pH敏感型盐酸左氧氟沙星眼用即型凝胶的制备及其体外释放考察

目的研制具有缓释作用的pH敏感型盐酸左氧氟沙星眼用即型凝胶。方法以卡波普为凝胶基质,以羟丙甲基纤维素为增稠剂,以溶液的粘度、即型凝胶形成能力及盐酸左氧氟沙星含量为评价指标,确定制备处方和工艺,并以优选处方进行体外释放考察。结果经实验,其优选处方为盐酸左氧氟沙星0.1 g,羟丙甲基纤维素E 50 LV 2.0 g,卡波普9 400.3g,磷酸氢二钠0.35 g,磷酸二氢钠0.45 g,氯化钠0.50 g,尼泊金乙酯0.03 g,加水共制成100 ml。体外释放结果显示其释药平缓,具有较好的缓释特征。结论优选处方工艺稳定,质量控制方法可靠,适用于pH敏感型盐酸左氧氟沙星眼用即型凝胶的制备和评价。

Preparation and in vitro release of pH-triggered levofloxacin hydrochloride in-situ forming gel for sustained ophthalmic delivery

Objective To develop the pH-triggered levofloxacin hydrochloride in-situ forming eye gel.Methods The gel was formed carpool as gel base and hydroxypropyl methylcellulose(HPMC) as thickening agents,and was the foluma evaluated according to the viscosity,the in-situ gelling capacity and the content of levofloxacin hydrochloride.Results The optimized formulation was made by dissolving levofloxacin hydrochloride 0.1 g,HPMC E50LV 2.0 g,carbopol 0.3 g,Na2HPO4 0.35 g,NaH2PO4 0.45 g,NaCl 0.50 g,and ethylparaben 0.03 g in 100 ml water.The gels showed good sustained release characteristics in vitro.Conclusion The optimized formulation has a good reproducibility and can be used for preparation of pH-triggered levofloxacin hydrochloride in-situ forming eye gel.