国产与进口头孢泊肟酯在健康人体的药代动力学和生物等效性

Pharmacokinetics and bioequivalence of domestic and imported cefpodoxime proxetil preparitions in healthy volunteers

目的研究国产与进口头孢泊肟酯在健康人体内的药代动力学与生物等效性。方法24名健康受试者按拉丁方分成3组,用自身交叉对照单次空腹口服进口和国产头孢泊肟酯片和头孢泊肟酯干混悬剂200mg,用微生物法测定人体血药浓度。结果进口头孢泊肟酯片(参比)和国产头孢泊肟酯片剂、干混悬剂(受试)的Cmax分别为(3.52±0.76),(3.62±0.90)和(3.67±0.58)mg·L-1;tmax分别为(2.8±0.4),(2.8±0.5)和(2.5±0.5)h;t1/2分别为(2.3±0.3),(2.4±0.3)和(2.4±0.3)h;AUC0-t分别为(19.12±5.08),(19.42±4.59)和(20.15±3.56)mg·h·L-1。3种制剂的Cmax、AUC0-t均无显著性差异(P>0.05)。国产头孢泊肟酯片、干混悬剂相对于进口头孢泊肟酯片的生物利用度分别为(104.2±21.4)%和(108.3±16.8)%。结论国产头孢泊肟酯片剂、干混悬剂与进口头孢泊肟酯片剂具有生物等效性。

Objective To study the pharmacokinetics and bioequivalence of domestic and imported preparations of cefpodoxime proxetil. Methods Plasma concentration of cefpodoxime was determined by microbiologic assay. Twenty-four volunteers were distributed into three groups by latin square design with a single oral dose of 200 mg of domestic cefpodoxime tablet (test) and domestic suspension preparation of cefpodoxime proxetil (test), and imported cefpodoxime tablet(reference). Results The pharmacokinetic parameters of the three preparations were as follow: C max of the two test drugs and one referrence drug were (3.52±0.76), (3.62±0.90) and (3.67±0.58) mg·L -1 respectively, t max were (2.8±0.4), (2.8±0.5) and (2.5±0.5) h respectively,t 1/2 were (2.3±0.3), (2.4±0.3) and (2.4±0.3) h respectively,and AUC 0-t were (19.12±5.08), (19.42±4.59) and (20.15±3.56) mg·h·L -1 respectively. There were no significant differences in C max and AUC 0-t between the three preparations (P>0.05). The relative bioavailability of the domestic cefpodoxime tablet was (104.2±21.4)%, and that of domestic suspension preparation of cefpodoxime proxetil was (108.3±16.8)% respectively. Conclusion The two tested preparations were of bioequivalence to the refference preparation.