本文選題：尼索地平 + 控釋貼劑��； 參考：《中國(guó)藥房》2015年28期

【摘要】：目的:建立尼索地平控釋貼劑(NCRP)在自發(fā)性高血壓大鼠(SHR)體內(nèi)的藥動(dòng)學(xué)-藥效學(xué)(PK-PD)結(jié)合模型。方法:將SHR隨機(jī)分為貼劑(NCRP)組和片劑(尼索地平片)組,每組6只,植入微透析探針,按尼索地平計(jì)每只給藥5 mg。收集給藥后36 h內(nèi)的血漿微透析液,采用高效液相色譜法測(cè)定尼索地平血藥濃度,Win Nonlin 5.3軟件計(jì)算藥動(dòng)學(xué)參數(shù),以心率和血壓為藥效學(xué)指標(biāo),進(jìn)行PK-PD結(jié)合模型研究。結(jié)果:與尼索地平片比較,NCRP具有控釋效果;NCRP藥物效應(yīng)與效應(yīng)室濃度以Sigmoid-Emax模型擬合,心率和收縮壓的PK-PD模型主要參數(shù)分別為Emax:(2.65±0.06)、(10.71±0.87),EC50:(83.65±35.25)、(1.29±0.26)ng/ml,γ:(0.83±0.91)、(1.2±0.35),Keo:(0.37±0.53)、(0.91±0.24)h-1。結(jié)論:成功建立了NCRP在SHR體內(nèi)的PK-PD結(jié)合模型。
[Abstract]:Aim: to establish a pharmacokinetic-pharmacodynamic PK-PD-binding model of nisoldipine controlled-release patch (NCRP) in spontaneously hypertensive rats (SHRs). Methods: SHR were randomly divided into two groups: patch group (n = 6) and tablet group (n = 6). Microdialysis probes were implanted into each group and each group was given 5 mg of nisoldipine. Plasma microdialysate was collected within 36 hours after administration. The plasma concentration of nisoldipine was determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were calculated by software win Nonlin 5.3. The PK-PD binding model was studied with heart rate and blood pressure as pharmacodynamic indexes. Results: compared with nisoldipine tablets, the drug effect of NCRP and the concentration of NCRP were fitted by Sigmoid-Emax model. The main parameters of PK-PD model of heart rate and systolic blood pressure were Emaxurus 2.65 鹵0.06GV, EC50: 83.65 鹵35.251.29 鹵0.26ng / ml, 緯: 0.83 鹵0.91g / ml, 緯: 0.83 鹵0.351g / ml, 緯: 0.83 鹵0.91kew 0.37 鹵0.53h-1, respectively. The main parameters of PK-PD model of heart rate and systolic blood pressure were: Emax 2.65 鹵0.87g / L EC50 鹵35.251.29 鹵0.26 ng / ml, 緯: 0.83 鹵0.91g / ml, r: 0.83 鹵0.91g / ml, r = 0.83 鹵0.91g / ml, respectively. Conclusion: the PK-PD binding model of NCRP in SHR was successfully established.
【作者單位】： 廣東省中藥研究所;廣東食品藥品職業(yè)學(xué)院;中山大學(xué)工學(xué)院;
【基金】：廣東省醫(yī)學(xué)科研基金(No.B2012063)
【分類(lèi)號(hào)】：R965

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