[关键词]
[摘要]
目的 探讨麝香保心pH依赖型梯度释药微丸和麝香保心丸的药效动力学参数。方法 以大鼠心肌营养性血流量为效应指标进行测定。结果 麝香保心丸在大鼠体内呈一室模型特征 ,其最低起效剂量为0.54mg/kg,效应呈现半衰期为0.53h,效应消除半衰期为1.21h,药效作用期为3.48h,效应达峰时间为 1.13h,效量吸收半衰期为0.23h,消除半衰期为1.47h,达峰时间为0.88h。统计矩结果表明麝香保心pH依赖型梯度释药微丸和麝香保心丸的平均效应维持时间分别为5.05h和2.33h,效量平均滞留时间分别为7.70 h和3.21h,麝香保心pH依赖型梯度释药微丸的效量相对生物利用度为104.03%。结论 麝香保心丸在体内具有吸收快、消除快和作用维持时间较短的特点 ,而麝香保心pH依赖型梯度释药微丸在体内具有起效迅速、药效持久、缓和的特征。
[Key word]
[Abstract]
Object To investigate the pharmaco kinetic parameters of Musk Protecting Heart Pellets with pH-dependent gradient-release (MPHP-pH) and Musk Protecting Heart Pills (MPHP) . Methods The cardiac muscle nutritional blood flow in rat was measured as effective index. Results It was one-compartment model when the rat was ig M PHP. The minimal effecting dose was 0.54 mg/kg ,the present half-life, the elimination half-life, medicinal effect and the peak time of effective action were 053, 1.21,3.48 and 1.13h , respectively. The absorption half-life, elimination half-life and peak time of effective dose were 0.23, 1.47 and 0.88 h, respectively. Stati stical moment analysis showed that the mean residence time mean residence time (MRT) of effective action were 5.05 h for MPHP-pH and 2.33 h for MPHP, the MRT of effective dose were 7.70 h for MPHP-pH and 3.21 h for MPHP. The relative bioavailability of effective dose for MPHP-pH was 104. 03% . Conclusion MPHP has the characteri stics of fast abso rption, fast elimination and short effective action time. Whereas MPHP-pHhas the characteristics of fast absorption, protonged and relaxed effective action compared with MPHP.
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[基金项目]
辽宁省博士启动基金资助课题(No.2001102042)