本文選題：甲磺酸齊拉西酮 + 藥動(dòng)學(xué)�。� 參考：《中國(guó)藥學(xué)雜志》2017年09期

【摘要】：目的評(píng)價(jià)單次肌內(nèi)注射用抗精神病藥甲磺酸齊拉西酮的藥動(dòng)學(xué)特點(diǎn),評(píng)價(jià)該藥對(duì)于健康志愿者的安全性。方法 12名中國(guó)健康志愿者(男、女各6例)單劑量肌內(nèi)注射用甲磺酸齊拉西酮10 mg后在規(guī)定的時(shí)間點(diǎn)采血。采用LC-MS/MS檢測(cè)齊拉西酮的血藥濃度。根據(jù)血藥濃度計(jì)算藥動(dòng)學(xué)參數(shù)。另外通過(guò)體檢、實(shí)驗(yàn)室和心電圖檢查等項(xiàng)初步評(píng)估注射用甲磺酸齊拉西酮的安全性。結(jié)果血藥濃度-時(shí)間曲線為二室模型。藥動(dòng)學(xué)參數(shù)ρ_(max)為(97.85±29.24)ng·mL~(-1);t_(max)為(0.56±0.30)h;MRT為(5.35±0.96)h;t_(1/2)為(4.29±0.88)h;AUC_(0→t)為(405.6±98.68)ng·h·mL~(-1),AUC_(0→∞)為(413.3±100.69)ng·h·mL~(-1);CL為(25.50±6.10)L·h~(-1);Vd為(157.48±47.60)L;Kel為(0.168±0.035)h。男、女比較各參數(shù)的差異均無(wú)統(tǒng)計(jì)學(xué)意義。常見(jiàn)的不良事件為嗜睡、惡心和乏力,程度均為輕至中度。結(jié)論 12名健康受試者肌肉注射甲磺酸齊拉西酮注射液10mg后藥動(dòng)學(xué)參數(shù)與國(guó)外文獻(xiàn)報(bào)道結(jié)果基本一致。通過(guò)藥物不良事件說(shuō)明該藥物的鎮(zhèn)靜作用較強(qiáng),比較適用于興奮躁動(dòng)狀態(tài)的精神障礙。
[Abstract]:Objective to evaluate the pharmacokinetic characteristics of single intramuscular injection of ziprasidone mesylate and its safety in healthy volunteers. Methods Blood samples were collected from 12 healthy Chinese volunteers (6 males and 6 females) at a time point after 10 mg of ziprasidone mesylate for intramuscular injection. The plasma concentration of ziprasidone was detected by LC-MS / MS. Pharmacokinetic parameters were calculated according to blood concentration. In addition, the safety of ziprasidone mesylate for injection was preliminarily evaluated by physical examination, laboratory and electrocardiogram examination. Results the plasma concentration-time curve was a two-compartment model. 鑽姩瀛﹀弬鏁跋乢(max)涓，

本文編號(hào)：2049154