论文部分内容阅读
大鼠静脉注射 PAT 15毫克/公斤,一小时内胆汁排锑量为给药量的29±13%,平均锑浓度为399±122微克/毫升,如在给 PAT 前先静脉注射 BSP 50毫克/公斤,则锑排泄率降为2±2%(P<0.001)。抑制程度与 BSP 的剂量及给药时间有关。大鼠静脉注射 BSP 15毫克/公斤,先收集胆汁一小时,再注射 PAT 30毫克/公斤及第二次 BSP15毫克/公斤,又收集胆汁一小时,结果实验组及对照组的 BSP 排泄率:第一次各为给药量的81±11%及75±7%,第二次各为47±14%及95±12%。给 PAT 后BSP 排泄率较对照组及自身对照期显著降低(P 值均<0.01)。上速竞争抑制现象在其他类型锑剂及酸性染料间也能获得证明。静脉注射(月弟)波芬,Sb-58或锑铵,剂量分别为40、20及17毫克/公斤,一小时内胆汁排锑率各为16.5±12.6%,6.45±4.4%及8.4±3.0%。若在给锑剂前先给 BSP 50毫克/公斤,则锑排泄率分别降至1.4±0.5%,1.9±1.2%及1.3±0.2%。大鼠结扎肾动静脉后注射 PAT 15毫克/公斤,一小时内胆汁排锑率为32±6%,若在给 PAT 前分别先注射50毫克/公斤溴甲酚绿或酚红,或100毫克/公斤萤光黄,则锑排泄率分别降至8±6%,17±12%及4±1%。家兔注射 PAT 或(月弟)波芬后,胆汁中锑在纸电泳时系向阳极泳动,且泳动速率变慢,证明锑剂代谢产物仍是阴离子,但已非原来的 PAT 或(月弟)波芬。对上述结果作了讨论,初步认为 PAT 经代谢后形成新的锑络合物,以阴离子形式,经肝—胆汁的酸性物质转运机构,通过特殊转运进入胆汁。
The rats were injected with 15 mg / kg of PAT intravenously and the amount of antimony in the gallbladder was 29 ± 13% of the dose within one hour with an average antimony concentration of 399 ± 122 μg / ml. For example, BSP 50 mg / Kg, the antimony excretion rate was reduced to 2 ± 2% (P <0.001). The degree of inhibition is related to the dose of BSP and the administration time. The rats were intravenously injected with BSP 15 mg / kg, bile for one hour, PAT 30 mg / kg and second BSP 15 mg / kg, and bile for another hour. Results The BSP excretion rate in the experimental and control groups was Each dose was 81 ± 11% and 75 ± 7% for the second dose of 47 ± 14% and 95 ± 12%. The BSP excretion rate after PAT was significantly lower than that of control group and self-control period (P <0.01). Propelling competitive inhibition is also evidenced in other types of antimony and acid dyes. Bovine, antimony Sb-58 or antimony was intravenously administered at monthly doses of 40, 20 and 17 mg / kg and the bile antimony rejection rates were 16.5 ± 12.6%, 6.45 ± 4.4% and 8.4 ± 3.0 in one hour %. Antimony excretion rates dropped to 1.4 ± 0.5%, 1.9 ± 1.2% and 1.3 ± 0.2%, respectively, for BSP 50 mg / kg prior to the antimony agent. Rat ligation of the renal artery and vein after injection of PAT 15 mg / kg, one hour bile antimony rejection rate of 32 ± 6%, respectively, before giving PAT to 50 mg / kg bromocresol green or phenol red, or 100 mg / Kg fluorescent yellow, the antimony excretion rate dropped to 8 ± 6%, 17 ± 12% and 4 ± 1%, respectively. Anti-bile antimony in the bile was electrophoresed on the anode when the paper was electrophoresed and the migration rate was slow, which proves that the antimony agent metabolite is still an anion, but the original PAT or ( Month brother) Bo Fen. The above results were discussed, initially believed that the metabolism of PAT after the formation of new antimony complexes, in the form of anions, the liver - bile of the acidic material transport mechanism, through special transport into the bile.