Pharmacokinetics differences between paclitaxel iiposome and injection in rabbits after intravenous injection

Objective To compare the pharmacokinetics of paclitaxel liposome and paclitaxel injection in rabbits after intravenous administration.Methods Paclitaxel liposome and paclitaxel injection were intravenously administrated to rabbits at a single dosage of 12 mg·h~(-1).The concentration-time data of paclitaxel in plasma samples were determined by HPLC-UV,and the pharmaeokinetic parameters were calculated and analyzed by DAS2.0 and SPSS12.0 software.Results The concentration-time data of paelitaxel liposome and paclitaxel injection were all fitted to two compartment-model,and the main pharmacokinetic parameters for paclitaxel liposome and paclitaxel injection were respectively as follows:t_(1/2α) were (1.206±0.205) and (0.538±0.236)h;t_(1/2α) were(33.560±6.685) and (12.187±1.255)h;V_d were(0.619±0.084)and(0.809±0.087) L;CL were(0.035±0.010)and(0.096±0.010)L·h~(-1);K_(10) were (0.043±0.010)and(0.134±0.020)h~(-1);K_(12) were(0.245±0.038)and(0.777±0.252)h~(-1);K_(21) were(0.321±0.058)and(0.594±0.193)h~(-1);AUC_(0→24) were(321.109±18.462) and (200.024±22.937)mg·h·L~(-1);AUC_(0→∞) were(722.195±170.360) and (272.300±38.568)mg·h·L~(-1).There were significantly differences in t_(1/2α),t(1/2β),V_d,CL,K_(10),K_(12),K_(21),AUC_(0→24) and AUC_(0→∞) between paclitaxel liposome and paclitaxel injection.Conclusion Paelitaxel liposome has higher efficacy,longer release time,higher target tissue concentration and lower side effect than paelitaxel injection.