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目的:建立人血浆中伪麻黄碱浓度的液相色谱-质谱测定法,进行人体药动学研究。方法:测定10名健康受试者口服受试制剂后血浆中伪麻黄碱浓度。结果:单剂量口服受试制剂(含伪麻黄碱120,240mg)后药动学参数T1/2β为(5.5±0.7)、(5.2±0.7)h,Tmax为(4.8±0.9)、(4.7±0.8)h,Cmax为(226.7±21.1)、(455.1±100.2)μg.L-1,CL为(41.0±18.6)、(43.9±15)L.h-1,V/F为(209.3±116.0)、(218.4±103.5)L,AUC(0-t)为(2929.9±474.9)、(5466.8±1372.6)μg.h.L-1,MRT为(10.2±0.7),(9.6±0.8)h。多剂量口服受试制剂(含伪麻黄碱120mg,bid)达稳态后药动学参数Csmsax为(272.0±52.6)μg.L-1,Csmsin为(105.0±37.2)μg.L-1,Cav为(198.6±39.0)μg.L-1,CL为(50.4±16.8)L.h-1,DF为(0.86±0.20),AUC(0-t)为(2382.6±467.4)μg.h.L-1。结论:本方法灵敏高,结果准确,伪麻黄碱在大部分人体内过程符合一室开放模型,其主要药动学参数与国内外文献相近,可为临床给药方案提供参考。
Objective: To establish a HPLC method for the determination of pseudoephedrine in human plasma and study the pharmacokinetics of human pseudo-ephedrine. Methods: The plasma concentrations of pseudoephedrine in 10 healthy subjects after oral administration of the test preparation were determined. Results: The pharmacokinetic parameters T1 / 2β were (5.5 ± 0.7), (5.2 ± 0.7) h, Tmax were (4.8 ± 0.9), (4.7 ± 0.8) h after a single oral dose of test compound (containing pseudoephedrine 120 and 240 mg) Cmax was (226.7 ± 21.1), (455.1 ± 100.2) μg.L-1, CL was (41.0 ± 18.6) and (43.9 ± 15) Lh-1, and V / F was 209.3 ± 116.0 and 218.4 ± 103.5) L, AUC (0-t) was (2929.9 ± 474.9), (5466.8 ± 1372.6) μg.hL-1, MRT was (10.2 ± 0.7), (9.6 ± 0.8) h. After reaching the steady state, Csmsax was (272.0 ± 52.6) μg.L-1 and Csmsin was (105.0 ± 37.2) μg.L-1 for multi-dose oral test preparations containing pseudoephedrine 120mg bid 198.6 ± 39.0) μg.L-1, CL was (50.4 ± 16.8) Lh-1, DF was (0.86 ± 0.20) and AUC (0-t) was (2382.6 ± 467.4) μg.hL-1. Conclusion: The method is sensitive and accurate. The process of pseudoephedrine conforms to the one-compartment open model in most human bodies. The main pharmacokinetic parameters of pseudoephedrine are similar to those of domestic and foreign literature, which can provide reference for clinical drug delivery.