不同水温下恩诺沙星在中华绒螯蟹体内药物代谢动力学

Pharmacokinetics of enrofloxacin in the Chinese mitten-handed crab,Eriocheir sinensis,at three water temperatures

研究不同水温对恩诺沙星(ENR)在中华绒螯蟹血淋巴、肌肉和肝脏组织中的代谢规律和组织分布的影响。在17、23和29℃水温下,以3.0 mg.kg-1剂量单次肌肉注射给药,于给药后1、10 min及0.5、1、2、8、16、24、48、72和168 h取各组织样品,ENR和环丙沙星(CIP)药物含量由高效液相色谱法同时测定。研究结果表明,在3个温度下,血淋巴和肌肉组织中ENR含量瞬时达到峰值,而肝脏中ENR含量则随给药时间,先上升后下降,在各组织中的含量从大到小依次为:血淋巴、肝脏、肌肉。23和29℃水温下,ENR转化率从大到小依次为:肝脏、血淋巴、肌肉;各组织中ENR的转化率与水温呈正相关。药物代谢动力学计算软件3P97分析结果表明:肝脏组织中ENR的代谢规律符合二室开放模型,在17、23和29℃下,吸收半衰期(分别为:1.81、0.97和0.14 h)、消除半衰期(分别为:240.27、60.57和37.59 h)、药时曲线下总面积(分别为:2 148.66、324.17和264.47μg.mL-1.h-1)均与温度呈负相关,而总体消除率与温度呈正相关,分别是0.001 4、0.009 3和0.011 L.kg-1.h-1。

A pharmacokinetic study of enrofloxacin （ENR） following a single intramuscular administration （ 3.0 mg · kg ^-1 ） was carried out in the Chinese mitten-handed crab at 17, 23 and 29 ℃water temperatures. Hemolymph, muscle and liver samples were collected at 1, 10 min and 0. 5, 1, 2, 8, 16, 24, 48, 72 and 168 h post-injection. The tissue level of ENR and ciprofloxacin （CIP） were simultaneously determined by high-performance liquid chromatography method. The ENR level in hemolymph and musule reached maximum momentarily, while those in liver appeared to be a maximum then declined. The data were analyzed with Practical Pharmacokinetics Program （ 3P97 ）. The kinetic profile of ENR in liver was conformed to a two-compartment model. At 17, 23 and 29 ℃, the absorption half-life （ 1.81, 0. 97 and 0. 14 h, respectively）, elimination half-life （240. 27, 60. 57 and 37. 59 h, respectively） and the area under the concentration-time curve from zero to infinity （2 148. 66, 324. 17 and 264.47 μg · mL^-1· h^-1 , respectively） of ENR in liver was found to have a negative relationship with temperature. Whereas total body clearance had a positive relationship with temperature, and were 0. 001 4, 0. 009 3 and 0. 011 0 L · kg^-1 · h^-1, respectively.