摘要
目的研究利复星联合卡波姆凝胶对家兔体外抗结核的安全性.方法采用HPLC法测定血清中利复星浓度,在体外检测MIC、MBC、时间-杀菌及耐药梯度.测定利复星凝胶的最小抑菌、杀菌浓度及家兔经支气管介入的安全性.结果 8例肺结核患者血药峰浓度于1.22 h达4.52±0.72 mg·L-1,分别1次给药24 h后,最低血药浓度为0.52±0.26 mg·L-1,表观分布容积V/FC为77.48±8.33 mg·L-1.该药MIC、MBC值分别为0.5 、1.0 mg·L-1,耐药梯度范围0.5～48 mg·L-1.利复星凝胶对H37RV标准株、牛型结核分枝杆菌、草分枝杆菌的MIC值分别为0.1、0.1、0.4 mg·L-1,MBC值分别为0.2、0.2、1.6 mg·L-1;与利复星单体的MIC、MBC比较无显著差异.结论耐药肺结核患者服用利复星24 h,其体内血药浓度维持在最低杀菌浓度MBC之上,介入治疗用药浓度应在48 mg·L-1以上.
OBJECTIVE To observe activity of Levofloxacin - methane sulfonic acid （LfxMSA） in vitro against mycobacterium tuberculosis and its safety in bronchial interventional therapy. METHODS The MIC and MBC of LfxMSA and LfxMSA gel were measured by handwork and instrumental methods, the safety of LfxMSA was assessed by bronchial interventional therapy using rabbits. RESULTS The peak concentration in serum of LfxMSA in 8 patients reached to 4.52 ＋ 0.72 mg·L^-1 in 1.22 hours, and the minimal concentration in serum of LfxMSA after given a single dose was 0.52±0.26 mg·L^-1. The apparent volume of distribution was 77.48± 8.33 mg·L^-1. The value of MIC and MBC were 0.5 mg·L^-1 and 1.0mg·L^-1 The range of drug resistance gradient was 0.5mg·L^-1 to 48mg·L^-1. The MIC of LfxMSA to tuberculo H37RV, boris and phlei was 0.1, 0.1 and 0.4 mg·L^-1 with MBC of 0.2, 0.2,1.6mg·L^-1, respeetively. The MIC and MBC of LfxMSA gel and LfxMSA had no significant difference. Rabbit experiment did not show any haruful effect. CONCLUSION The dosage and internal time of LfxMSA inpatients with pulmonary tuberculosis would be controlled, the concentration of LfxMSA in serum around 24 hours would be maintained above the minimal concentration of bactericide, and the dosage of LfxMSA in interventioal therapy would be above 48mg·L^-1.
出处
《华西药学杂志》
CAS
CSCD
北大核心
2005年第4期305-308,共4页
West China Journal of Pharmaceutical Sciences
基金
全军十五规划课题资助项目(No.01MA217)
关键词
利复星
药效学
卡波姆凝胶
抗结核药
介入
Levofloxacin - methane sulfonic acid
Pharmacodynamics
Antituberculosis drugs
Intervention
Carboxypolmethylene gel
