可吸收聚乳酸-替硝唑抗菌缓释剂体外药物释放效果的测定  

Dynamic Release of Tinidazole from the Degradable PLLA-tinidazole Blend Gel

作　　者：刘娟[1] 肖丽英[1] 李伟[1] 丁一[1] 张萍[1] 袁明龙[2] 

机构地区：[1]口腔生物医学工程教育部重点实验室 [2]四川琢新生物材料研究所,四川成都610041

出　　处：《华西口腔医学杂志》2005年第3期237-239,共3页West China Journal of Stomatology

基　　金：教育部留学回国人员科研启动基金资助项目(0040305402005)

摘　　要：目的用高效液相色谱法(HPLC)测定可吸收聚乳酸-替硝唑抗菌缓释剂中替硝唑的体外释放动力学,以观察聚乳酸-替硝唑共混缓释剂在作为抗牙周炎治疗剂时的药物持续释放时间和有效释放浓度。方法采用C18色谱柱分离,以水-甲醇-冰醋酸为流动相,流速为1.5ml min,测试波长为310nm,柱温为30℃,测定可吸收聚乳酸-替硝唑抗菌缓释剂中替硝唑的持续释放时间和有效释放浓度。结果①替硝唑的保留时间约为12min。②混合凝胶中替硝唑的浓度与峰面积呈良好的线性关系,方程:y=0.836+8.4522×10_5x(r=0.9986),线性范围为5～500mg L,相对标准差为0.2%。③聚乳酸对替硝唑的测定无干扰。替硝唑平均每日释放度为5.60%,14d累计释放度约为78.40%。结论聚乳酸-替硝唑共混缓释剂具有较长时间保持有效抑菌浓度的药物释放能力;HPLC是评价局部药物释放剂简便、准确和具有良好重复性的有效方法。Objective To determine the dynamic release of tinidazole from the degradable poly_lactic acid (PLLA)_tinidazole blend gel (a periodontal local drug delivery) by high_performance liquid chromatography (HPLC) in vitro and to observe the poly_lactic acid (as a vector of tinidazole) how to affect the release of tinidazole. Methods HPLC analysis was conducted. The operating conditions were C-{18}_ODS_A column, water_methanol_acetic acid as mobile phase at a flow rate of 1.5 ml/min and a detection wavelength at 310 nm and a column temperature at 30 ℃. Results ①The retention time of tinidazole was about 12 min. ②There was good linear relationship between the concentrations of tinidazole in blend gel and their peak areas in the ranges of 5～500 mg/L. The regression reaction was y=0.836+8.452 2×10~{-5}x (r=0.998 6). RSD was 0.2%. ③Polylactic acid had no influence on the determination of tinidazole. The daily average release of tinidazole was 5.60%.The cumulative release of tinidazole was about 78.40% in 14 days.Conclusion The in vitro drug release analysis is an useful method in evaluating the performance of local drug delivery system. HPLC analysis is a simple and accurate method with good reproducibility.

关 键 词：高效液相色谱法 聚乳酸 替硝唑 

分 类 号：R781.4[医药卫生—口腔医学]