A Comparative Study of Pharmacokinetic Characteristics between Paclitaxel Liposomes for Injection and Commecial Paclitaxel Injection in Chinese Tumor Patients

OBJECTIVE To provide a theoretical basis for rational use of drug in clinic and get the messages of the rules of absorption,distribution and elimination of paclitaxel liposomes in human by comparing pharmacokinetic characteristics between the two formulations of paclitaxel in single intravenous infusion.METHODS A combinative design included monocycle and cross over design(two periods) was employed.The patients received a single dose of 175 mg·m-2 paclitaxel liposomes and paclitaxel injection,respectively.The blood samples collected were determined by HPLC-MS/MS.RESULTS The main pharmacokinetic parameters of paclitaxel liposome and paclitaxel injection were as follows: ρmax(883.11±353.69) and(6 250.00±1 635.12) μg·L-1,tmax were(1.94±1.01) and(3.00±0)h,t1/2(5.00±1.87) and(3.37±0.61)h.AUC0-tn(2 828.40±1 113.36) and(17 304.28±5 064.30) μg·h·L-1,AUC0-∞(3 077.96±1 195.39) and(17 400.43±5 053.15) μg·h·L-1.The 4 examples which completed the cross over design test got the main pharmacokinetic parameters as follows: The mean ρmax(767.75±182.94) and(6 805.00±881.38)μg·L-1,tmax(2.50±1.0) and(3.00±0)h,t1/2(5.16±2.42) and(3.30±0.88) h,AUC0-tn were(2 675.39±385.24) and(18 036.51±5 239.99) μg·h·L-1,AUC0-∞(2 913.80±238.66) and(18 186.84±5 187.37) μg·h·L-1.CONCLUSION The ρmax and AUC0-tn of paclitaxel liposome were lower than paclitaxel injection and t1/2 higher than paclitaxel injection obviously in the same doses.Compared with paclitaxel injection,paclitaxel liposome had the obvious effect of delayed release.