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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2012, Vol. 17 ›› Issue (6): 672-676.

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Clinical Phase I Pharmacokinetics of rhproUK

SONG Hai-jing1, YANG Wei-zhi2, ZHANG Zhuo-mei3, OU Lun4, Chen Fang4, Wang Qing-qing4, DONG Li-hou4, LIU Xiu-wen4   

  1. 1emergency Medicine Department of the 306th hospital, PLA, Beijing 100105, China;
    2Department of Orthopedics, Tenth People's hospital of Shanghai, Tongji University, Shanghai 200072, China;
    3Department of Gynaecology and Obstetrics, General Hospital of People's Armed Police Forces, Beijing 100039, China;
    4Department of Pharmacology and Toxicology, Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
  • Received:2012-04-05 Revised:2012-06-13 Online:2012-06-26 Published:2012-06-25

Abstract: AIM: To investigate pharmacokinetics of rhproUK in healthy subjects. METHODS: ELISA and ELISA combined with chromogenic substrated method were used to determinate the plasma concentration of uPA, sc-uPA and plasminogen activity. RESULTS: The ratio of AUC of uPA and sc-uPA is 1∶2.1 ∶3.3 and 1 ∶1.9 ∶2.9 after single administration of rhproUK in the healthy subjects at the dose of 20,40 and 60 mg per person,AUC and Cmax increase with dosage increasment, there are no significant difference in CLS、VSS、MRT、t1/2 and tmax between three groups.The increasment of AUC and Cmax in plasminogen activity are more than the increasment proportion of dosage, the ratio of Cmax and AUC is 1∶2.3∶3.9 and 1∶2.9∶4.7, showed non-linear increasment. CLS and Vd reduce with dosage increasement. CONCLUSION: The course of u-PA, sc-uPA in healthy subjects fitted with the linear pharmacokinetics model in the range from 20 to 60 mg per person, But plasminogen activity showed slightly non-linear pharmacokinetics.

Key words: Single chain urokinase-type plasminogen activator, Pharmacokinetics, ELISA, Blood drug concentration

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