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目的:研究盐酸奥普力农葡萄糖注射液在健康人体内的药动学。方法:采用拉丁方三交叉自身随机对照试验,对12例志愿受试者(男女各半)于不同试验周期静脉推注低(5μg·kg-1)、中(10μg·kg-1)、高(20μg·kg-1)3个单负荷剂量盐酸奥普力农葡萄糖注射液。采用HPLC-MS/MS法测定血浆中奥普力农(olprinone,OLP)浓度,用PhoenixTMWin Nonlin 6.1药动学软件计算主要药动学参数;测定中剂量组尿液中OLP的浓度,计算各时间段尿药排泄率。结果:推注3个剂量的盐酸奥普力农葡萄糖注射液后,主要药动学参数为:Cmax分别为(17.74±9.82),(40.31±11.80)和(75.00±31.52)μg·L-1,Tmax分别为(7.92±3.96),(5.42±1.44)和(5.00±0.00)min,t1/2分别为(61.20±14.42),(72.01±14.40)和(69.87±14.48)min,AUC0-t分别为(463.01±105.88),(849.54±149.23)和(1 758.35±378.46)μg·L-1·min-1,AUC0-∞分别为(470.64±106.65),(863.46±153.24)和(1 783.07±388.52)μg·L-1·min-1。中剂量(10μg·kg-1)组24 h尿药累积排泄率为(61.79±5.46)%。结论:盐酸奥普力农葡萄糖注射液在5~20μg·kg-1剂量范围内可能具有线性动力学特征。中剂量24 h的尿药累积排泄率为(61.79±5.46)%,表明盐酸奥普力农主要经肾脏清除。
Objective: To study the pharmacokinetics of ophthalmic acid hydrochloride injection in healthy volunteers. Methods: A randomized controlled trial of Latin square three-crosses was conducted. Twelve volunteers (half male and half female) were intravenously injected with low (5 μg · kg -1), medium (10 μg · kg -1) (20μg · kg-1) three single-loading doses of ophthalmic acid hydrochloride injection. The plasma concentrations of olprinone (OLP) were determined by HPLC-MS / MS. The main pharmacokinetic parameters were calculated by using the PhoenixTMWin Nonlin 6.1 pharmacokinetic software. The concentrations of OLP in the urine of the middle-dose group were measured and the time Paraquat urinary excretion rate. Results: The main pharmacokinetic parameters were as follows: Cmax were (17.74 ± 9.82), (40.31 ± 11.80) and (75.00 ± 31.52) μg · L-1 after bolus injection of three doses of ophthalmic acid dextrose injection , Tmax were (7.92 ± 3.96), (5.42 ± 1.44) and (5.00 ± 0.00) min respectively, and t1 / 2 were (61.20 ± 14.42), (72.01 ± 14.40) and (69.87 ± 14.48) min respectively. The AUC0-t (463.01 ± 105.88), (849.54 ± 149.23) and (1 758.35 ± 378.46) μg · L-1 · min-1 respectively, and the AUC0-∞ were (470.64 ± 106.65), (863.46 ± 153.24) and ± 388.52) μg · L-1 · min-1. The cumulative urinary excretion rate of 24 h urinary drug in the medium dose (10 μg · kg -1) group was (61.79 ± 5.46)%. CONCLUSION: Oplinid Hydrochloride Glucose Injection may have a linear kinetic characteristic in the range of 5 ~ 20μg · kg-1. Urine accumulative excretion rate in the middle dose of 24 h was (61.79 ± 5.46)%, indicating that the main obsidian hydrochloride was cleared by the kidneys.