FU Qianga�� LIAO Quanb�� YE Mina�� ZHOU Taob�� ZHU Zhua�� ZHAO Yu-peib*
Peking Union Medical College Hospital�� Chinese Academy of Medical Sciences-Peking Union Medical College��a.Department of Pharmacy�� b.Department of General Surgery�� Beijing 100730�� China
Abstract��
OBJECTIVE To study the PK/PD of cefoperazone (CPZ in pancreatic tissue of patients using population pharmacokinetic sampling model. METHODS Blood and tissue samples were obtained simultaneously in pancreatectomy during 0-12 h after 45 min infusion administration of 2 g SUPERAZON�j (1 g CPZ�� 1 g Sul in 26 patients. CPZ concentrations in plasma and tissue were determined by HPLC. The PK behavior and parameters were analyzed using WinNonlin(v5.2 program. The dynamic penetration ratios (PR0-12 h�� Ctissue/Cplasma�� penetration index (PI�� AUCtissue/AUCplasma�� and %T>MIC were calculated�� respectively. RESULTS The PK process of CPZ in plasma and tissue complied with one-compartment model. The tmax�� ��max�� AUC0-12 and t1/2 of CPZ in plasma and tissue were 0.75 and 4.0 h�� 83.50 mg��L-1 and 23.25 mg��kg-1�� 298.82 mg��h��L-1 and 98.08 mg��h��kg-1�� 2.21 and 2.82 h�� respectively. The average PR0-12 h and PI were ��41.55��21.38% and 32.82%�� and the %T>MIC of CPZ in plasma and tissue were 81.3% and 50.0% when MIC=8�� 62.5% and 33.3% when MIC=16�� respectively. CONCLUSION The elimination phase of CPZ in plasma was similar to that in pancreatic tissue. After 45 min infusion administration of 2 g SUPERAZON�j�� effective concentrations were obtained and maintained for 12 h in pancreatic tissue and plasma�� and bactericidal efficacy was achieved for the treatment of pancreatitis and also for the prophylaxis of wound infection after pancreatectomy.
.Pharmacokinetics and Pharmacodynamics of Cefoperazone and Its Penetration into Pancreatic Tissue in Patients[J] Chinese Pharmaceutical Journal, 2011,V46(6): 447-449