OBJECTIVE To study the pharmacokinetics and biodistribution of pur derivative nanopaticles 4ac in mice. METHOD After intravenous administration of 15 mg x kg(-1) of pur derivative 4ac, the plasma and tissue concentration was detected by HPLC. The pharmacokinetics parameters were calculated by the method of 3p97. RESULT The concentration time curves were conformed to two compartment model. The Re of 4ac nanopaticles was 21.18 times higher than suspension. CONCLUSION Our present study demonstrates that, compared to nanopaticles and suspension, nanopaticles significantly alter the pharmacokinetics in plasma and tissues targeting. Biodistribution of pur derivative 4ac nanopaticles in heart of mice was better than 4ac suspension. It will become a new drug for cardiovascular disease therapy.