头孢克肟咀嚼片与胶囊的相对生物利用度比较

Comparison of relative bioavailability between cefixime mastication tablets and capsules

目的 :比较头孢克肟咀嚼片与胶囊在健康人体内的相对生物利用度。方法 :反相高效液相色谱法测定 2 0例健康受试者随机交叉单剂量口服4 0 0mg头孢克肟咀嚼片以及胶囊后头孢克肟的血药浓度 ,3P87程序计算药动学参数 ,并对AUC ,Cmax进行方差分析及双单侧t检验。结果 :头孢克肟咀嚼片和胶囊的主要药动学参数分别为 :AUC0 ∞(2 9±s 10 ) ,(30± 9)mg·h·L- 1;AUC0 16 (2 8± 9) ,(2 8± 9)mg·h·L- 1;Tmax(4 .0± 0 .4 ) ,(4 .0± 0 .3)h ;Cmax(4 .8± 1.1) ,(4 .8± 1.1)mg·L- 1,T1/ 2(3.2± 0 .5 ) ,(3.0± 0 .4 )h ;MRT0 16 (5 .8± 0 .6 ) ,(5 .8± 0 .6 )h。以头孢克肟胶囊为参比 ,头孢克肟咀嚼片相对生物利用度F0 16 为 (98± 8) % ,F0 ∞ 为(98± 8) %。结论

AIM: To compare the relative bioavailability between cefixime mastication tablets and capsules in human. METHODS: The study was performed with 20 healthy male volunteers according to a randomized 2 ways crossover design. A reversed-phase high performance liquid chromatography was used for determination of the plasma concentration of cefixime after single dose oral administration of cefixime mastication tablet or capsule (400 mg). The pharmacokinetic parameters were counted by 3P87 program and AUC, C_(max) were measured by the analysis of variance and t tests. RESULTS: The main pharmacokinetic parameters of cefixime mastication tablets and capsules were as follows: AUC_(0-∞)(29±s 10), (30±9) mg·h·L^(-1); AUC_(0-16)(28±9), (28±9) mg·h·L^(-1); T_(max)(4.0±(0.4)), (4.0±0.3) h; C_(max)(4.8±1.1),(4.8±1.1) mg·L^(-1); T_(1/2)(2.5±0.5), (2.5±(0.4)) h; MRT_(0-16)((5.8±)0.6), (5.8±0.6) h. The relative bioavailability of cefixime mastication tablets was F_(0-16)(98±8) % and F_(0-∞)(98±8) %. CONCLUSION: The cefixime mastication tablets and capsules are bioequivalent.