李铜铃, 庞其捷, 贺于玲, 王平. 肝靶向抗疟药半乳糖基拟糖白蛋白-伯氨喹偶联物和磷酸伯氨喹的药代动力学J. 药学学报, 1995, 30(10): 721-725.
引用本文: 李铜铃, 庞其捷, 贺于玲, 王平. 肝靶向抗疟药半乳糖基拟糖白蛋白-伯氨喹偶联物和磷酸伯氨喹的药代动力学J. 药学学报, 1995, 30(10): 721-725.
TLLi, QJ Pang, YL He , P Wang, . STUDY OF PHARMACOKINETICS OF LIVER TARGETING ANTIMALARIAL AGENT NEOGLYCOALBUMIN-PRIMAQUINE CONJUGATE(NGA-PQ)AND PRIMAQUINE PHOSPHATE IN MOUSEJ. Acta Pharmaceutica Sinica, 1995, 30(10): 721-725.
Citation: TLLi, QJ Pang, YL He , P Wang, . STUDY OF PHARMACOKINETICS OF LIVER TARGETING ANTIMALARIAL AGENT NEOGLYCOALBUMIN-PRIMAQUINE CONJUGATE(NGA-PQ)AND PRIMAQUINE PHOSPHATE IN MOUSEJ. Acta Pharmaceutica Sinica, 1995, 30(10): 721-725.

肝靶向抗疟药半乳糖基拟糖白蛋白-伯氨喹偶联物和磷酸伯氨喹的药代动力学

STUDY OF PHARMACOKINETICS OF LIVER TARGETING ANTIMALARIAL AGENT NEOGLYCOALBUMIN-PRIMAQUINE CONJUGATE(NGA-PQ)AND PRIMAQUINE PHOSPHATE IN MOUSE

  • 摘要: 用HPLC法对肝靶向抗疟药NGA-PQ各磷酸伯氨喹(PQP)在小鼠体内的药代动力学行为进行了比较研究。结果表明NGA-pQ在血中有较好的稳定性,不易解离出PQ。NGA-PQ和PQP在肝中的Tm分别为10和15min,在血中的T1/2分别为20.44和35.74min。在肝中的T1/2分别为43.95和21.46min,肝中的AUC分别为2305.80和333.29min·μg-1·g-1。说明NGA-PQ在血中很快消除并浓集于肝脏,在肝脏的保留时间长,从而证实NGA-PQ具肝靶向分布特性。

     

    Abstract: A normal phase high-performance liquid chromatography process was used to separate and detect primaquine in blood and liver after a single intravenous dose of the hepatictargeting agent neoglycoalbumine-primaquine conjugate(NGA-PQ)and primaquine phosphate (PQP)in mice.6-Methoxy-8-(4-amino- butyrylamino ) quinoline synthesized and identified by us was usedas an internal standard to be added to biologic samples obtained from mice at different times after givenNGA-PQ or PQP.The mixture was extracted with ether after alkalinization in the PQP group. In theNGA- PQ group ,the biological samples must be hydrolized by heating under nitrogen and acidcondition in a domestic pressure cooker before extraction. The extracts were evaporated to drynessunder nitrogen ,then dissolved in the mobile phase(chloroform-methanol-amonium hydroxide=86.8:12.5:0.7).The results showed that the hepatic PQ collecting ratio and the retention time ofPQ in liver in the NGA-PQ group were higher and longer than those in the PQP group. The resultsalso point out that NGA-PQ has liver targeting property.

     

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