氟苯尼考-羟丙基-β-环糊精包合物的研制

Preparation and Identification of Florfenicol-hydroxypropyl-β-cyclodextrin

为了提高氟苯尼考在水中的溶解度,探讨氟苯尼考包合物批量生产工艺,采用胶体磨和喷雾干燥技术制备氟苯尼考-羟丙基-β-环糊精包合物,并用正交试验法优化工艺参数,以包合率和得率为判断指标,得到包合物的最佳条件为氟苯尼考与羟丙基-β-环糊精摩尔投料比是1∶1,包合时间为1h,氟苯尼考在整个溶液体系中的药物浓度为6mg/mL。所得包合物经红外光谱法、差示扫描量热分析法进行分析鉴定,表明氟苯尼考与羟丙基-β-环糊精形成了包合物,其包合率可达到83.74%,得率达98.48%,氟苯尼考溶解度由原来的1.25 mg/mL提高到了40.76mg/mL。表明该工艺能够用于氟苯尼考-羟丙基-β-环糊精包合物的批量制备。

Florfenicol-hydroxypropyl-β-cyclodextrin was prepared by colloid mill technique using orthogonal experiment technology to improve its solubility. The inclusion rate and getting ratio of the complex were taken as indexes to analyze the effect. The optimum preparation procedure was the proportion of 1：1 for HP-β-CD to florfenicol, the concentration was 6 mg/mL and the time was 1 h. Its structure was proved by DSC and IR, which suggested that the florfenicol was wrapped by HP-β-CD. The inclusion rate was 83.74% and the getting ratio was 98.48%. The solubility of florfenicol was increased from 1.25 mg/mL to 40.76 mg/mL.Thus, it showed that the process was suitable for batch preparation of florfenicol-hydroxypropyl-β-cyclodextrin inclusion complex.