromatography （HPLC） method was developed to determine the concent of FF. It was found that the spectra of x - ray diffraction, infrared spectroscopy of the SDs were significant different from that of FF and physical mixture. The structure of FF was the crystal lamellar structure, while the structure of SDs was amorphous state. The dissolution rate of SDs was higher than that of FF and physical mixture. Solubility of FF was 3. 441 mg/mL for the formation of SDs. The solubility of FF was increased for the formation of SDs. The method was simple in preparation and easy to spread to the other hydrophobic drugs.%采用无溶剂熔融法，对难溶性药物氟苯尼考的水溶性粉进行了研究。以聚乙二醇6000（PEG6000）为载体，制备氟苯尼考（florfenicol，FF）固体分散体，用X-射线衍射法、红外光谱法、电子显微镜扫描法和溶出速率法对固体分散体进行了表征，比较氟苯尼考原粉、氟苯尼考PEG6000固体分散体、氟苯尼考-PEG6000物理混合物的溶出速率，并用高效液相法测定固体分散体的溶解度。结果显示，氟苯尼考原粉、固体分散体和混合物的X-射线衍射图谱、红外光谱、电镜结果和溶出速率存在明显差异，氟苯尼考原粉是晶体态的片层结构，固体分散体则为无定形态，固体分散体的溶出速率高于氟苯尼考原粉和物理混合物，固体分散体的溶解度达到3．441mg／mL。无溶剂熔融法制备氟苯尼考PEG6000固体分散体可以提高氟苯尼考溶解度，且方法简单，易于推广。