目的:建立头孢他啶血浆浓度的测定方法,并评价注射用头孢他啶试验与参比制剂是否生物等效。方法:20名健康男性志愿者随机分为2组,采用开放、随机、双周期、自身对照交叉试验设计,对受试者进行单次肌内注射给药,两周期间的洗脱期为3d;采用高效液相色谱法测定头孢他啶经时血药浓度,利用DAS Ver2.0程序计算药动学参数并进行统计分析。结果:头孢他啶参比制剂(含头孢他啶1.0g)和试验制剂(含头孢他啶1.0g)的主要药动学参数Cmax分别为(27.5±5.5)mg.L-1和(27.6±5.4)mg.L-1,tmax分别为(1.2±0.5)h和(1.2±0.5)h,t1/2分别为(2.3±0.4)h和(2.15±0.26)h,AUC0-10分别为(115.3±16.8)mg.L-1.h和(108.2±19.5)mg.L-1.h,AUC0-∞分别为(122.4±16.7)mg.L-1.h和(113.7±20.2)mg.L-1.h。2组间Cmax、AUC0-10、AUC0-∞、tmax的差异均无显著性(P>0.05);试验制剂的Cmax、AUC0-10和AUC0-∞的90%可信区间均未超出参比制剂的80%～125%范围。试验制剂对参比制剂的相对生物利用度F为(93.9±11.2)%,RSD为11.9%。结论:头孢他啶血药浓度测定的方法适用;试验制剂与参比制剂具有生物等效性。 OBJECTIVE: To establish a method for the determination of ceftazidime in plasma and evaluate the bioequivalence of ceftazidime test and reference preparations. Methods: Twenty healthy male volunteers were randomly divided into two groups. The subjects were given a single intramuscular injection with an open, randomized, double-cycle, self-controlled crossover design. The elution period was two days The plasma concentration of ceftazidime was determined by HPLC. The pharmacokinetic parameters were calculated by DAS Ver2.0 program and analyzed statistically. Results: The main pharmacokinetic parameters of ceftazidime (including ceftazidime 1.0g) and test preparations (containing ceftazidime 1.0g) were (27.5 ± 5.5) mg.L-1 and (27.6 ± 5.4) mg.L- 1, tmax were (1.2 ± 0.5) h and (1.2 ± 0.5) h respectively, and t1 / 2 were (2.3 ± 0.4) h and (2.15 ± 0.26) h respectively. The AUC0-10 was (115.3 ± 16.8) mg. L-1.h and (108.2 ± 19.5) mg.L-1.h and AUC0-∞ were (122.4 ± 16.7) mg.L-1.h and (113.7 ± 20.2) mg.L-1.h respectively. There were no significant differences in Cmax, AUC0-10, AUC0-∞ and tmax between the two groups (P> 0.05). The 90% confidence intervals of Cmax, AUC0-10 and AUC0-∞ of the test formulation did not exceed the reference formulation Of the 80% ~ 125% range. The relative bioavailability of the test formulation to the reference formulation was F (93.9 ± 11.2)% and RSD was 11.9%. Conclusion: The method of determination of ceftazidime blood concentration is applicable; the bioequivalence of test preparation and reference preparation is validated.