单次肌内注射用甲磺酸齐拉西酮在中国健康志愿者中的药动学研究

发布时间：2018-06-21 15:02

  本文选题：甲磺酸齐拉西酮 + 药动学　； 参考：《中国药学杂志》2017年09期

【摘要】：目的评价单次肌内注射用抗精神病药甲磺酸齐拉西酮的药动学特点,评价该药对于健康志愿者的安全性。方法 12名中国健康志愿者(男、女各6例)单剂量肌内注射用甲磺酸齐拉西酮10 mg后在规定的时间点采血。采用LC-MS/MS检测齐拉西酮的血药浓度。根据血药浓度计算药动学参数。另外通过体检、实验室和心电图检查等项初步评估注射用甲磺酸齐拉西酮的安全性。结果血药浓度-时间曲线为二室模型。药动学参数ρ_(max)为(97.85±29.24)ng·mL~(-1);t_(max)为(0.56±0.30)h;MRT为(5.35±0.96)h;t_(1/2)为(4.29±0.88)h;AUC_(0→t)为(405.6±98.68)ng·h·mL~(-1),AUC_(0→∞)为(413.3±100.69)ng·h·mL~(-1);CL为(25.50±6.10)L·h~(-1);Vd为(157.48±47.60)L;Kel为(0.168±0.035)h。男、女比较各参数的差异均无统计学意义。常见的不良事件为嗜睡、恶心和乏力,程度均为轻至中度。结论 12名健康受试者肌肉注射甲磺酸齐拉西酮注射液10mg后药动学参数与国外文献报道结果基本一致。通过药物不良事件说明该药物的镇静作用较强,比较适用于兴奋躁动状态的精神障碍。
[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�鍔ㄥ�﹀弬鏁跋乢(max)涓，

本文编号：2049154