盐酸环丙沙星在中华绒螯蟹体内药物代谢动力学研究

PHARMACOKINETICS OF CIPROFLOXACINUM IN CHINESE MITTEN-HANDED CRAB, ERIOCHEIR SINENSIS

  • 摘要: 应用反向高效液相色谱法对盐酸环丙沙星在中华绒螯蟹雄、雌蟹血淋巴与肌肉内的代谢规律进行了研究.肌肉注射给药后血淋巴中盐酸环丙沙星的浓度立即达到峰值,药物开始向肌肉等组织中运转,血药浓度在1h内迅速下降,而肌肉中的浓度达到峰值;此后无论是血淋巴还是肌肉中的盐酸环丙沙星浓度均缓慢下降,到第120h雌、雄蟹中盐酸环丙沙星的浓度均在1μg·mL-1(g-1)以下,到216h均不能检出.研究表明:中华绒螯蟹血淋巴中盐酸环丙沙星的药物浓度可用一级吸收二室开放模型描述,雄、雌蟹的消除半衰期(T1/2β)分别为40.34±1.48h和22.07±0.31h;中华绒螯蟹的性别对盐酸环丙沙星在其体内的代谢有较大的影响.

     

    Abstract: To study the metabolic law of Ciprofloxacinum in Chinese mitten-handed Crab,Eriocheir sinensis,its concentrations both in hemolymph and muscle were measured by using RP-HPLC after intramuscular injection at a dose of 8.17±0.56mg·kg-1and 6.25±0.85mg·kg-1 to male and female crab at the first experiment,or at a dose of 5.99±0.27mg·kg-1 and 6 05±0 32mg·kg-1at the second experiment respectively The concentration of Ciprofloxacinum in the hemolymph was the highest immediately after injection Within an hour,the blood-drug concentration dropped sharply On the other hand,the concentration in the muscle reached maximum an hour after injection and decreased gradually thereafter It was lower than 1μg·mL-1(g-1)at 120h and undetectable at 216h This finding indicated that the injected Ciprofloxacinum moved into muscles via hemolymph in the crab.The concentrations of Ciprofloxacinum in hemolymph were best described by a two-compartment open model with first-order absorption To male and female crab,the pharmacokinetic parameter,T 1/2β,was 40.34±1.48h and 22.07±0.31h respectively Also,Pharmacokinetic difference between male and female crab was observed.

     

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