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本研究系比较CT与其水解产物——DSA对大鼠的利尿作用并探讨DSA在大鼠体内的转化、吸收、分布和排泄。大鼠口服20及100毫克/公斤时DSA的利尿及排氯作用与CT相同,口服CT或DSA 4毫克/公斤后,则作用均不明显。水解前后比色或纸层分析都证明服药后的大鼠尿中没有DSA的乙酰化产物或其他代谢产物。口服DSA 20毫克/公斤后,药物被迅速吸收,1、3、9小时的胃腸道含药量分别为口服剂量的55、20及12％。大鼠口服DSA 4—100毫克/公斤后,3小时内自尿排出剂量的30％左右,口服CT4毫克/公斤后同时期内排出剂量的34％,但加大剂量到20及100毫克/公斤时,仅排出剂量的17—18％。反之,静脉注射20毫克/公斤后,CT自尿排出比DSA迅速。自胆汁排出的药量少于口服剂量的1％。大鼠口服DSA 20毫克/公斤后1小时,药物在肾脏分布最多,肝次之。但总的说来,本药在各脏的浓度较趋平均。
This study compared the diuretic effects of CT and its hydrolyzate - DSA in rats and explored the transformation, absorption, distribution and excretion of DSA in rats. DSA diuresis and chloral hydrate in rats at oral doses of 20 and 100 mg / kg were the same as those of CT, and no significant effect was observed after 4 mg / kg oral CT or DSA. Colorimetric or paper layer analysis before and after hydrolysis demonstrated that there was no acetylated or other metabolites of DSA in the urine of rats after administration. After oral DSA 20 mg / kg, the drug was rapidly absorbed, and the gastrointestinal drug concentrations at 1, 3 and 9 hours were 55, 20 and 12% of the oral dose, respectively. Rat oral DSA 4-100 mg / kg, within 3 hours from urinary discharge dose of about 30%, oral CT4 mg / kg 34% of the same period after the discharge dose, but to increase the dose to 20 and 100 mg / kg Only 17-18% of the dose is excreted. Conversely, after intravenous injection of 20 mg / kg, CT excreted faster than DSA from the urine. The dose of bile is less than 1% of the oral dose. One hour after oral administration of DSA 20 mg / kg, the drug was most distributed in the kidneys and followed by the liver. But in general, the average concentration of the drug in the more average.