本文選題：甲磺酸齊拉西酮 + 藥動學　； 參考：《中國藥學雜志》2017年09期

【摘要】：目的評價單次肌內(nèi)注射用抗精神病藥甲磺酸齊拉西酮的藥動學特點,評價該藥對于健康志愿者的安全性。方法 12名中國健康志愿者(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)定的時間點采血。采用LC-MS/MS檢測齊拉西酮的血藥濃度。根據(jù)血藥濃度計算藥動學參數(shù)。另外通過體檢、實驗室和心電圖檢查等項初步評估注射用甲磺酸齊拉西酮的安全性。結(jié)果血藥濃度-時間曲線為二室模型。藥動學參數(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)的差異均無統(tǒng)計學意義。常見的不良事件為嗜睡、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后藥動學參數(shù)與國外文獻報道結(jié)果基本一致。通過藥物不良事件說明該藥物的鎮(zhèn)靜作用較強,比較適用于興奮躁動狀態(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：2049154