罗红霉素颗粒剂在健康人体内的相对生物利用度

Relative bioavailability of roxithromycin granule in healthy volunteers

目的 :研究罗红霉素颗粒剂在健康人体内的相对生物利用度。方法 :采用微生物法测定 8名志愿者单剂量交叉口服 30 0mg罗红霉素颗粒剂和片剂后不同时间血清中的药物浓度。结果 :二者药 时曲线均符合二室模型 ,Cmax分别为 (1 1 4 0± 1 6 0 )mg·L-1和 (9 6 5± 1 2 6 )mg·L-1;Tmax分别为 (1 36± 0 2 4)h和 (1 71± 0 2 7)h ;T1/ 2 分别为 (1 2 88± 0 88)h和 (1 3 4 6± 0 95 )h ;AUC是 (1 1 1 1 8± 1 8 4 4)mg·h·L-1和 (1 0 8 91± 1 6 94)mg·h·L-1,罗红霉素颗粒剂的相对生物利用度为 (1 0 2 0 8± 8 0 2 ) % (88 0 1 %～ 1 1 5 5 3% )。结论

Aim: To study the relative bioavailability of roxithromycin granule.Methods: The roxithromycin concentrations in serum were determined by microbiological method after a single oral dose of roxithromycin granule and roxithromycin tablet were respectively given to 8 volunteers in an open randomized cross over test. Results: The concentration time curves of roxithromycin granule and tablet fitted to a two compartment open model. The C max was (11 40±1 60) mg·L -1 and (9 65±1 26) mg·L -1 ; T max was (1 36±0 24) h and (1 71±0 27) h; T 1/2 was (12 88±0 88) h and (13 46±0 95) h; AUC was (111 18±18 44) mg·h·L -1 and (108 91±16 94) mg·h·L -1 ,of roxithromycin granule and roxithromycin tablet respectively. The pharmacokinetic parameters obtained from our studies showed no significant difference between two formulations ( P >0 05). The relative bioavailability was (102 08±8 02)%(88 01%～115 53%) of roxithromycin granule. Conclusion: The results of statistical analysis suggest that the two formulations be bioequivalent.