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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2012, Vol. 17 ›› Issue (12): 1433-1440.

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Research on the pharmacokinetics of prodrugs

ZHU Yin-ci, SUN Jian-guo, PENG Ying, WANG Guang-ji   

  1. Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China
  • Received:2012-04-19 Revised:2012-07-26 Published:2012-12-31

Abstract: Prodrugs are chemicals with little or no pharmacological activity, which can be changed to therapeutically active metabolite after undergoing biotransformation in vivo. The design of prodrugs has become an important way to overcome the shortcomings of drugs such as poor solubility, low bioavailability, short elimination half-life, devoid of ideal targets and so on. However, there still lacks criteria to evaluate pharmacokinetic properties of prodrugs. This paper reviews the pharmacokinetic profiles of various types of prodrugs in recent years, and proposes full evaluation from absorption, distribution, metabolism and excretion perspectives.

Key words: Prodrug, Pharmacokinetics, Biotransform

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