【摘要】 目的研究(1∶1)头孢哌酮(第3代头孢类抗生素)/舒巴坦(β内酰胺酶抑制剂)在成年与老年的药代动力学。方法44名健康受试者(成年:男12人,女12人;老年:男20人)每次静脉给予头孢哌酮和舒巴坦各1g,每日2次,连续给药3天,第4天首次给药后,采集不同时间的血样,分离血清,用HPLC方法分别测定头孢哌酮和舒巴坦的血药浓度。结果舒巴坦:稳态时,成年男性、女性和老年人的CL分别为(30.6±5.2),(29.3±4.3),(13.7±4.9)L·h-1;Vd分别为(49.7±21.2),(58.8±23.1),(28.7±15.7)L;t1/2分别(1.2±0.5),(1.4±0.4),(1.4±0.4)h;Cmax分别(27.9±4.8),(26.5±4.3),(54.7±19.9)mg·L-1;AUC分别(33.7±6.74),(34.7±4.64),(81.8±28.4)mg·h·L-1。头孢哌酮:稳态时,成年男性、女性和老年人的CL分别为(5.7±1.2),(4.8±1.3),(4.2±1.2)L·h-1;Vd分别为(11.7±2.7),(11.7±4.6),(12.8±3.8);t1/2分别为(1.5±0.5),(1.7±0.4),(2.2±0.6)h;Cmax分别为(89.4±10.7),(110.8±24.7),(102.0±15.3)mg·L-1;AUC分别(182.3±49.6),(224.7±60.7),(256.3±72.0)mg·h·L-1。结论成年人和老年人的药代动力学中,舒巴坦存在明显差异;而头孢哌酮的差异不明显;两性间的药代动力学差异不明显。更多还原

【Abstract】 Objective To study the pharmacokinetics of cefoperazone and sulbactam (1∶1) in healthy adult and old people. Methods Of the 44 volunteers enrolled, 24 were adults(male 12, female 12), 20 were male old people. Volunteers were iv given 1g cefoperazone and 1g sulbactam q.d, for 3 consecutive days. On day 4, blood samples were taken at different time intervals after the first administration.Serum was separated and HPLC methods were used to determine the concentrations of cefoperazone and sulbactam in serum.Results Sulbactam:at steady state, the paremerters for male adults, female adults and old people were as follows:CL were (30.6±5.2),(29.3±4.3),(13.7±4.9) L·h -1;V_d were (49.7±21.2),(58.8±23.1),(28.7±15.7) L;t_ 1/2 were (1.2±0.5),(1.4±0.4),(1.4±0.4) h; C_ max were (27.9±4.8),(26.5±4.3),(54.7±19.9) mg·L -1;AUC were (33.7±6.74),(34.7±4.64),(81.8±28.4) mg·h·L -1 respectively. Cefoperazone: at steady state , the paremerters for male adults, female adults, and old people were as follows: CL were (5.7±1.2),(4.8±1.3),[LM]( 4.2±1.2) L·h -1;V_d were (11.7±2.7),(11.7±4.6),(12.8±3.8) L; t_ 1/2 were (1.5±0.5),(1.7±0.4),(2.2±0.6) h; C_ max were (89.4±10.7),(110.8±24.7),(102.0±15.3) mg·L -1;AUC were (182.3±49.6),(224.7±60.7),(256.3±72.0) mg·h·L -1 respectively. Conclusion There were significant differences in pharmacokinetic parameters of sulbactam between adults and old people. While the differences in the pharmacokinetic parameters of cefoperazone were not significant in these two groups. The sexual difference between male and female adults was not significant either.更多还原