头孢克肟口腔崩解片与胶囊在健康人体内生物利用度比较

Comparison of Relative Bioavailability between Disintegration Tablets and Capsules of Cefixime in Healthy Volunteers

目的比较头孢克肟口腔崩解片与头孢克肟胶囊在健康志愿者体内的药动学及生物等效性。方法采用开放、随机、自身交叉对照试验法,20例男性健康受试者分别单剂量口服试验制剂200 mg或参比制剂200 mg。用高效液相色谱(HPLC)法测定血清中头孢克肟的浓度,并拟合药动学参数,以双单侧t检验法比较两种头孢克肟制剂AUC、Cmax、tmax之间的差异。结果头孢克肟口腔崩解片与头孢克肟胶囊在健康志愿者体内的主要药动学参数平均值:AUC分别为(19.438±9.400)和(21.220±9.751)mg.h.L-1;Cmax分别为(2.614±0.931)和(2.811±1.030)mg.L-1;tmax分别为(3.499±0.596)和(3.314±0.825)h。两种头孢克肟制剂各主要药动学参数间均差异无显著性(P>0.05)。头孢克肟口腔崩解片对头孢克肟胶囊的相对生物利用度为(110.14±12.70)%。结论两种头孢克肟制剂具有相同的生物效应。

Objective To compare the pharmacokinetic parameters and relative bioavailability between disintegration tablets and capsules of cefixime. Methods An open, randomized, two-period crossover study was conducted in 20 healthy volunteers after a single dosage of 200 mg cefixime or reference one orally. Concentration of cefixime in serum was assayed by HPLC method. The pharmacokinetics parameters were calculated, and AUC, Cmax and tmax were analyzed by two one-sided t test. Results The AUC, Cmax and tmax of disintegration tablets and capsules were （ 19. 438 ± 9. 400 ） and （ 21. 220 ± 9. 751） mg · h · L^-1 , （2. 614 ± 0. 931 ） and （2. 811 ± 1. 030） mg·L^-1, （ 3. 499 ±0. 596） and （3. 314 ± 0. 825） h, respectively. The main pharmacokinetics parameters of cefixime between two groups were corresponding （ P 〉 0.05 ）. The relative bioavailability of cefixime disintegration tablets was （ 110. 14 ± 12.70 ） %. Conclusion The disintegration tablets and capsules of cefixime are bioequivalent.