pH敏感型口服原位凝胶在Beagle犬体内的药物动力学

Pharmacokinetics of pH-sensitive in situ gel in Beagle dogs

目的研究pH敏感型布洛芬口服原位凝胶(IBU-ISG)在Beagle犬体内的药物动力学。方法用RP-HPLC法测定6只Beagle犬口服IBU-ISG和布洛芬混悬液(100mg)后不同时间血浆中布洛芬的浓度,计算药物动力学参数。结果IBU-ISG与布洛芬混悬液的药物动力学参数分别为:tmax为(1.75±0.63)和(0.42±0.13)h,ρmax为(29.19±7.65)和(37.77±2.23)mg·L-1,t1/2为(2.30±0.53)和(2.02±0.91)h,tMR0-∞为(4.27±0.80)和(3.26±1.00)h,AUC0-t为(131.05±38.64)和(117.30±23.07)mg·h·L-1。结论布洛芬pH敏感型口服原位凝胶较布洛芬混悬液释药缓慢。

Objective To study the pharmacokinetics of ibuprofen pH-sensitive in situ gel(IBU-ISG) in Beagle dogs.Methods A single dose of IBU-ISG and IBU suspension(100 mg) were given orally to 6 healthy Beagle dogs in a randomized crossover design.Ibuprofen concentration in the plasma at different sampling time was determined by RP-HPLC.The pharmacokinetic parameters were calculated.Results tmax of IBU-ISG and IBU suspension were(1.75±0.63) h and(0.42±0.13) h;ρmax values were(29.19±7.65) mg·L-1 and(37.77±2.23) mg·L-1;t1/2 were(2.30±0.53) h and(2.02±0.91) h;tMR0-∞ were(4.27±0.80) h and(3.26±1.00) h,and AUC0-t were(131.05±38.64) mg·h·L-1 and(117.30± 23.07) mg·h·L-1,respectively.Conclusions The tmax,ρmax and tMR0-∞ of the two preparations were significantly different,while their AUCs were comparable.The IBU-ISG has longer residence time compared with IBU suspension.