曲马朵药物树脂缓释混悬剂小鼠药效学与药动学研究  

Studies on pharmacokinetics and pharmacodynamics of tramadol-resin sustained release suspension in mice

作　　者：张志燕[1] 平其能[1] 叶晓霞[1] 

机构地区：[1]中国药科大学药剂教研室,江苏南京210009

出　　处：《中国药学杂志》2001年第6期399-402,共4页Chinese Pharmaceutical Journal

基　　金：国家‘九五’攻关资助项目 !(96-90 2 -0 2 -0 5 )

摘　　要：目的　以小鼠为模型动物 ,研究曲马朵药物树脂缓释混悬剂的药效学与药动学 ,并对二者之间的关系进行初步探讨。方法　以小鼠扭体反应抑制率为药效指标 ,用HPLC 荧光法检测小鼠血药浓度 ,并用PKAnalys软件对血药浓度经 时数据进行拟合。结果　缓释制剂在药效上存在明显的剂量依赖性 ;与同剂量普通制剂相比 ,缓释制剂镇痛作用维持时间明显延长 ;药动学研究结果表明 ,二者体内分布配置符合单室模型 ,普通制剂Ka为 4.89h-1,缓释制剂Ka为 0 .99h-1,后者具有较好的缓释效果 ;相对生物利用度为 91.32 % ,与普通制剂生物等效。结论　药动 药效 (PK PD)关系研究表明 ,普通制剂为“单调变化型” ,药效与血药浓度经时过程基本同步 ;缓释制剂为“逆时针履历型” 。OBJECTIVE: To study the pharmacokinetics(PK) and pharmacodynamics(PD) of tramadol-resin sustained release(SR) suspension and to evaluate the relationship between them. METHODS: The inhibition rate(IR)of mouse torsion-body(TB) was used as the index of PD; The serum concentration of tramadol was determined by HPLC-fluorescence assay. The data were fitted with PKAnalys software. RESULTS: Compared with the solution, the analgesic duration of SR suspension was consistent with significantly increased(7 h vs 4 h). The PD of SR. suspension was dose - dependent; The disposition in vivo was single-compartment model. The main PK parameters of SR suspension and solution were Ka 0.99 h-1 and 4.89 h-1, respectively; the effect of SR suspension was satisfactory and bioequivalent to the solution. CONCLUSION: The relationship between PK and PD of SR suspension and solution was counterclockwise hysteresis and monotonous variation respectively.

关 键 词：曲马朵 缓释混悬剂 药效学 药动学 小鼠 

分 类 号：R971.1[医药卫生—药品] R969.1[医药卫生—药学]