左氧氟沙星热敏型耳用凝胶的制备及其性能检测

Preparation of levofloxacin thermosensitive otic gel and its characteristic property test analysis

目的制备左氧氟沙星热敏型耳用凝胶,并对其体外释放性能进行检测。方法制备以泊洛沙姆407为基质的左氧氟沙星热敏性耳用凝胶,根据中耳温度筛选泊洛沙姆407的最佳处方浓度,采用立式Franz扩散池模型对该制剂的体外释放性能进行研究。结果左氧氟沙星检测浓度的线性范围为3.0～10.5mg/L,在此浓度范围内吸光度(A)和浓度(C)呈良好的线性关系,即C(mg/L)=12.582A+0.2976(r=0.9986,n=6);平均回收率为100.09%,相对标准偏差(RSD)=0.61%(n=6);泊洛沙姆407在处方中的最佳浓度为17%;药物释放具有一定的控释性,释放符合零级动力学特征。结论该耳用热敏型凝胶具有较好的控释性能,且制备方法简单,用药剂量易于控制。

Objective To prepare the levofloxacin（LEF） thermosensitive gel for otitis drug delivery, and to detect the characteristic properties of the drug release in vitro. Methods Poloxamer 407 was studied as themosensitive material for the LEF ear drop. The best prescription concentration of poloxamer was selected according to the temperature of gel. The Franz vertical diffusion cell method was used to study the drug release. Results The detected concentration of LEF was in the linear range of 3.0 - 10.5 mg/L, and in this range the concentration（C） had a well linear relationship with absorbance （A）： C （mg/L） = 12.582A ＋0.2976（r =0.9986,n =6）. The average rate of recovery was 100.09% and the relative standard deviation （RSD） = 0.61% （n = 6）. The best concentration of poloxamer in prescription was 17%. The drug possessed the characteristic properties of controlled release, and the release followed zero-order kinetics. Conclusions Levoflocacin thermosensitive otic gel possessed the characteristic properties of controlled release, and the preparation was simple in method and easy to control in dosage.