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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Neill E A, Chapple D J

Xenobiotica. 1982 Mar;12(3):203-10. doi: 10.3109/00498258209046795.

Atracurium is a novel bis-quaternary competitive neuromuscular blocking agent designed to undergo rapid non-enzymic inactivation at physiological pH and temperature. 2. Studies of [14C]atracurium in anaesthetized cats using h.p.l.c. techniques showed that the radioactivity eliminated in bile and urine was predominantly metabolites rather than unchanged drug. Both chemical decomposition and enzyme hydrolysis products were observed in vivo. 3. The plasma elimination half life of atracurium after administration via the jugular vein was c. 20 min. Similar results were obtained if the drug was given via the hepatic portal vein or in animals with bilateral renal ligation. These studies indicate that atracurium is rapidly inactivated in vivo and that neither the liver nor the kidneys play a major role in its metabolism or elimination, in accord with the premise on which the drug molecule was designed.

阿曲库铵是一种新型的双季铵竞争性神经肌肉阻滞剂，设计用于在生理pH值和温度下快速进行非酶失活。2. 使用高效液相色谱技术对麻醉猫体内的[14C]阿曲库铵进行的研究表明，胆汁和尿液中消除的放射性主要是代谢产物，而非未变化的药物。体内观察到了化学分解产物和酶水解产物。3. 通过颈静脉给药后，阿曲库铵的血浆消除半衰期约为20分钟。如果通过肝门静脉给药或在双侧肾结扎的动物中给药，也会得到类似结果。这些研究表明，阿曲库铵在体内迅速失活，肝脏和肾脏在其代谢或消除过程中均不起主要作用，这与该药物分子的设计前提一致。

Neill E A, Chapple D J

Xenobiotica. 1982 Mar;12(3):203-10. doi: 10.3109/00498258209046795.

Atracurium is a novel bis-quaternary competitive neuromuscular blocking agent designed to undergo rapid non-enzymic inactivation at physiological pH and temperature. 2. Studies of [14C]atracurium in anaesthetized cats using h.p.l.c. techniques showed that the radioactivity eliminated in bile and urine was predominantly metabolites rather than unchanged drug. Both chemical decomposition and enzyme hydrolysis products were observed in vivo. 3. The plasma elimination half life of atracurium after administration via the jugular vein was c. 20 min. Similar results were obtained if the drug was given via the hepatic portal vein or in animals with bilateral renal ligation. These studies indicate that atracurium is rapidly inactivated in vivo and that neither the liver nor the kidneys play a major role in its metabolism or elimination, in accord with the premise on which the drug molecule was designed.

阿曲库铵是一种新型的双季铵竞争性神经肌肉阻滞剂，设计用于在生理pH值和温度下快速进行非酶失活。2. 使用高效液相色谱技术对麻醉猫体内的[14C]阿曲库铵进行的研究表明，胆汁和尿液中消除的放射性主要是代谢产物，而非未变化的药物。体内观察到了化学分解产物和酶水解产物。3. 通过颈静脉给药后，阿曲库铵的血浆消除半衰期约为20分钟。如果通过肝门静脉给药或在双侧肾结扎的动物中给药，也会得到类似结果。这些研究表明，阿曲库铵在体内迅速失活，肝脏和肾脏在其代谢或消除过程中均不起主要作用，这与该药物分子的设计前提一致。