单剂量与多剂量口服罗红霉素缓释片与普通片的犬体药物动力学研究

目的　研究健康家犬单剂量与多剂量口服罗红霉素(Rox)缓释片的药物动力学。方法　采用健康家犬 6只随机交叉单剂量与多剂量口服Rox缓释片与普通片 ,微生物法测定血药浓度 ,应用 3p97程序计算主要药动学参数 ,对AUC0～∞ 、AUC0～T或AUC0～τ的对数值进行方差分析、双单侧t检验等统计学处理 ,以 80 %～ 12 5 %为等效标准 ,评价缓释制剂与普通制剂的生物等效性。结果　单剂量时Rox缓释片的Tmax、Cmax、AUC0～T、AUC0～∞ 和MRT分别为(2 2 5± 0 99)h、(4 2 6± 1 70 )mg·L-1、(2 8 73± 10 4 6 )mg·h·L-1、(34 6 4± 9 5 7)mg·h·L-1和 (15 84± 1 6 3)h ,普通片的上述参数分别为 (1 33± 0 2 6 )h、(6 32± 2 79)mg·L-1、(2 8 6 8± 8 16 )mg·h·L-1、(34 4 9± 5 6 3)mg·h·L-1和 (12 95± 1 5 6 )h。多剂量达稳态时Rox缓释片的Tmax、Cmax、Cmin、AUC0～τ、AUC0～∞ 、Cav、DF和FI分别为(2 5 0± 0 4 5 )h、(4 38± 1 2 5 )mg·L-1、(0 4 9± 0 0 6 )mg·L-1、(2 4 91± 2 38)mg·h·L-1、(39 71± 6 4 8)mg·h·L-1、(1 0 4± 0 10 )mg·L-1、370 4 2 %± 98 4 1%和 15 7 36 %±11 86 % ,普通片的上述参数分别为 (1 4 2±0 38 )h、(6 13± 1 2 6 )mg·L-1、(0 4 3± 0

Pharmacokinetics of orally administered sustained release cupsles and conventional tablets of roxithromycin in dogs

Aim To study the pharmaco-rinetics of sustained release cupsles and conventional tablets of roxithromycin(Rox)in dogs.Methods The concentration of Rox was measured by bioassay after a single dose of the cupsles and multiple dose of conrentional tablets in dogs,the pharmacokinetic parameters of the two preparations were calculated by 3p87 program,the lnAUC 0-∞ or lnAUC 0-T were used to evaluate the bioequivalence of the two preparations with analysis of variance and two one side t-test.Results For the cupsles,the main pharmacokinetic parameters of T max,C max,AUC 0-T,AUC 0～∞ and MRT were(2.25±0.99) h and(1.33±0.26) h,(4.26±1.70) mg·L -1 and(6.32±2.79) mg·L -1,(28.73±10.46) mg·h·L -1 and(28.68±8.16) mg·h·L -1,(34.64±9.57) mg·h·L -1and(34.49±5.63) mg·h·L -1,(15.84±1.63)h and(12.95±1.56) h,respectively.For the conventional tablets,the steady state pharmacokinetic parameters of T max,C max,C min,AUC 0-T,AUC 0～∞,CT 1,DF and FI were(2.50±0.45) h and(1.42±0.38) h,(4.38±1.25) mg·L -1 and(6.13±1.26) mg·L -1,(0.49±0.06) mg·L -1 and(0.43±0.11) mg·L -1,(24.91±2.38) mg·h·L -1 and(23.30±2.06) mg·h·L -1,(39.71±6.48) mg·h·L -1 and(39.53±12.74) mg·h·L -1,(1.04±0.10) mg·L -1 and(0.97±0.09) mg·L -1,370.42%±98.41% and 585.77%±113.25%,157.36%±11.86% and 172.83%±8.34%,respectively.The lnAUC 0～∞or lnAUC 0～T were bioequivalent between Rox sustained release cupsles and conventional tablets.Conclusion The Rox cupsles have an obvious effect of sustaining release in dogs