甲氧苄啶在家蚕体内的药代动力学研究  

A Study on Pharmacokinetics of Trimethoprim Inside Silkworm Body

作　　者：孙波[1] 周洪英[1] 吴洪丽[1] 叶建美[1] 许淑琼[1] 

机构地区：[1]湖北省农业科学院经济作物研究所,武汉430064

出　　处：《蚕业科学》2014年第1期59-63,共5页ACTA SERICOLOGICA SINICA

摘　　要：甲氧苄啶是广谱类抗菌药物，研究其用于防治家蚕细菌病在蚕体内的药物代谢动力学特征，为制定合理的给药方案提供依据。家蚕5龄第5天幼虫以22μg／g剂量给药后，于不同时间点采集蚕体血浆样品进行固相萃取预处理，采用高效液相色谱（HPLC）法测定血浆中的甲氧苄啶浓度，并用DAS3．0．1软件做药代动力学分析。方法学验证结果表明，采用固相萃取-HPLC法测定蚕体血浆中的甲氧苄啶浓度，其精密度、准确度和回收率均在规定范围内，血浆中甲氧苄啶的质量浓度在0．63—40．00μg／mL范围内，峰面积与药物浓度呈现良好的线性关系。甲氧苄啶在家蚕体内的药代动力学参数为：AUC（0-t）=414．81mg／L·h-1，Tmax=24h，Cmax=17．36mg／L，T1／2=8．53h，MRT（0-t）=19．77h。研究结果提示：甲氧苄啶在蚕体内的吸收、代谢良好，可在蚕体内维持较长时间的抑菌效果。Trimethoprim is a broad-spectrum antibiotic agent. In order to provide a theoretical basis for design of reasonable dosage regimen to control silkworm （Bombyx mori） bacterial diseases, pharmacokinetic properties of trimethoprim inside silkworm body was studied. After administration of 22 μg/g trimethoprim to day 5 silkworm larvae of the 5th instar, blood samples were collected at different time points. After being pre-treated by solid-phase extraction, concentration of trimethoprim in plasma was determined by high performance liquid chromatography （HPLC）. Pharmacokinetic analysis was conducted with DAS 3.0.1 software. The above analyses demonstrated that the precision, accuracy and recovery rate of solid-phase extraction-HPLC determination method were within the set range. Within the range of 0.63-40.00 μg/mL trimethoprim in plasma, the peak area showed good linear relationship with drug concentration. The pharmacokinetic parameters of trimethoprim inside silkworm body were as follows.AUC（0-t） = 414.81 mg/L. h-1, Tmax =24 h, Cr;a; = 17.36 mg/L, T1/2 =8.53 h, MRT（0-t） = 19.77 h. The results indicated that trimethoprim can be absorbed and degraded well in silkworm body and the antibacterial effect of trimethoprim could sustain for a long time.

关 键 词：蚕用药剂 甲氧苄啶 固相萃取 高效液相色谱 血药浓度 药代动力学参数 

分 类 号：R969.1[医药卫生—药理学] S884.4[医药卫生—药学]