摘要
目的探讨布洛芬和安定混合溶液的药理学特征.方法在确认布洛芬与安定两药相混后理化性质无变化前提下,以单药作比较,评价该混合溶液动物直肠用药后的药代动力学及药效学.结果两药相混后的外观及含量与混合前无显著差异.该混合液分别在 20℃～ 25℃、 37℃～ 40℃下贮存 2月,外观及含量稳定,而在 3℃～ 5℃贮存后有少量结晶析出致含量降低,提示该混合液适合常温保存.该混合液连续多次直肠给药后对大鼠直肠粘膜无明显刺激作用.经直肠施予该混合液后,布洛芬(或安定)在各时点的血药浓度及各项药动学参数( Tlag、 Tmax、 Cmax、 AUC、 T1/2)与单用时不存在显著性差异,都在约 12 min(或 10 min)迅速达到峰浓度,其止惊退热疗效也分别与两单药应用时无显著差异.结论布洛芬和安定溶液混和制剂,对两单药的理化性质、药代动力学以及止惊或退热疗效均无显著影响.
Objective To explore the pharmacological feature of a mixed soluble preparation consisting of ibuprofen and diazepam. Methods Based on the confirmation that there were no physical and chemical alterations of each drug after mixing, the pharmacokinetic and pharmacodynamic alternations of the preparation were investigated after administration through rectum to rabbits or to rats, and compared with those when ibuprofen or diazepam used alone. Results The appearance and content of each drug in the mixed solution did not changed. The mixed solution was stable stored at 20℃ -25℃or at 37℃ -40℃ for two months, and just a little crystal was found when it was stored at 3℃ - 5℃. There were no obviously pathological changes in the rectal tissues after repeat administration through rectum with the mixed solution. In comparison with ibuprofen or diazepam used alone, there were no significant differences in the plasma concentration of ibuprofen or diazepam at all time points and in all of the tested pharmacokinetic parameters （Tlag, Tmax, Cmax, AUC, T1/2） when the mixed solution administered through rectum. The peak concentrations were reached rapidly in about 12 mins（for ibuprofen）and 10 mins（for diazepam）,respectively,after the administration. The antipyretic and antionvulsion effects of the mixed solution had no significant changes in comparison with diazepam or ibuprofen used alone. Conclusions In comparison with ibuprofen or diazepam used alone, there are no significant influences on the physical and chemical nature and on the pharmacokinetic and pharmcodynamic features of the drugs when they are used as a mixed soluble preparation.
出处
《临床儿科杂志》
CAS
CSCD
北大核心
2005年第10期737-740,共4页
Journal of Clinical Pediatrics
关键词
布洛芬
安定
溶液
动物
相互作用
ibuprofen diazepam solution animal interaction
