Zhang Juan, Tang Yishan, Liu Qide
North China Pharmaceutical Group, New Drug Research and Development Co., Ltd., Shijiazhuang 050011, China.
Zhongguo Zhong Yao Za Zhi. 2010 Jul;35(13):1750-3. doi: 10.4268/cjcmm20101321.
To study the toxicokinetics and tissue distribution of total arsenic after giving different doses realgar to rats.
The concentration of arsenic in blood, urine and main organs were determined after single oral administration of 3.738, 1.869, 0.935 g x kg(-1) realgar in rats.
The distribution half life (t(1/2 alpha)) and elimination half life (t(1/2 beta)) of total arsenic were 7.73 h and 17.21 h respectively in high dose group. The apparent distribution volume (Vd) were 10.8, 5.6, 3.9 L x kg(-1) respectively, the total clearance (Cltot) were 0.437, 0.16, 0.111 L x h(-1) x kg(-1) respectively in the three groups. The excretion of total urine arsenic got rid of 5.5%-13.0% of realgar which given to rats in 96 hours. Arsenic could be detected distributing into rat's main organs and tissues after administration of a single dose. Suprarenal gland, bladder and ovary accumulated most of the arsenic, while liver, spleen, lung and kidney accumulated less. Heart, brain, stomach and testis accumulated the least amount.
It has nonlinear dynamics in the body of rats in toxic doses as the kinetics of realgar was changed according to the dosage.
研究给大鼠灌胃不同剂量雄黄后总砷的毒代动力学及组织分布情况。
大鼠单次口服3.738、1.869、0.935 g·kg⁻¹雄黄后，测定血液、尿液及主要脏器中砷的含量。
高剂量组总砷的分布半衰期（t₁/₂α）和消除半衰期（t₁/₂β）分别为7.73 h和17.21 h。三组的表观分布容积（Vd）分别为10.8、5.6、3.9 L·kg⁻¹，总清除率（Cltot）分别为0.437、0.16、0.111 L·h⁻¹·kg⁻¹。给药后96小时内，总尿砷排泄量占大鼠摄入雄黄量的5.5% - 13.0%。单次给药后可检测到砷分布于大鼠的主要脏器和组织中。肾上腺、膀胱和卵巢蓄积的砷最多，而肝、脾、肺和肾蓄积较少。心脏、脑、胃和睾丸蓄积量最少。
雄黄在大鼠体内呈非线性动力学特征，其动力学随剂量改变而变化。
