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