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Toxicokinetics of lambda-cyhalothrin in rats.

机译:氟氯氰菊酯在大鼠中的毒代动力学。

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The toxicokinetics of lambda-cyhalothrin after single 20mgkg(-1) oral and 3mgkg(-1) intravenous doses were studied in rats. Serial blood samples were obtained after oral and intravenous administration. Liver, brain, spinal cord, sciatic nerve, vas deferens, anococcygeus and myenteric plexus tissue samples were also collected. Plasma, liver, hypothalamus, cerebellum, medulla oblongata, frontal cortex, striatum, hippocampus, midbrain, spinal cord, vas deferens, anococcygeus, myenteric plexus and sciatic nerve concentrations of lambda-cyhalothrin were determined by HPLC. The plasma and tissue concentration-time data for lambda-cyhalothrin were found to fit a two-compartment open model. For lambda-cyhalothrin, the elimination half-life (T(1/2beta)) and the mean residence time from plasma were 7.55 and 8.55h after i.v. and 10.27 and 14.43h after oral administration. The total plasma clearance was not influenced by dose concentration or route and reached a value of 0.060lh(-1)kg(-1). After i.v. administration, the apparent volume of distribution and at steady state were 0.68 and 0.53lkg(-1), suggesting a diffusion of the pyrethroid into tissue. After oral administration, lambda-cyhalothrin was extensively but slowly absorbed (T(max), 2.69h). The oral bioavailability was found to be 67.37%. Significant differences in the kinetic parameters between nervous tissues and plasma was observed. The maximum concentrations in hypothalamus (C(max), 24.12mugg(-1)) and myenteric plexus (C(max), 25.12mugg(-1)) were about 1.5 times higher than in plasma (C(max), 15.65mugml(-1)) and 1.3 times higher than in liver (C(max), 18.42mugml(-1)). Nervous tissue accumulation of lambda-cyhalothrin was also reflected by the area under the concentration curve ratios of tissue/plasma (liver). The T(1/2beta) for lambda-cyhalothrin was significantly greater for the nerve tissues, including neuromuscular fibres, (range 12-26 and 15-34h, after i.v. and oral doses) than for plasma (7.55 and 10.27h, respectively).
机译:在大鼠中研究了单次口服20mgkg(-1)和3mgkg(-1)静脉内给药后λ氟氯氰菊酯的毒代动力学。口服和静脉内给药后获得系列血样。还收集了肝,脑,脊髓,坐骨神经,输精管,无囊球菌和肌丛神经组织样品。用高效液相色谱法测定血浆,肝脏,下丘脑,小脑,延髓,额叶皮层,纹状体,海马,中脑,脊髓,输精管,无球藻,肌间神经丛和坐骨神经的氟氯氰菊酯浓度。发现了氟氯氰菊酯的血浆和组织浓度-时间数据符合两室开放模型。对于lamcyda-cyhalothrin,静脉输注后的消除半衰期(T(1 / 2beta))和从血浆的平均停留时间分别为7.55和8.55h。口服后10.27和14.43h。总血浆清除率不受剂量浓度或途径的影响,并达到0.060lh(-1)kg(-1)的值。在i.v.之后给药时,表观分布量和稳态时分别为0.68和0.53lkg(-1),表明拟除虫菊酯向组织扩散。口服后,lamcyda-cyhalothrin广泛但缓慢吸收(T(max),2.69h)。口服生物利用度为67.37%。观察到神经组织和血浆之间的动力学参数存在显着差异。下丘脑(C(max),24.12mugg(-1))和肌层神经丛(C(max),25.12mugg(-1))的最大浓度约为血浆(C(max),15.65mugml)的1.5倍(-1)),是肝脏的最高1.3倍(C(max),18.42mugml(-1))。氟氯氰菊酯的神经组织蓄积也通过组织/血浆(肝脏)的浓度曲线比率下的面积来反映。 lamcyda-cyhalothrin的T(1 / 2beta)对于包括神经肌肉纤维在内的神经组织的T(1 / 2beta)(静脉和口服给药后范围分别为12-26和15-34h)明显大于血浆(分别为7.55和10.27h) 。

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