摘要:
目的 比较头孢克肟胶囊、片剂与世福素胶囊(市售头孢克肟胶囊)在健康人体内的相对生物利用度。方法 采用三制剂、三周期交叉试验设计,用反相高效液相色谱法测定21名健康受试者单剂量口服400mg孢克肟胶囊及片剂以及世福素胶囊后头孢克肟的血药浓度。用3P87程序计算药动学参数。将AUC、Cmax进行对数转换后进行方差分析并计算90%可信区间。结果 头孢克肟胶囊与片剂和世福素胶囊的主要药动学参数分别为:AUC0→t(27.29±8.76)μg/mL·h、(28.12±8.91)μg/mL·h和(27.76±8.25)μg/mL·h,AUC0→∞(28.12±9.1 1)μg/mL·h、(28.98±9.33)μg/mL·h和(28.72±8.78)μg/mL·h,tmax(4.004±0.36)h、(4.00±0.35)h和(4.00±0.37)h,Cmax(4.75±1.21)μg/mL、(4.76±1.05)μg/mL和(4.75±1.10)μg/mL,t1/2分另4为(2.704±0.38)h、(2.65±0.57)h和(2.78±0.61)h,MRT0-1分别为(5.52±0.60)h、(5.57±0.59)h和(5.54±0.57)h。以世福素胶囊为参比,头孢克肟胶囊和片剂生物利用度F0-1为(98.23±10.47)%和(101.12±10.58)%。F0→∞为(97.96±10.39)%和(100.81±10.60)%。结论 方差分析及双单侧t检验表明,三种制剂具有生物等效性。
Abstract:
Objective To compare the bioavailability of cefixime tablets and capsules with Cefspan's (marketed cefixime capsules) in human subjects. Methods A reversed-phase high performance liquid chromatography was used for the determination of cefixime in plasma after a single oral dose of 400mg cefixime tablets,capsules and cefspan in a crossover design. Results The pharmaco-kinetic parameters of cefixime tablets, capsules and cefspan are as follows: AUC0→1(27.29±8.76)μg/mL·h,(28.12±8.91)μg/mL·h and(27.76±8.25)μg/mL·h,AUC0→∞(28.12±9.11)μg/mL·h,(28.98 ±9.33)μg/mL·h and(28.72±8.78)μg/mL·h,tmax(4.00±0.36)h,(4.00±0.35)h and (4.00±0.37)h.Cmax(4.75±1.21)μg/mL,(4.76±1.05)μg/mL and(4.75 ±1.10)μg/mL,t1/2(2.70±0.38)h, (2.65±0.57)h and (2.78±0.61)h, MRT0-T(5.52±0.60)h, (5.57±0.59)h and (5.54±0.57)h. Conclusion The cefixime capsules and tablets are bioequivalent with Cefspan.
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