头孢呋辛酯片剂在健康志愿受试者体内生物等效性的研究  

Bioequivalance of cefuroxime axetil tablets in the human healthy volunteers

作　　者：吕万良[1] 张强[1] 赵甘霖[1] 孙华东[1] 张大卫[1] 马付勇[1] 刘欣 李洁 高晔 

机构地区：[1]北京大学药学院药剂学研究室,北京100083

出　　处：《北京医科大学学报》2000年第3期244-247,共4页Journal of Peking University(Health Sciences)

摘　　要：研究国内研制的头孢呋辛酯片剂与参比制剂 (西力欣 )在健康人体内的生物利用度与生物等效性。方法 :用高效液相 紫外法测定血浆中的头孢呋辛的浓度 ,以头孢呋辛酯的市售片剂西力欣为对照 ,通过 2 2名受试者的单剂量交叉给药 ,对研制的头孢呋辛酯片剂进行相对人体生物利用度及生物等效性考察。结果 :研制的头孢呋辛酯片剂和西力欣片的AUC[0 ∞ ] 分别为 (12 .7± 4.5 )和 (13.2± 4.8)mg·L-1·h ;Cmax分别为 (3.5± 1.2 )和(3 .9± 1.7)mg·L-1;Tmax分别为 (1.9± 0 .9)和 (2 .2± 1.0 )h ;MRT分别为 (3 .9± 1.3)和 (3 .8± 1.5 )h ;T1/ 2 分别为(2 .3± 1.8)和 (1.9± 1.7)h。说明研制的头孢呋辛酯片和西力欣片的各种主要的药物动力学参数接近。研制的头孢呋辛酯片的相对生物利用度 (F)达到 95 .42 %。研制的头孢呋辛酯片剂和参比制剂西力欣片的AUC[0 ∞ ] 之间差异无显著性 (P >0 .0 5 ) ,90 %的置信区间在 80 %～ 12 5 %范围内 ;Cmax的 90 %置信区间也在 70 %～ 143 %的范围内。结论 :研制的头孢呋辛酯片和市售进口的西力欣片在健康人体内达生物等效。Objective:To study the bioequivalence between the generic cefuroxime axetil tablets and the commericial ones (Zinacef tablets). Methods: An HPLC UV method was established to determine the concentrations of cefuroxime axetil following oral administration of the two preparations. A single dosage crossover design was applied and 22 male healthy volunteers were included in this trial after the informed consent agreement was signed for each. Results: The mobile phase was acetonitril 0.05 mol·L -1 sodium dihydrogen phosphate (11:89, volume fraction), the flow rate 1.5 ml·min -1 and the determination wavelength 273 nm. The main pharmacokinetic parameters of generic tablets, AUC [0 ∞] , C max , T max , MRT, T 1/2 , were (12.7±4.5)mg·L -1 ·h,(3.5±1.2) mg·L -1 ,(1.9± 0.9 ) h, (3.9±1.3) h,and (2.3±1.8) h,respectively. The relative bioavailability of generic tablets was 95.42% compared with that of Zinacef tablets. No significant differences were found between the AUC [0 ∞] of the two preparations according to statistical methods of the two one side t test, etc.. Conclusion: The bioequivalence can be reached between the generic cefuroxime axetil tablets and the Zinacef ones.

关 键 词：头孢呋辛酯片 生物利用度 治疗等效 药代动力学 

分 类 号：R978.11[医药卫生—药品] R969.1[医药卫生—药学]