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目的:制备左氧氟沙星骨植入缓释片受试制剂,并进行初步的药理毒理学评价。方法:采用溶剂挥发法制备受试制剂。不同时间点检测植入动物体内的受试制剂中左氧氟沙星释放浓度。进行稳定性试验、溶血性实验和局部刺激性实验。结果:受试制剂质地均匀紧实、表面平整光滑。左氧氟沙星的骨释放量为170.8μg·g-1,血浆浓度为4.43μg·mL-1。高温条件下10 d后受试制剂重量损耗0.369%,左氧氟沙星含量变化率1.558%,高湿条件下10 d后吸湿增重2.071%、左氧氟沙星含量变化率3.738%。受试制剂无溶血反应发生,植入组织局部未见炎性细胞及异型细胞,无局部刺激性。结论:缓释片制备方法可行,体内释放效果能满足4~6周的临床需要,其稳定性好,无局部刺激性。
OBJECTIVE: To prepare the levofloxacin sustained-release preparations for bone implantation and evaluate its pharmacology and toxicology. Methods: The solvent was prepared by evaporation method. The concentration of levofloxacin in the test preparation implanted in animals was measured at different time points. Stability tests, hemolytic experiments and local irritation experiments. Results: The test preparation was uniform and firm, the surface was smooth. Levofloxacin bone release was 170.8μg · g-1, plasma concentration was 4.43μg · mL-1. After 10 days of high temperature, the weight loss of the test preparation was 0.369%, the levofloxacin content was 1.558%, the moisture absorption weight gain was 2.071% after 10 days and the levofloxacin content was 3.738%. There was no hemolytic reaction in the test preparations, no inflammatory cells and abnormal cells were found in the part of the implanted tissue, and no local irritation was found. Conclusion: The preparation method of sustained-release tablets is feasible, the release effect in vivo can meet the clinical needs of 4 to 6 weeks, its stability is good, no local irritation.